PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 21289522-1 2011 BACKGROUND: AT-101 is an inhibitor of Bcl-2 family proteins including Bcl-2, Bcl-xL, Mcl-1, and Bcl-w. gossypol acetic acid 12-18 BCL2 apoptosis regulator Homo sapiens 38-43 22112969-0 2012 Randomized phase II trial of docetaxel plus prednisone in combination with placebo or AT-101, an oral small molecule Bcl-2 family antagonist, as first-line therapy for metastatic castration-resistant prostate cancer. gossypol acetic acid 86-92 BCL2 apoptosis regulator Homo sapiens 117-122 22112969-1 2012 BACKGROUND: AT-101 (A), a small molecule oral inhibitor of the Bcl-2 family, has activity alone and in combination with docetaxel (Taxotere) and prednisone (DP) in metastatic castration-resistant prostate cancer (mCRPC). gossypol acetic acid 12-18 BCL2 apoptosis regulator Homo sapiens 63-68 22411600-0 2012 Pretreatment with AT-101 enhances tumor necrosis factor-related apoptosis-inducing ligand (TRAIL)-induced apoptosis of breast cancer cells by inducing death receptors 4 and 5 protein levels. gossypol acetic acid 18-24 TNF superfamily member 10 Homo sapiens 34-89 22411600-0 2012 Pretreatment with AT-101 enhances tumor necrosis factor-related apoptosis-inducing ligand (TRAIL)-induced apoptosis of breast cancer cells by inducing death receptors 4 and 5 protein levels. gossypol acetic acid 18-24 TNF superfamily member 10 Homo sapiens 91-96 22411600-2 2012 AT-101, an (-)-enantiomer of gossypol, is a potent anticancer agent that is shown to be an inhibitor of Bcl-2/Bcl-XL. gossypol acetic acid 0-6 BCL2 apoptosis regulator Homo sapiens 104-109 22411600-2 2012 AT-101, an (-)-enantiomer of gossypol, is a potent anticancer agent that is shown to be an inhibitor of Bcl-2/Bcl-XL. gossypol acetic acid 0-6 BCL2 like 1 Homo sapiens 110-116 22411600-11 2012 CONCLUSIONS: These findings all together, strongly suggest that pretreatment with AT-101 enhances TRAIL-induced death-inducing signaling complex resulting in the engagement of the mitochondrial pathway to apoptosis in breast cancer cells. gossypol acetic acid 82-88 TNF superfamily member 10 Homo sapiens 98-103 22171982-0 2012 Downregulation of BCL2 by AT-101 enhances the antileukaemic effect of lenalidomide both by an immune dependant and independent manner. gossypol acetic acid 26-32 BCL2 apoptosis regulator Homo sapiens 18-22 22171982-7 2012 This effect was further enhanced with pre-treatment of tumour cells with AT-101 (a BH3 mimetic that functions as BCL2 antagonist). gossypol acetic acid 73-79 BCL2 apoptosis regulator Homo sapiens 113-117 23185240-0 2012 Pan-Bcl-2 inhibitor AT-101 enhances tumor cell killing by EGFR targeted T cells. gossypol acetic acid 20-26 BCL2 apoptosis regulator Homo sapiens 4-9 23185240-0 2012 Pan-Bcl-2 inhibitor AT-101 enhances tumor cell killing by EGFR targeted T cells. gossypol acetic acid 20-26 epidermal growth factor receptor Homo sapiens 58-62 23185240-5 2012 We found that pretreatment of tumor cells with AT-101 enhanced susceptibility of L3.6pl and MiaPaCa-2 tumor cells to ATC and aATC-mediated cytotoxicity, which was in part mediated via enhanced release of cytolytic granule GrzB from ATC and aATC. gossypol acetic acid 47-53 granzyme B Homo sapiens 222-226 23185240-7 2012 Priming (conditioning) of PC cells with AT-101 can significantly enhance the anti-tumor activity of EGFRBi armed ATC through increased IFN-gamma induced activation of pS(727)-Stat1 and inhibition of pY(705)-Stat3 phosphorylation, and resulting in increased ratio of pro-apoptotic to anti-apoptotic proteins. gossypol acetic acid 40-46 interferon gamma Homo sapiens 135-144 23185240-7 2012 Priming (conditioning) of PC cells with AT-101 can significantly enhance the anti-tumor activity of EGFRBi armed ATC through increased IFN-gamma induced activation of pS(727)-Stat1 and inhibition of pY(705)-Stat3 phosphorylation, and resulting in increased ratio of pro-apoptotic to anti-apoptotic proteins. gossypol acetic acid 40-46 signal transducer and activator of transcription 1 Homo sapiens 175-180 21505732-0 2011 [Gossypol acetic acid induces DNA double-strand breaks in human mucoepidermoid carcinoma cell MEC-1]. gossypol acetic acid 1-21 ATR serine/threonine kinase Homo sapiens 94-99 21505732-1 2011 The present study was conducted to investigate the effects of gossypol acetic acid (GAA) on the proliferation of human mucoepidermoid carcinoma cell line MEC-1 in vitro and its possible molecular mechanisms of DNA double-strand breaks (DSB). gossypol acetic acid 62-82 alpha glucosidase Homo sapiens 84-87 21505732-1 2011 The present study was conducted to investigate the effects of gossypol acetic acid (GAA) on the proliferation of human mucoepidermoid carcinoma cell line MEC-1 in vitro and its possible molecular mechanisms of DNA double-strand breaks (DSB). gossypol acetic acid 62-82 ATR serine/threonine kinase Homo sapiens 154-159 21289522-1 2011 BACKGROUND: AT-101 is an inhibitor of Bcl-2 family proteins including Bcl-2, Bcl-xL, Mcl-1, and Bcl-w. gossypol acetic acid 12-18 BCL2 apoptosis regulator Homo sapiens 70-75 21289522-1 2011 BACKGROUND: AT-101 is an inhibitor of Bcl-2 family proteins including Bcl-2, Bcl-xL, Mcl-1, and Bcl-w. gossypol acetic acid 12-18 BCL2 like 1 Homo sapiens 77-83 21289522-1 2011 BACKGROUND: AT-101 is an inhibitor of Bcl-2 family proteins including Bcl-2, Bcl-xL, Mcl-1, and Bcl-w. gossypol acetic acid 12-18 MCL1 apoptosis regulator, BCL2 family member Homo sapiens 85-90 21289522-1 2011 BACKGROUND: AT-101 is an inhibitor of Bcl-2 family proteins including Bcl-2, Bcl-xL, Mcl-1, and Bcl-w. gossypol acetic acid 12-18 BCL2 like 2 Homo sapiens 96-101 21289522-19 2011 AT-101 is the first oral, pan Bcl-2 family inhibitor to exhibit a possible survival benefit in a randomized study. gossypol acetic acid 0-6 BCL2 apoptosis regulator Homo sapiens 30-35 21357440-7 2011 TRA-8 combined with AT-101 or BH3I-2", inhibitors of antiapoptotic Bcl-2 proteins, produced synergistic cytotoxicity against ZR-75-1, BT-474, and T47D cells. gossypol acetic acid 20-26 BCL2 apoptosis regulator Homo sapiens 67-72 20832445-1 2010 Gossypol acetic acid (GAA) displays anti-fertility and antioxidant behavior. gossypol acetic acid 0-20 alpha glucosidase Rattus norvegicus 22-25 20808253-1 2010 INTRODUCTION: AT-101 is an oral, pan Bcl-2 family protein inhibitor that has demonstrated activity in small cell lung cancer (SCLC) models. gossypol acetic acid 14-20 BCL2 apoptosis regulator Homo sapiens 37-42 20589722-8 2010 VCaP cells treated with AT-101 demonstrated an increase in apoptosis and downregulation of Bcl-2 pro-survival proteins. gossypol acetic acid 24-30 BCL2 apoptosis regulator Homo sapiens 91-96 19556859-11 2009 AT-101, which also neutralizes Mcl1, had single-agent cytotoxicity, further augmented by Mcl1 knockdown. gossypol acetic acid 0-6 MCL1 apoptosis regulator, BCL2 family member Homo sapiens 31-35 20354451-0 2010 AT-101, a pan-Bcl-2 inhibitor, leads to radiosensitization of non-small cell lung cancer. gossypol acetic acid 0-6 BCL2 apoptosis regulator Homo sapiens 14-19 20030926-6 2009 At the same time, gossypol acetic acid could also down-regulate the mitochondrial membrane potential, up-regulate the expression of the apoptosis-related protein such as BAX and caspase-3. gossypol acetic acid 18-38 BCL2 associated X, apoptosis regulator Homo sapiens 170-173 20030926-6 2009 At the same time, gossypol acetic acid could also down-regulate the mitochondrial membrane potential, up-regulate the expression of the apoptosis-related protein such as BAX and caspase-3. gossypol acetic acid 18-38 caspase 3 Homo sapiens 178-187 19852810-0 2009 AT-101, a small molecule inhibitor of anti-apoptotic Bcl-2 family members, activates the SAPK/JNK pathway and enhances radiation-induced apoptosis. gossypol acetic acid 0-6 BCL2 apoptosis regulator Homo sapiens 53-58 19852810-0 2009 AT-101, a small molecule inhibitor of anti-apoptotic Bcl-2 family members, activates the SAPK/JNK pathway and enhances radiation-induced apoptosis. gossypol acetic acid 0-6 mitogen-activated protein kinase 9 Homo sapiens 89-93 19852810-0 2009 AT-101, a small molecule inhibitor of anti-apoptotic Bcl-2 family members, activates the SAPK/JNK pathway and enhances radiation-induced apoptosis. gossypol acetic acid 0-6 mitogen-activated protein kinase 9 Homo sapiens 94-97 19852810-10 2009 Like radiation, AT-101 activated SAPK/JNK which was blocked by the kinase inhibitor SP600125. gossypol acetic acid 16-22 mitogen-activated protein kinase 9 Homo sapiens 33-37 19852810-10 2009 Like radiation, AT-101 activated SAPK/JNK which was blocked by the kinase inhibitor SP600125. gossypol acetic acid 16-22 mitogen-activated protein kinase 9 Homo sapiens 38-41 19852810-12 2009 CONCLUSION: Our data show that AT-101 strongly enhances radiation-induced apoptosis in human leukemic cells and indicate a requirement for the SAPK/JNK pathway in AT-101-induced apoptosis. gossypol acetic acid 163-169 mitogen-activated protein kinase 9 Homo sapiens 143-147 19852810-12 2009 CONCLUSION: Our data show that AT-101 strongly enhances radiation-induced apoptosis in human leukemic cells and indicate a requirement for the SAPK/JNK pathway in AT-101-induced apoptosis. gossypol acetic acid 163-169 mitogen-activated protein kinase 9 Homo sapiens 148-151 19556859-11 2009 AT-101, which also neutralizes Mcl1, had single-agent cytotoxicity, further augmented by Mcl1 knockdown. gossypol acetic acid 0-6 MCL1 apoptosis regulator, BCL2 family member Homo sapiens 89-93 17597109-9 2007 Furthermore, an intraperitoneal injection of GOS or gossypol acetic acid (GAA) significantly reduced the growth of colorectal carcinoma induced by a subcutaneous injection of COLO205 cells in nude mice. gossypol acetic acid 52-72 alpha glucosidase Homo sapiens 74-77 18836097-0 2009 AT-101 induces apoptosis in CLL B cells and overcomes stromal cell-mediated Mcl-1 induction and drug resistance. gossypol acetic acid 0-6 MCL1 apoptosis regulator, BCL2 family member Homo sapiens 76-81 18836097-3 2009 Because AT-101 binds to the BH3 motif of all Bcl-2-family antiapoptotic proteins, we hypothesized that this molecule could overcome resistance. gossypol acetic acid 8-14 BCL2 apoptosis regulator Homo sapiens 45-50 18836097-6 2009 However, AT-101 induced similar extent of down-regulation of Mcl-1 and apoptosis in CLL lymphocytes cultured in suspension or on stroma (P = .999). gossypol acetic acid 9-15 MCL1 apoptosis regulator, BCL2 family member Homo sapiens 61-66 18346839-2 2008 R-(-)-gossypol (AT-101) is a small molecule that mimics the BH3 domain of cellular Bcl-2 inhibitors and interferes with the function of prosurvival Bcl-2 proteins. gossypol acetic acid 16-22 BCL2 apoptosis regulator Homo sapiens 83-88 18346839-2 2008 R-(-)-gossypol (AT-101) is a small molecule that mimics the BH3 domain of cellular Bcl-2 inhibitors and interferes with the function of prosurvival Bcl-2 proteins. gossypol acetic acid 16-22 BCL2 apoptosis regulator Homo sapiens 148-153 18346839-8 2008 Apoptosis was activated via the mitochondrial pathway in multiple myeloma cell lines treated with AT-101 as demonstrated by an increased Bax to Bcl-2 ratio, mitochondrial membrane depolarization, and caspase activation. gossypol acetic acid 98-104 BCL2 associated X, apoptosis regulator Homo sapiens 137-140 18346839-8 2008 Apoptosis was activated via the mitochondrial pathway in multiple myeloma cell lines treated with AT-101 as demonstrated by an increased Bax to Bcl-2 ratio, mitochondrial membrane depolarization, and caspase activation. gossypol acetic acid 98-104 BCL2 apoptosis regulator Homo sapiens 144-149 18292288-3 2008 AT-101 is a BH3 mimetic known to be a potent inhibitor of antiapoptotic Bcl-2 family members including Bcl-2, Bcl-X(L), and Mcl-1. gossypol acetic acid 0-6 B cell leukemia/lymphoma 2 Mus musculus 72-77 18292288-3 2008 AT-101 is a BH3 mimetic known to be a potent inhibitor of antiapoptotic Bcl-2 family members including Bcl-2, Bcl-X(L), and Mcl-1. gossypol acetic acid 0-6 B cell leukemia/lymphoma 2 Mus musculus 103-108 18292288-3 2008 AT-101 is a BH3 mimetic known to be a potent inhibitor of antiapoptotic Bcl-2 family members including Bcl-2, Bcl-X(L), and Mcl-1. gossypol acetic acid 0-6 BCL2-like 1 Mus musculus 110-118 18292288-3 2008 AT-101 is a BH3 mimetic known to be a potent inhibitor of antiapoptotic Bcl-2 family members including Bcl-2, Bcl-X(L), and Mcl-1. gossypol acetic acid 0-6 myeloid cell leukemia sequence 1 Mus musculus 124-129 18084610-4 2007 Here, we investigated the efficacy of AT-101 (R-(-)-gossypol acetic acid; a pan small molecule inhibitor of Bcl-2, Bcl-x(L), and Mcl-1) in combination with surgical castration to delay the onset of androgen-independent growth in vivo. gossypol acetic acid 46-72 BCL2 apoptosis regulator Homo sapiens 108-113 18084610-4 2007 Here, we investigated the efficacy of AT-101 (R-(-)-gossypol acetic acid; a pan small molecule inhibitor of Bcl-2, Bcl-x(L), and Mcl-1) in combination with surgical castration to delay the onset of androgen-independent growth in vivo. gossypol acetic acid 46-72 BCL2 like 1 Homo sapiens 115-120 18084610-4 2007 Here, we investigated the efficacy of AT-101 (R-(-)-gossypol acetic acid; a pan small molecule inhibitor of Bcl-2, Bcl-x(L), and Mcl-1) in combination with surgical castration to delay the onset of androgen-independent growth in vivo. gossypol acetic acid 46-72 MCL1 apoptosis regulator, BCL2 family member Homo sapiens 129-134 18084610-8 2007 CONCLUSIONS: We conclude that AT-101 in combination with surgical castration delays the onset of androgen-independent prostate cancer in vivo by disrupting the antiapoptotic activity of Bcl-2 upregulation during the transition to androgen independence. gossypol acetic acid 30-36 BCL2 apoptosis regulator Homo sapiens 186-191 10231019-1 1999 Gossypol acetic acid (GAA) has been shown to have male antifertility effects, but there are pronounced differences among animal species. gossypol acetic acid 0-20 alpha glucosidase Homo sapiens 22-25 9879931-0 1998 Induction of c-fos, and cytochrome c oxidase subunits I and II by gossypol acetic acid in rat liver cells. gossypol acetic acid 66-86 Fos proto-oncogene, AP-1 transcription factor subunit Rattus norvegicus 13-18 9879931-0 1998 Induction of c-fos, and cytochrome c oxidase subunits I and II by gossypol acetic acid in rat liver cells. gossypol acetic acid 66-86 cytochrome c oxidase I, mitochondrial Rattus norvegicus 24-62 9408707-1 1997 In our earlier study, we have observed that hypokalemia in langur monkeys, following gossypol acetic acid (GAA) treatment (5 mg dose level) when used as an antispermatogenic agent, and potassium salt supplementation partially maintained body potassium level of the animals. gossypol acetic acid 85-105 alpha glucosidase Homo sapiens 107-110 8000225-2 1994 The binding capacity of cytosolic estradiol receptor (E2R) and progesterone receptor (PR) in groups treated with gossypol acetate or progesterone decreased. gossypol acetic acid 113-129 progesterone receptor Homo sapiens 63-84 8835944-2 1996 Platinum compounds inhibited the enzyme in the forward reaction (pyruvate-->lactate) only, n-hexanediol and colchicine showed no inhibition and gossypol acetic acid (GAA) strongly inhibited both the forward and reverse reactions and the reactions were time-dependent. gossypol acetic acid 147-167 alpha glucosidase Homo sapiens 169-172 8000225-2 1994 The binding capacity of cytosolic estradiol receptor (E2R) and progesterone receptor (PR) in groups treated with gossypol acetate or progesterone decreased. gossypol acetic acid 113-129 progesterone receptor Homo sapiens 86-88 3340619-1 1988 Carbon disulfide (CS2), tetraethyl lead (TEL), tetraethyl tin (TeET), dithiothreitol (DTT), and gossypol acetic acid (GAA) significantly decreased brain norepinephrine (NE) in rats. gossypol acetic acid 96-116 alpha glucosidase Rattus norvegicus 118-121 2063399-2 1991 The control group (n = 5) were injected with vehicle intramuscularly on the 17th, 18th and 19th day of pregnancy, and the gossypol treated group (n = 4) were injected with gossypol acetic acid (GAA) (25 mg/kg of body weight) intramuscularly on the 17th, 18th and 19th day and were decapitated on the 20th day of pregnancy. gossypol acetic acid 172-192 alpha glucosidase Rattus norvegicus 194-197 3402348-1 1988 Gossypol-acetic acid (GAA) has been shown to be a powerful chelator of iron. gossypol acetic acid 0-20 alpha glucosidase Rattus norvegicus 22-25 2975138-0 1988 [Effects of gossypol acetic acid on heart mitochondrial membranes ATPase]. gossypol acetic acid 12-32 dynein axonemal heavy chain 8 Homo sapiens 66-72 1668561-0 1991 [Effect of gossypol acetic acid on hCG-stimulated progesterone production of dissociated rat luteal cells]. gossypol acetic acid 11-31 hypertrichosis 2 (generalised, congenital) Homo sapiens 35-38 1668561-1 1991 The effect of gossypol acetic acid on hCG-stimulated progesterone synthesis and secretion in isolated rat luteal cells and its possible mechanism were investigated. gossypol acetic acid 14-34 hypertrichosis 2 (generalised, congenital) Homo sapiens 38-41 1668561-6 1991 The present experiment indicates that gossypol acetic acid can inhibit the progesterone production stimulated by hCG in isolated rat luteal cells through direct cellular mechanism. gossypol acetic acid 38-58 hypertrichosis 2 (generalised, congenital) Homo sapiens 113-116 2083490-4 1990 Subcutaneous administration in both low (15 mg/kg) and high (30 mg/kg) doses of gossypol acetic acid for five consecutive days significantly (P less than 0.00001) reduced hepatic aniline hydroxylase activity, as well as cytochrome P-450 and b5 levels. gossypol acetic acid 80-100 cytochrome P450, family 2, subfamily g, polypeptide 1 Rattus norvegicus 220-243 34827665-2 2021 Gossypol acetic acid (GAA), a natural product taken from the seeds of cotton plants, prevents oxidative stress. gossypol acetic acid 0-20 alpha glucosidase Rattus norvegicus 22-25 35484333-8 2022 Most importantly, gossypol-acetic acid (GAA) was recently reported by our team as the first specific inhibitor of LRPPRC. gossypol acetic acid 18-38 alpha glucosidase Homo sapiens 40-43 35484333-8 2022 Most importantly, gossypol-acetic acid (GAA) was recently reported by our team as the first specific inhibitor of LRPPRC. gossypol acetic acid 18-38 leucine rich pentatricopeptide repeat containing Homo sapiens 114-120 3190716-0 1988 Inhibition kinetics of lactate dehydrogenase isoenzymes by gossypol acetic acid. gossypol acetic acid 59-79 lactate dehydrogenase Capra hircus 23-44 3447817-1 1987 The studies in this report evaluate the inhibitory effects of long-term gossypol acetic acid (gossypol) administration on spermatozoal lactate dehydrogenase (LDH-X) activity, fertility and reversibility. gossypol acetic acid 72-92 lactate dehydrogenase C Rattus norvegicus 158-163 3626595-1 1987 Gossypol acetic acid (GAA) at the dosage of 30 mg/kg daily for 2 weeks could prolong the sleeping time of pentobarbital, increase the SGPT level, decrease the liver concentration of cytochrome P-450 and GSH content, inhibit the activity of cytochrome C reductase and aminopyrine-N-demethylase, but was without effect on cytochrome b5 and aniline hydroxylase. gossypol acetic acid 0-20 alpha glucosidase Rattus norvegicus 22-25 3625427-2 1987 Gossypol acetic acid (GAA), fed to juvenile chickens from 1 to 35 days, caused a decreased weight gain when compared to controls on untreated feed. gossypol acetic acid 0-20 alpha glucosidase 2 Gallus gallus 22-25 3626595-1 1987 Gossypol acetic acid (GAA) at the dosage of 30 mg/kg daily for 2 weeks could prolong the sleeping time of pentobarbital, increase the SGPT level, decrease the liver concentration of cytochrome P-450 and GSH content, inhibit the activity of cytochrome C reductase and aminopyrine-N-demethylase, but was without effect on cytochrome b5 and aniline hydroxylase. gossypol acetic acid 0-20 cytochrome P450, family 2, subfamily g, polypeptide 1 Rattus norvegicus 182-206 3626595-1 1987 Gossypol acetic acid (GAA) at the dosage of 30 mg/kg daily for 2 weeks could prolong the sleeping time of pentobarbital, increase the SGPT level, decrease the liver concentration of cytochrome P-450 and GSH content, inhibit the activity of cytochrome C reductase and aminopyrine-N-demethylase, but was without effect on cytochrome b5 and aniline hydroxylase. gossypol acetic acid 0-20 cytochrome b5 type A Rattus norvegicus 320-333 6454365-2 1981 Effect of gossypol acetic acid on the motility and ATPase activity of human spermatozoa. gossypol acetic acid 10-30 dynein axonemal heavy chain 8 Homo sapiens 51-57 2939980-0 1985 [Synergic effects of gossypol acetate and sulphadiazine on the LDH-x activity and viability of human sperm]. gossypol acetic acid 21-37 lactate dehydrogenase C Homo sapiens 63-68 6421193-1 1983 Male adult Wistar rats were exposed daily or every other day to oral gossypol acetic acid (GAA) concentrations of 2.5-30 mg/kg for 10-20 weeks. gossypol acetic acid 69-89 alpha glucosidase Rattus norvegicus 91-94 7114507-1 1982 Fertility response and sperm motility of male Wistar rats exposed to various concentrations (2.5 - 30 mg / kg / day) of gossypol acetic acid (GAA) was studied. gossypol acetic acid 120-140 alpha glucosidase Rattus norvegicus 142-145 3568662-1 1987 Gossypol acetic acid could induce total infertility in male Wistar/NIN strain rats at a dose of 30 mg per kg body weight per day, for 52 days. gossypol acetic acid 0-20 ninein Rattus norvegicus 67-70 3735252-1 1986 The inhibitory effect of (+)-, (-)-, (+/-)-gossypol and (+/-)-gossypol acetic acid upon testicular cytosolic LDH-X was measured in vitro. gossypol acetic acid 56-82 lactate dehydrogenase C Homo sapiens 109-114 3735252-2 1986 Gossypol acetic acid (0-100 mumol/l) inhibited LDH-X prepared from the testes of the mouse greater than rabbit greater than human greater than rat greater than hamster. gossypol acetic acid 0-20 lactate dehydrogenase C Mus musculus 47-52 6868221-0 1983 Ultrastructural analysis of rat testes after gossypol acetic acid (GAA) treatment. gossypol acetic acid 45-65 alpha glucosidase Rattus norvegicus 67-70 7160182-3 1982 Varying concentrations of gossypol acetic acid were incubated with 3H-methyl-S-adenosyl-methionine, COMT, a different concentrations of norepinephrine. gossypol acetic acid 26-46 catechol-O-methyltransferase Rattus norvegicus 100-104 31264066-0 2020 In vivo and in vitro inhibition of osteosarcoma growth by the pan Bcl-2 inhibitor AT-101. gossypol acetic acid 82-88 BCL2 apoptosis regulator Homo sapiens 66-71 32982170-3 2020 Gossypol-acetic acid (GAA) is a male contraceptive agent that shows anti-tumor effects on multiple types of cancers. gossypol acetic acid 0-20 alpha glucosidase Homo sapiens 22-25 33495516-6 2021 Gossypol acetate dose-dependently inhibited the enzymatic activity of VCP in vitro with IC50 of 6.53+-0.6 muM. gossypol acetic acid 0-16 valosin containing protein Homo sapiens 70-73 33495516-9 2021 Taken together, gossypol acetate acted through a gain-of-function way to induce the formation of VCP-LC3-mHTT ternary complex, triggering autophagic degradation of mHTT. gossypol acetic acid 16-32 valosin containing protein Mus musculus 97-100 33495516-9 2021 Taken together, gossypol acetate acted through a gain-of-function way to induce the formation of VCP-LC3-mHTT ternary complex, triggering autophagic degradation of mHTT. gossypol acetic acid 16-32 microtubule associated protein 1 light chain 3 alpha Homo sapiens 101-104 33487592-3 2021 We sought to elucidate the antitumour action of a BCL-2 inhibitor, AT101 in GEC in vitro, in vivo and in a clinical trial. gossypol acetic acid 67-72 BCL2 apoptosis regulator Homo sapiens 50-55 33487592-7 2021 AT-101 induced apoptosis, reduced proliferation and tumour sphere formation in MCL-1/BCL-2 high GC cells. gossypol acetic acid 0-6 BCL2 apoptosis regulator Homo sapiens 85-90 33487592-10 2021 In vivo studies confirmed the combination of AT101 and docetaxel demonstrated stronger antitumour activity accompanied with significant decrease of CSCs biomarkers (YAP1/SOX9). gossypol acetic acid 45-50 Yes1 associated transcriptional regulator Homo sapiens 165-169 33487592-10 2021 In vivo studies confirmed the combination of AT101 and docetaxel demonstrated stronger antitumour activity accompanied with significant decrease of CSCs biomarkers (YAP1/SOX9). gossypol acetic acid 45-50 SRY-box transcription factor 9 Homo sapiens 170-174 31264066-10 2020 Our results demonstrated that AT-101 inhibits prosurvival signaling pathways depending on Akt, p38 MAPK and JNK. gossypol acetic acid 30-36 AKT serine/threonine kinase 1 Homo sapiens 90-93 31264066-10 2020 Our results demonstrated that AT-101 inhibits prosurvival signaling pathways depending on Akt, p38 MAPK and JNK. gossypol acetic acid 30-36 mitogen-activated protein kinase 14 Homo sapiens 95-98 31264066-10 2020 Our results demonstrated that AT-101 inhibits prosurvival signaling pathways depending on Akt, p38 MAPK and JNK. gossypol acetic acid 30-36 mitogen-activated protein kinase 8 Homo sapiens 108-111 31388792-2 2020 This phase I trial investigated the MTD of AT-101 in combination with paclitaxel and carboplatin in patients with advanced solid tumors. gossypol acetic acid 43-49 metallothionein 1E Homo sapiens 36-39 31657561-7 2019 The screened compound, gossypol-acetic acid (GAA), is an old medicine which can accomplish the new function for targeted LRPPRC knockdown. gossypol acetic acid 23-43 leucine rich pentatricopeptide repeat containing Homo sapiens 121-127 31657561-7 2019 The screened compound, gossypol-acetic acid (GAA), is an old medicine which can accomplish the new function for targeted LRPPRC knockdown. gossypol acetic acid 45-48 leucine rich pentatricopeptide repeat containing Homo sapiens 121-127 30605780-4 2019 The present study investigated the inhibitory effects of gossypol acetate on rat 5alpha-reductase 1, 3alpha-hydroxysteroid dehydrogenase, and retinol dehydrogenase 2 for androgen metabolism. gossypol acetic acid 57-73 aldo-keto reductase family 1, member C14 Rattus norvegicus 101-136 30605780-9 2019 Gossypol acetate inhibited 5alpha-reductase 1 and 3alpha-hydroxysteroid dehydrogenase with IC50 values of 3.33 +- 0.07 and 0.52 +- 0.06 x 10-6 M in the expressed enzymes as well as 8.512 +- 0.079 and 1.032 +- 0.068 x 10-6 M in intact rat immature Leydig cells, respectively. gossypol acetic acid 0-16 aldo-keto reductase family 1, member C14 Rattus norvegicus 50-85 30605780-11 2019 Gossypol acetate weakly inhibited retinol dehydrogenase 2 with IC50 value over 1 x 10-4 M. Molecular docking analysis showed that gossypol partially bound to the steroid-binding site of the crystal structure of rat 3alpha-hydroxysteroid dehydrogenase. gossypol acetic acid 0-16 retinol dehydrogenase 16 Rattus norvegicus 34-57 30605780-11 2019 Gossypol acetate weakly inhibited retinol dehydrogenase 2 with IC50 value over 1 x 10-4 M. Molecular docking analysis showed that gossypol partially bound to the steroid-binding site of the crystal structure of rat 3alpha-hydroxysteroid dehydrogenase. gossypol acetic acid 0-16 aldo-keto reductase family 1, member C14 Rattus norvegicus 215-250 30605780-12 2019 Gossypol acetate is a potent inhibitor of rat 5alpha-reductase 1 and 3alpha-hydroxysteroid dehydrogenase, possibly inhibiting the formation of androgen in the prostate cancer cells. gossypol acetic acid 0-16 aldo-keto reductase family 1, member C14 Rattus norvegicus 69-104 27431492-4 2016 In this study, enhanced antitumor effect of AT-101, a-pan-Bcl-2 inhibitor, on gefitinib was explored in NSCLC with T790M mutation. gossypol acetic acid 44-50 BCL2 apoptosis regulator Homo sapiens 58-63 30483745-0 2019 AT-101 induces G1/G0 phase arrest via the beta-catenin/cyclin D1 signaling pathway in human esophageal cancer cells. gossypol acetic acid 0-6 catenin beta 1 Homo sapiens 42-54 30483745-0 2019 AT-101 induces G1/G0 phase arrest via the beta-catenin/cyclin D1 signaling pathway in human esophageal cancer cells. gossypol acetic acid 0-6 cyclin D1 Homo sapiens 55-64 30483745-1 2019 AT-101, an orally available and well-tolerated natural pan-Bcl-2 family protein inhibitor, has been reported to be effective against a variety of cancers. gossypol acetic acid 0-6 BCL2 apoptosis regulator Homo sapiens 59-64 28710745-0 2017 The pan-Bcl2 Inhibitor AT101 Activates the Intrinsic Apoptotic Pathway and Causes DNA Damage in Acute Myeloid Leukemia Stem-Like Cells. gossypol acetic acid 23-28 BCL2 apoptosis regulator Homo sapiens 8-12 28575052-8 2017 Treatment of hiPSC precursors with autophagy stimulators Rapamycin, Perifosine, or AT101 showed reduction in VCP pathology markers TDP-43, LC3-I/II and p62/SQSTM1. gossypol acetic acid 83-88 valosin containing protein Homo sapiens 109-112 28575052-8 2017 Treatment of hiPSC precursors with autophagy stimulators Rapamycin, Perifosine, or AT101 showed reduction in VCP pathology markers TDP-43, LC3-I/II and p62/SQSTM1. gossypol acetic acid 83-88 TAR DNA binding protein Homo sapiens 131-137 28575052-8 2017 Treatment of hiPSC precursors with autophagy stimulators Rapamycin, Perifosine, or AT101 showed reduction in VCP pathology markers TDP-43, LC3-I/II and p62/SQSTM1. gossypol acetic acid 83-88 sequestosome 1 Homo sapiens 152-155 28575052-8 2017 Treatment of hiPSC precursors with autophagy stimulators Rapamycin, Perifosine, or AT101 showed reduction in VCP pathology markers TDP-43, LC3-I/II and p62/SQSTM1. gossypol acetic acid 83-88 sequestosome 1 Homo sapiens 156-162 30459622-12 2018 In addition, the treatment with AT-101 was able to: (a) decrease the ErbB2 protein expression; (b) increase the EGFR protein expression; (c) affect the phosphorylation of ERK1/2, p38 and AKT; (d) stimulate JNK1/2 and c-jun phosphorylation. gossypol acetic acid 32-38 erb-b2 receptor tyrosine kinase 2 Homo sapiens 69-74 30459622-12 2018 In addition, the treatment with AT-101 was able to: (a) decrease the ErbB2 protein expression; (b) increase the EGFR protein expression; (c) affect the phosphorylation of ERK1/2, p38 and AKT; (d) stimulate JNK1/2 and c-jun phosphorylation. gossypol acetic acid 32-38 epidermal growth factor receptor Homo sapiens 112-116 30459622-12 2018 In addition, the treatment with AT-101 was able to: (a) decrease the ErbB2 protein expression; (b) increase the EGFR protein expression; (c) affect the phosphorylation of ERK1/2, p38 and AKT; (d) stimulate JNK1/2 and c-jun phosphorylation. gossypol acetic acid 32-38 mitogen-activated protein kinase 3 Homo sapiens 171-177 30459622-12 2018 In addition, the treatment with AT-101 was able to: (a) decrease the ErbB2 protein expression; (b) increase the EGFR protein expression; (c) affect the phosphorylation of ERK1/2, p38 and AKT; (d) stimulate JNK1/2 and c-jun phosphorylation. gossypol acetic acid 32-38 mitogen-activated protein kinase 1 Homo sapiens 179-182 30459622-12 2018 In addition, the treatment with AT-101 was able to: (a) decrease the ErbB2 protein expression; (b) increase the EGFR protein expression; (c) affect the phosphorylation of ERK1/2, p38 and AKT; (d) stimulate JNK1/2 and c-jun phosphorylation. gossypol acetic acid 32-38 AKT serine/threonine kinase 1 Homo sapiens 187-190 30459622-12 2018 In addition, the treatment with AT-101 was able to: (a) decrease the ErbB2 protein expression; (b) increase the EGFR protein expression; (c) affect the phosphorylation of ERK1/2, p38 and AKT; (d) stimulate JNK1/2 and c-jun phosphorylation. gossypol acetic acid 32-38 mitogen-activated protein kinase 8 Homo sapiens 206-212 30459622-12 2018 In addition, the treatment with AT-101 was able to: (a) decrease the ErbB2 protein expression; (b) increase the EGFR protein expression; (c) affect the phosphorylation of ERK1/2, p38 and AKT; (d) stimulate JNK1/2 and c-jun phosphorylation. gossypol acetic acid 32-38 Jun proto-oncogene, AP-1 transcription factor subunit Homo sapiens 217-222 27431492-9 2016 RESULTS: In this study, we found that treatment with AT-101 in combination with gefitinib significantly inhibited cell proliferation, as well as promoted apoptosis of EGFR TKIs resistant lung cancer cells. gossypol acetic acid 53-59 epidermal growth factor receptor Homo sapiens 167-171 27431492-10 2016 The apoptotic effects of the use of AT-101 was related to the blocking of antiapoptotic protein: Bcl-2, Bcl-xl, and Mcl-1 and downregrulation of the molecules in EGFR pathway. gossypol acetic acid 36-42 BCL2 apoptosis regulator Homo sapiens 97-102 27431492-10 2016 The apoptotic effects of the use of AT-101 was related to the blocking of antiapoptotic protein: Bcl-2, Bcl-xl, and Mcl-1 and downregrulation of the molecules in EGFR pathway. gossypol acetic acid 36-42 BCL2 like 1 Homo sapiens 104-110 27431492-10 2016 The apoptotic effects of the use of AT-101 was related to the blocking of antiapoptotic protein: Bcl-2, Bcl-xl, and Mcl-1 and downregrulation of the molecules in EGFR pathway. gossypol acetic acid 36-42 MCL1 apoptosis regulator, BCL2 family member Homo sapiens 116-121 27431492-10 2016 The apoptotic effects of the use of AT-101 was related to the blocking of antiapoptotic protein: Bcl-2, Bcl-xl, and Mcl-1 and downregrulation of the molecules in EGFR pathway. gossypol acetic acid 36-42 epidermal growth factor receptor Homo sapiens 162-166 27431492-13 2016 The addition of AT-101 to gefitinib is a promising strategy to overcome EGFR TKIs resistance in NSCLC with EGFR T790M mutations. gossypol acetic acid 16-22 epidermal growth factor receptor Homo sapiens 72-76 27431492-13 2016 The addition of AT-101 to gefitinib is a promising strategy to overcome EGFR TKIs resistance in NSCLC with EGFR T790M mutations. gossypol acetic acid 16-22 epidermal growth factor receptor Homo sapiens 107-111 26721623-5 2016 AT-101 treatment induced a prominent conversion of LC3-I to LC3-II and apoptotic cell death characterized by the appearance of Annexin-positive/PI-negative early apoptotic cells and PARP cleavage. gossypol acetic acid 0-6 collagen type XI alpha 2 chain Homo sapiens 182-186 26531719-0 2016 Octreotide in combination with AT-101 induces cytotoxicity and apoptosis through up-regulation of somatostatin receptors 2 and 5 in DU-145 prostate cancer cells. gossypol acetic acid 31-37 somatostatin receptor 2 Homo sapiens 98-128 26476589-0 2016 A Phase II Study of AT-101 to Overcome Bcl-2--Mediated Resistance to Androgen Deprivation Therapy in Patients With Newly Diagnosed Castration-Sensitive Metastatic Prostate Cancer. gossypol acetic acid 20-26 BCL2 apoptosis regulator Homo sapiens 39-44 26476589-1 2016 UNLABELLED: In a phase II multicenter study, men with castration sensitive metastatic prostate cancer were treated with AT-101, a small molecule Bcl-2 inhibitor, and androgen deprivation therapy. gossypol acetic acid 120-126 BCL2 apoptosis regulator Homo sapiens 145-150 26309203-0 2015 Gossypol acetate induced apoptosis of pituitary tumor cells by targeting the BCL-2 via the upregulated microRNA miR-15a. gossypol acetic acid 0-16 BCL2, apoptosis regulator Rattus norvegicus 77-82 26535659-1 2015 We investigated the effects of gossypol acetic acid (GAA) on the proliferation, apoptosis, and expression of DNA methyltransferase 1 (DNMT1) mRNA in human adenoid cystic carcinoma (ACC-M) cells in vitro. gossypol acetic acid 31-51 DNA methyltransferase 1 Homo sapiens 109-132 26223311-0 2015 Targeting anti-apoptotic Bcl-2 by AT-101 to increase radiation efficacy: data from in vitro and clinical pharmacokinetic studies in head and neck cancer. gossypol acetic acid 34-40 BCL2 apoptosis regulator Homo sapiens 25-30 26223311-5 2015 The aim of this study was to evaluate combined effects of radiation and the pan-Bcl-2 inhibitor AT-101 in HNSCC in vitro. gossypol acetic acid 96-102 BCL2 apoptosis regulator Homo sapiens 80-85 26309203-0 2015 Gossypol acetate induced apoptosis of pituitary tumor cells by targeting the BCL-2 via the upregulated microRNA miR-15a. gossypol acetic acid 0-16 microRNA mir-15a Rattus norvegicus 112-119 26089640-6 2015 AT-101 also enhanced the inhibitory effect of CDDP on DNA repair and redox activities of apurinic/apyrimidinic endonuclease 1 (APE1) in A549 cells. gossypol acetic acid 0-6 apurinic/apyrimidinic endodeoxyribonuclease 1 Homo sapiens 127-131 26089640-8 2015 These results suggest that AT-101 can enhance the antitumor activity of CDDP in NSCLC via inhibition of APE1 DNA repair and redox activities and by angiogenesis and induction of apoptosis, but other mechanisms cannot be excluded. gossypol acetic acid 27-33 apurinic/apyrimidinic endodeoxyribonuclease 1 Homo sapiens 104-108 26089640-0 2015 Small-molecule BH3 mimetic and pan-Bcl-2 inhibitor AT-101 enhances the antitumor efficacy of cisplatin through inhibition of APE1 repair and redox activity in non-small-cell lung cancer. gossypol acetic acid 51-57 BCL2 apoptosis regulator Homo sapiens 35-40 25548514-0 2014 Sequential treatment with AT-101 enhances cisplatin chemosensitivity in human non-small cell lung cancer cells through inhibition of apurinic/apyrimidinic endonuclease 1-activated IL-6/STAT3 signaling pathway. gossypol acetic acid 26-32 apurinic/apyrimidinic endodeoxyribonuclease 1 Homo sapiens 133-169 26089640-0 2015 Small-molecule BH3 mimetic and pan-Bcl-2 inhibitor AT-101 enhances the antitumor efficacy of cisplatin through inhibition of APE1 repair and redox activity in non-small-cell lung cancer. gossypol acetic acid 51-57 apurinic/apyrimidinic endodeoxyribonuclease 1 Homo sapiens 125-129 26089640-1 2015 AT-101 is a BH3 mimetic and pan-Bcl-2 inhibitor that has shown potent anticancer activity in non-small-cell lung cancer (NSCLC) in murine models, but failed to show clinical efficacy when used in combination with docetaxel in NSCLC patients. gossypol acetic acid 0-6 B cell leukemia/lymphoma 2 Mus musculus 32-37 26089640-2 2015 Our recent study has demonstrated that AT-101 enhanced the antitumor effect of cisplatin (CDDP) in a murine model of NSCLC via inhibition of the interleukin-6/signal transducer and activator of transcription 3 (STAT3) pathway. gossypol acetic acid 39-45 signal transducer and activator of transcription 3 Mus musculus 145-209 26089640-2 2015 Our recent study has demonstrated that AT-101 enhanced the antitumor effect of cisplatin (CDDP) in a murine model of NSCLC via inhibition of the interleukin-6/signal transducer and activator of transcription 3 (STAT3) pathway. gossypol acetic acid 39-45 signal transducer and activator of transcription 3 Mus musculus 211-216 26089640-6 2015 AT-101 also enhanced the inhibitory effect of CDDP on DNA repair and redox activities of apurinic/apyrimidinic endonuclease 1 (APE1) in A549 cells. gossypol acetic acid 0-6 apurinic/apyrimidinic endodeoxyribonuclease 1 Homo sapiens 89-125 25802279-0 2015 Gossypol Acetic Acid Prevents Oxidative Stress-Induced Retinal Pigment Epithelial Necrosis by Regulating the FoxO3/Sestrin2 Pathway. gossypol acetic acid 0-20 forkhead box O3 Homo sapiens 109-114 25802279-0 2015 Gossypol Acetic Acid Prevents Oxidative Stress-Induced Retinal Pigment Epithelial Necrosis by Regulating the FoxO3/Sestrin2 Pathway. gossypol acetic acid 0-20 sestrin 2 Homo sapiens 115-123 25802279-3 2015 In this study, we screened U.S. Food and Drug Administration-approved natural compounds and identified gossypol acetic acid (GAA) as a potent inhibitor of oxidative stress-induced RPE cell death. gossypol acetic acid 103-123 alpha glucosidase Homo sapiens 125-128 25885284-3 2015 The small-molecule pan-Bcl-2 inhibitor (-)-gossypol (AT-101) is known to induce apoptotic cell death, but can also induce autophagy through release of the pro-autophagic BH3 only protein Beclin-1 from Bcl-2. gossypol acetic acid 53-59 BCL2 apoptosis regulator Homo sapiens 23-28 25885284-3 2015 The small-molecule pan-Bcl-2 inhibitor (-)-gossypol (AT-101) is known to induce apoptotic cell death, but can also induce autophagy through release of the pro-autophagic BH3 only protein Beclin-1 from Bcl-2. gossypol acetic acid 53-59 beclin 1 Homo sapiens 187-195 25885284-3 2015 The small-molecule pan-Bcl-2 inhibitor (-)-gossypol (AT-101) is known to induce apoptotic cell death, but can also induce autophagy through release of the pro-autophagic BH3 only protein Beclin-1 from Bcl-2. gossypol acetic acid 53-59 BCL2 apoptosis regulator Homo sapiens 201-206 25530717-0 2014 Induction of H2AX phosphorylation in tumor cells by gossypol acetic acid is mediated by phosphatidylinositol 3-kinase (PI3K) family. gossypol acetic acid 52-72 H2A.X variant histone Mus musculus 13-17 25530717-2 2014 Our study shows that gossypol acetic acid (GAA) alone can induce gammaH2AX in Human mucoepidermoid carcinoma cell line (MEC-1) in vitro. gossypol acetic acid 21-41 alpha glucosidase Homo sapiens 43-46 25530717-2 2014 Our study shows that gossypol acetic acid (GAA) alone can induce gammaH2AX in Human mucoepidermoid carcinoma cell line (MEC-1) in vitro. gossypol acetic acid 21-41 H2A.X variant histone Mus musculus 65-74 25530717-2 2014 Our study shows that gossypol acetic acid (GAA) alone can induce gammaH2AX in Human mucoepidermoid carcinoma cell line (MEC-1) in vitro. gossypol acetic acid 21-41 ATR serine/threonine kinase Homo sapiens 120-125 26113054-1 2015 PURPOSE: AT-101 is considered as a putative pan-inhibitor of anti-apoptotic Bcl-2 family protein members acting as a BH3 mimetic. gossypol acetic acid 9-15 B cell leukemia/lymphoma 2 Mus musculus 76-81 26113054-6 2015 Furthermore, we identified that AT-101 potentially acted on smoothened (Smo) by sharing the same binding site with cyclopamine, a classical Hh signaling pathway inhibitor. gossypol acetic acid 32-38 smoothened, frizzled class receptor Mus musculus 60-70 26113054-6 2015 Furthermore, we identified that AT-101 potentially acted on smoothened (Smo) by sharing the same binding site with cyclopamine, a classical Hh signaling pathway inhibitor. gossypol acetic acid 32-38 smoothened, frizzled class receptor Mus musculus 72-75 26113054-7 2015 Taking advantage of the patch+/-; p53-/- mouse medulloblastoma model, we observed that AT-101 significantly suppressed the Hh-driven medulloblastoma growth in vitro and in vivo. gossypol acetic acid 87-93 transformation related protein 53, pseudogene Mus musculus 34-37 26113054-8 2015 CONCLUSIONS: This study demonstrates that AT-101 significantly and selectively inhibits Hh pathway activity by potentially targeting Smo and consequently suppresses the growth of Hh-driven cancer. gossypol acetic acid 42-48 smoothened, frizzled class receptor Mus musculus 133-136 25548514-0 2014 Sequential treatment with AT-101 enhances cisplatin chemosensitivity in human non-small cell lung cancer cells through inhibition of apurinic/apyrimidinic endonuclease 1-activated IL-6/STAT3 signaling pathway. gossypol acetic acid 26-32 interleukin 6 Homo sapiens 180-184 25548514-0 2014 Sequential treatment with AT-101 enhances cisplatin chemosensitivity in human non-small cell lung cancer cells through inhibition of apurinic/apyrimidinic endonuclease 1-activated IL-6/STAT3 signaling pathway. gossypol acetic acid 26-32 signal transducer and activator of transcription 3 Homo sapiens 185-190 24434521-0 2014 RhoA/ROCK/PTEN signaling is involved in AT-101-mediated apoptosis in human leukemia cells in vitro and in vivo. gossypol acetic acid 40-46 ras homolog family member A Homo sapiens 0-4 24703900-0 2014 Glucocorticoid sensitisation in Mixed Lineage Leukaemia-rearranged acute lymphoblastic leukaemia by the pan-BCL-2 family inhibitors gossypol and AT-101. gossypol acetic acid 145-151 BCL2 apoptosis regulator Homo sapiens 108-113 24703900-4 2014 METHODS: We exposed GC-resistant MLL-rearranged SEMK2 cells to potent MCL1-inhibiting agents, including gossypol, AT-101, rapamycin, SU9516 and obatoclax (GX15-070) and determined GC sensitisation using 3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide (MTT) assays. gossypol acetic acid 114-120 lysine methyltransferase 2A Homo sapiens 33-36 24703900-6 2014 RESULTS: Only gossypol and its synthetic analogue AT-101 induced GC sensitivity in MLL-rearranged ALL cells. gossypol acetic acid 50-56 lysine methyltransferase 2A Homo sapiens 83-86 24703900-8 2014 CONCLUDING REMARKS: In conclusion, gossypol and AT-101 induce GC sensitivity in MLL-rearranged ALL cells, most likely mediated by the activation of BID and BIM without the necessity to down-regulate anti-apoptotic BCL-2 family members like MCL1. gossypol acetic acid 48-54 lysine methyltransferase 2A Homo sapiens 80-83 24703900-8 2014 CONCLUDING REMARKS: In conclusion, gossypol and AT-101 induce GC sensitivity in MLL-rearranged ALL cells, most likely mediated by the activation of BID and BIM without the necessity to down-regulate anti-apoptotic BCL-2 family members like MCL1. gossypol acetic acid 48-54 BCL2 apoptosis regulator Homo sapiens 214-219 24703900-8 2014 CONCLUDING REMARKS: In conclusion, gossypol and AT-101 induce GC sensitivity in MLL-rearranged ALL cells, most likely mediated by the activation of BID and BIM without the necessity to down-regulate anti-apoptotic BCL-2 family members like MCL1. gossypol acetic acid 48-54 MCL1 apoptosis regulator, BCL2 family member Homo sapiens 240-244 24703900-9 2014 Hence, co-administration of either gossypol or AT-101 during GC treatment of GC-resistant MLL-rearranged ALL patients may overcome GC resistance and improve prognosis in this high-risk childhood leukaemia. gossypol acetic acid 47-53 lysine methyltransferase 2A Homo sapiens 90-93 24236538-4 2014 Thus, we investigated the anti-tumour effects of a pan-BCL2 inhibitor, AT-101, which has high binding specificity for BCL2 and MCL1 in preclinical models of plasma cell cancers (Multiple myeloma and Waldenstrom macroglobulinaemia). gossypol acetic acid 71-77 BCL2 apoptosis regulator Homo sapiens 55-59 24236538-4 2014 Thus, we investigated the anti-tumour effects of a pan-BCL2 inhibitor, AT-101, which has high binding specificity for BCL2 and MCL1 in preclinical models of plasma cell cancers (Multiple myeloma and Waldenstrom macroglobulinaemia). gossypol acetic acid 71-77 BCL2 apoptosis regulator Homo sapiens 118-122 24236538-4 2014 Thus, we investigated the anti-tumour effects of a pan-BCL2 inhibitor, AT-101, which has high binding specificity for BCL2 and MCL1 in preclinical models of plasma cell cancers (Multiple myeloma and Waldenstrom macroglobulinaemia). gossypol acetic acid 71-77 MCL1 apoptosis regulator, BCL2 family member Homo sapiens 127-131 24236538-7 2014 This cytotoxic effect and BCL2 downregulation were further potentiated when AT-101 was combined with lenalidomide/dexamethasone (LDA). gossypol acetic acid 76-82 BCL2 apoptosis regulator Homo sapiens 26-30 24665650-1 2014 OBJECTIVE: This paper aims to study the effects of gossypol acetic acid (GAA) on proliferation and methylation level of human MutL homologue 1 (hMLH1) gene in human tongue cancer cell line Tca8113. gossypol acetic acid 51-71 alpha glucosidase Homo sapiens 73-76 24665650-1 2014 OBJECTIVE: This paper aims to study the effects of gossypol acetic acid (GAA) on proliferation and methylation level of human MutL homologue 1 (hMLH1) gene in human tongue cancer cell line Tca8113. gossypol acetic acid 51-71 mutL homolog 1 Homo sapiens 144-149 24434521-0 2014 RhoA/ROCK/PTEN signaling is involved in AT-101-mediated apoptosis in human leukemia cells in vitro and in vivo. gossypol acetic acid 40-46 phosphatase and tensin homolog Homo sapiens 10-14 24434521-9 2014 Constitutively active Akt prevented the AT-101-induced Mcl-1 downregulation, Bad dephosphorylation, and apoptosis. gossypol acetic acid 40-46 AKT serine/threonine kinase 1 Homo sapiens 22-25 24434521-9 2014 Constitutively active Akt prevented the AT-101-induced Mcl-1 downregulation, Bad dephosphorylation, and apoptosis. gossypol acetic acid 40-46 MCL1 apoptosis regulator, BCL2 family member Homo sapiens 55-60 24434521-11 2014 In vivo, the tumor growth inhibition caused by AT-101 was also associated with RhoA/ROCK1/PTEN activation and Akt inactivation in a mouse leukemia xenograft model. gossypol acetic acid 47-53 ras homolog family member A Mus musculus 79-83 24434521-11 2014 In vivo, the tumor growth inhibition caused by AT-101 was also associated with RhoA/ROCK1/PTEN activation and Akt inactivation in a mouse leukemia xenograft model. gossypol acetic acid 47-53 Rho-associated coiled-coil containing protein kinase 1 Mus musculus 84-89 24434521-11 2014 In vivo, the tumor growth inhibition caused by AT-101 was also associated with RhoA/ROCK1/PTEN activation and Akt inactivation in a mouse leukemia xenograft model. gossypol acetic acid 47-53 phosphatase and tensin homolog Mus musculus 90-94 24434521-11 2014 In vivo, the tumor growth inhibition caused by AT-101 was also associated with RhoA/ROCK1/PTEN activation and Akt inactivation in a mouse leukemia xenograft model. gossypol acetic acid 47-53 thymoma viral proto-oncogene 1 Mus musculus 110-113 23708869-0 2013 Induction of apoptosis and antitumor effects of a small molecule inhibitor of Bcl-2 and Bcl-xl, gossypol acetate, in multiple myeloma in vitro and in vivo. gossypol acetic acid 96-112 BCL2 apoptosis regulator Homo sapiens 78-83 23685020-3 2014 PATIENTS AND METHODS: A retrospective analysis was conducted on 221 patients with mCRPC treated with docetaxel plus prednisone combined with AT-101 (bcl-2 antagonist) or placebo on a prospective randomized phase II trial. gossypol acetic acid 141-147 BCL2 apoptosis regulator Homo sapiens 149-154 24299314-0 2014 Autophagy inhibition enhances pan-Bcl-2 inhibitor AT-101-induced apoptosis in non-small cell lung cancer. gossypol acetic acid 50-56 BCL2 apoptosis regulator Homo sapiens 34-39 23708869-0 2013 Induction of apoptosis and antitumor effects of a small molecule inhibitor of Bcl-2 and Bcl-xl, gossypol acetate, in multiple myeloma in vitro and in vivo. gossypol acetic acid 96-112 BCL2 like 1 Homo sapiens 88-94 23410041-5 2013 The method was implemented with anticancer activity of Gossypol acetic acid against BCL2 target for colorectal cancer. gossypol acetic acid 55-75 BCL2 apoptosis regulator Homo sapiens 84-88 23410041-9 2013 The suggested compounds were further validated by docking study with Gossypol acetic acid and "Tetrahydroisoquinoline amide substituted phenyl pyrazole" cocrystallized with chimeric BCL2-XL (PDBID: 2W3L) protein. gossypol acetic acid 69-89 BCL2 apoptosis regulator Homo sapiens 182-186 23708869-7 2013 Bcl-2 and Bcl-xl expression was decreased by 86.5+-1.2% and 35.9+-3.6%, respectively, after treatment with gossypol acetate at 25 micromol/l for 24 h. Preliminary studies in vivo showed that a growth inhibition (T/C) of 30.9% (gossypol acetate 40 mg/kg) was obtained in Balb/C mice bearing Wus1 cells. gossypol acetic acid 107-123 BCL2 apoptosis regulator Homo sapiens 0-5 23708869-7 2013 Bcl-2 and Bcl-xl expression was decreased by 86.5+-1.2% and 35.9+-3.6%, respectively, after treatment with gossypol acetate at 25 micromol/l for 24 h. Preliminary studies in vivo showed that a growth inhibition (T/C) of 30.9% (gossypol acetate 40 mg/kg) was obtained in Balb/C mice bearing Wus1 cells. gossypol acetic acid 107-123 BCL2 like 1 Homo sapiens 10-16 23708869-7 2013 Bcl-2 and Bcl-xl expression was decreased by 86.5+-1.2% and 35.9+-3.6%, respectively, after treatment with gossypol acetate at 25 micromol/l for 24 h. Preliminary studies in vivo showed that a growth inhibition (T/C) of 30.9% (gossypol acetate 40 mg/kg) was obtained in Balb/C mice bearing Wus1 cells. gossypol acetic acid 227-243 BCL2 apoptosis regulator Homo sapiens 0-5 23708869-7 2013 Bcl-2 and Bcl-xl expression was decreased by 86.5+-1.2% and 35.9+-3.6%, respectively, after treatment with gossypol acetate at 25 micromol/l for 24 h. Preliminary studies in vivo showed that a growth inhibition (T/C) of 30.9% (gossypol acetate 40 mg/kg) was obtained in Balb/C mice bearing Wus1 cells. gossypol acetic acid 227-243 BCL2 like 1 Homo sapiens 10-16 23708869-9 2013 Our results demonstrated that the potent inhibitor of Bcl-2 and Bcl-xl gossypol acetate had significant antiproliferative and antiapoptotic effects on multiple myeloma cells in vitro and in vivo. gossypol acetic acid 71-87 BCL2 like 1 Homo sapiens 64-70 23708869-10 2013 Gossypol acetate may represent a promising new anticancer agent with a novel molecular mechanism and warrants further investigation as a single agent, or in combination with other chemotherapeutics, for human multiple myeloma with Bcl-2 overexpression. gossypol acetic acid 0-16 BCL2 apoptosis regulator Homo sapiens 231-236 23734725-2 2013 Small molecule inhibitors such as AT-101 (a BH3-mimetic drug) have been developed to inhibit the antiapoptotic activity of Bcl-2 proteins, which proved effective in restoring radio- and chemo-sensitivity in head and neck cancer cells. gossypol acetic acid 34-40 BCL2 apoptosis regulator Homo sapiens 123-128 23734725-3 2013 However, high doses of AT-101 are associated with gastrointestinal, hepatic, and fertility side effects, which prompted the search for other Bcl-2 inhibitors. gossypol acetic acid 23-29 BCL2 apoptosis regulator Homo sapiens 141-146 23734725-8 2013 Results also show that combining "smart" anti-Bcl-2 particles with the IC25 of AT-101 (inhibitory concentration responsible for killing 25% of the cells) synergistically inhibits cancer cell proliferation and increases cell apoptosis, which reduce the survival of UM-SCC-17B cancer cells compared to treatment with AT-101 alone. gossypol acetic acid 79-85 BCL2 apoptosis regulator Homo sapiens 46-51 23734725-8 2013 Results also show that combining "smart" anti-Bcl-2 particles with the IC25 of AT-101 (inhibitory concentration responsible for killing 25% of the cells) synergistically inhibits cancer cell proliferation and increases cell apoptosis, which reduce the survival of UM-SCC-17B cancer cells compared to treatment with AT-101 alone. gossypol acetic acid 315-321 BCL2 apoptosis regulator Homo sapiens 46-51 23269627-1 2013 We investigated the effects of AT-101/cisplatin combination treatment on the expression levels of apoptotic proteins and epigenetic events such as DNA methyltransferase (DNMT) and histone deacetylase (HDAC) enzyme activities in OVCAR-3 and MDAH-2774 ovarian cancer cells. gossypol acetic acid 31-37 DNA methyltransferase 1 Homo sapiens 147-168 23269627-1 2013 We investigated the effects of AT-101/cisplatin combination treatment on the expression levels of apoptotic proteins and epigenetic events such as DNA methyltransferase (DNMT) and histone deacetylase (HDAC) enzyme activities in OVCAR-3 and MDAH-2774 ovarian cancer cells. gossypol acetic acid 31-37 DNA methyltransferase 1 Homo sapiens 170-174 23820203-0 2013 Gossypol acetic acid induces apoptosis in RAW264.7 cells via a caspase-dependent mitochondrial signaling pathway. gossypol acetic acid 0-20 caspase 9 Mus musculus 63-70 23820203-4 2013 Finally, the GA-induced cell apoptosis was evaluated by flow cytometry in the present of caspase inhibitors Z-VAD-FMK and Ac-LEHD-FMK, respectively. gossypol acetic acid 13-15 caspase 9 Mus musculus 89-96 23820203-7 2013 Notably, GA-induced cell apoptosis was markedly inhibited by caspase inhibitors. gossypol acetic acid 9-11 caspase 9 Mus musculus 61-68 23820203-8 2013 These results suggest that GA-induced RAW264.7 cell apoptosis may be mediated via a caspase-dependent mitochondrial signaling pathway. gossypol acetic acid 27-29 caspase 9 Mus musculus 84-91