PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 15741653-0 2005 Hypolipidemic action of the SERM acolbifene is associated with decreased liver MTP and increased SR-BI and LDL receptors. ritetronium 33-43 microsomal triglyceride transfer protein Homo sapiens 79-82 16140902-10 2005 In livers of rats fed the reference diet, ACOL, but not pair feeding, increased protein abundance of the scavenger receptor, class B, type 1, and the LDL receptor, thought to be involved in ACOL-mediated cholesterol lowering. ritetronium 42-46 low density lipoprotein receptor Rattus norvegicus 150-162 17020999-0 2006 The combination of the rexinoid, LG100268, and a selective estrogen receptor modulator, either arzoxifene or acolbifene, synergizes in the prevention and treatment of mammary tumors in an estrogen receptor-negative model of breast cancer. ritetronium 109-119 estrogen receptor 1 (alpha) Mus musculus 59-76 17020999-0 2006 The combination of the rexinoid, LG100268, and a selective estrogen receptor modulator, either arzoxifene or acolbifene, synergizes in the prevention and treatment of mammary tumors in an estrogen receptor-negative model of breast cancer. ritetronium 109-119 estrogen receptor 1 (alpha) Mus musculus 188-205 15925950-0 2005 Estrogen receptor alpha-mediated adiposity-lowering and hypocholesterolemic actions of the selective estrogen receptor modulator acolbifene. ritetronium 129-139 estrogen receptor 1 (alpha) Mus musculus 0-23 15925950-0 2005 Estrogen receptor alpha-mediated adiposity-lowering and hypocholesterolemic actions of the selective estrogen receptor modulator acolbifene. ritetronium 129-139 estrogen receptor 1 (alpha) Mus musculus 101-118 15925950-1 2005 OBJECTIVE: The selective estrogen receptor (ER) modulator (SERM) acolbifene (ACOL), a potent and pure antiestrogen in the mammary gland and uterus, exerts beneficial pro-estrogenic actions on energy balance, insulin sensitivity and lipid metabolism. ritetronium 65-75 estrogen receptor 1 (alpha) Mus musculus 25-42 15925950-1 2005 OBJECTIVE: The selective estrogen receptor (ER) modulator (SERM) acolbifene (ACOL), a potent and pure antiestrogen in the mammary gland and uterus, exerts beneficial pro-estrogenic actions on energy balance, insulin sensitivity and lipid metabolism. ritetronium 65-75 estrogen receptor 1 (alpha) Mus musculus 44-46 15925950-1 2005 OBJECTIVE: The selective estrogen receptor (ER) modulator (SERM) acolbifene (ACOL), a potent and pure antiestrogen in the mammary gland and uterus, exerts beneficial pro-estrogenic actions on energy balance, insulin sensitivity and lipid metabolism. ritetronium 77-81 estrogen receptor 1 (alpha) Mus musculus 25-42 15925950-1 2005 OBJECTIVE: The selective estrogen receptor (ER) modulator (SERM) acolbifene (ACOL), a potent and pure antiestrogen in the mammary gland and uterus, exerts beneficial pro-estrogenic actions on energy balance, insulin sensitivity and lipid metabolism. ritetronium 77-81 estrogen receptor 1 (alpha) Mus musculus 44-46 15741653-0 2005 Hypolipidemic action of the SERM acolbifene is associated with decreased liver MTP and increased SR-BI and LDL receptors. ritetronium 33-43 scavenger receptor class B member 1 Homo sapiens 97-102 15741653-6 2005 However, in the fasted state, liver concentration of scavenger receptor class B type I (SR-BI) protein, but not mRNA, was 3-fold higher in ACOL-treated than in control animals and correlated with plasma HDL-CHOL levels (r = 0.80, P < 0.002). ritetronium 139-143 scavenger receptor class B member 1 Homo sapiens 53-86 15741653-6 2005 However, in the fasted state, liver concentration of scavenger receptor class B type I (SR-BI) protein, but not mRNA, was 3-fold higher in ACOL-treated than in control animals and correlated with plasma HDL-CHOL levels (r = 0.80, P < 0.002). ritetronium 139-143 scavenger receptor class B member 1 Homo sapiens 88-93 12554772-6 2003 Similarly, treatment with the antagonists 4-hydroxytamoxifen and EM-652 abolished all interactions between ERalpha and the SRC RIDs. ritetronium 65-71 estrogen receptor 1 Homo sapiens 107-114 15720121-10 2005 Incubations of acolbifene with GSH and either tyrosinase or human and rat liver microsomes also produced acolbifene quinone methide-GSH conjugates. ritetronium 15-25 tyrosinase Homo sapiens 46-56 15544933-4 2004 SCH 57068 also significantly reduced the increase in bone turnover markers, serum pyridinoline and serum osteocalcin levels, induced by OVX, and increased mechanical bone strength. ritetronium 0-9 bone gamma-carboxyglutamate protein Rattus norvegicus 105-116 11850228-2 2001 EM-652 inhibits the AF-1 and AF-2 functions of both ERalpha and beta while the inhibitory action of OH-TAM is limited to AF-2. ritetronium 0-6 estrogen receptor 1 Homo sapiens 52-59 12566126-0 2003 Acute vascular effects of the selective estrogen receptor modulator EM-652 (SCH 57068) in the rat mesenteric vascular bed. ritetronium 76-85 estrogen receptor 1 Rattus norvegicus 40-57 12566126-12 2003 The estrogen receptor (ER) antagonist ICI 182,780 attenuated E2-induced relaxations but only partially block the effects of EM-652. ritetronium 124-130 estrogen receptor 1 Rattus norvegicus 23-25 12566126-15 2003 EM-652 attenuated the vasoconstrictor responses induced by adrenergic agonists and endothelin-1. ritetronium 0-6 endothelin 1 Rattus norvegicus 83-95 31289113-11 2019 Structural features of bazedoxifene and lasofoxifene contributed to AOX1 inhibition, whereas those of acolbifene rendered it considerably less susceptible to AOX1 inhibition. ritetronium 102-112 aldehyde oxidase 1 Homo sapiens 158-162 9605415-4 1998 EM-652 is 20x more potent than ICI 164384 and Droloxifene while it is 400 times more potent than Toremifene in displacing [3H]E2 from the rat uterine estrogen receptor. ritetronium 0-6 estrogen receptor 1 Rattus norvegicus 150-167 31289113-3 2019 Therefore, a detailed in vitro and in silico study involving parent drugs and their analogs was conducted to investigate the effect of specific SERMs, particularly acolbifene, bazedoxifene, and lasofoxifene on AOX1 catalytic activity, as assessed by carbazeran 4-oxidation, an AOX1-selective catalytic marker. ritetronium 164-174 aldehyde oxidase 1 Homo sapiens 210-214 31289113-4 2019 The rank order in the potency (based on IC50 values) of AOX1 inhibition by SERMs was raloxifene > bazedoxifene ~ lasofoxifene > tamoxifen > acolbifene. ritetronium 149-159 aldehyde oxidase 1 Homo sapiens 56-60 10418981-9 1999 EM-652 has the most potent inhibitory activity on both ER alpha and ER beta compared to any of the other antiestrogens tested. ritetronium 0-6 estrogen receptor 1 Homo sapiens 55-63 10418981-9 1999 EM-652 has the most potent inhibitory activity on both ER alpha and ER beta compared to any of the other antiestrogens tested. ritetronium 0-6 estrogen receptor 2 Homo sapiens 68-75 10418981-10 1999 An important aspect of EM-652 is that it inhibits both the AF1 and AF2 functions of both ER alpha and ER beta while the inhibitory action of hydroxytamoxifen is limited to AF2, the ligand-dependent function of the estrogen receptors. ritetronium 23-29 interferon gamma receptor 2 Homo sapiens 59-62 10418981-10 1999 An important aspect of EM-652 is that it inhibits both the AF1 and AF2 functions of both ER alpha and ER beta while the inhibitory action of hydroxytamoxifen is limited to AF2, the ligand-dependent function of the estrogen receptors. ritetronium 23-29 estrogen receptor 1 Homo sapiens 89-97 10418981-10 1999 An important aspect of EM-652 is that it inhibits both the AF1 and AF2 functions of both ER alpha and ER beta while the inhibitory action of hydroxytamoxifen is limited to AF2, the ligand-dependent function of the estrogen receptors. ritetronium 23-29 estrogen receptor 2 Homo sapiens 102-109 10418981-12 1999 EM-652 inhibits Ras-induced transcriptional activity of ER alpha and ER beta and blocks SRC-1-stimulated activity of the two receptors. ritetronium 0-6 estrogen receptor 1 Homo sapiens 56-64 10418981-12 1999 EM-652 inhibits Ras-induced transcriptional activity of ER alpha and ER beta and blocks SRC-1-stimulated activity of the two receptors. ritetronium 0-6 estrogen receptor 2 Homo sapiens 69-76 10418981-12 1999 EM-652 inhibits Ras-induced transcriptional activity of ER alpha and ER beta and blocks SRC-1-stimulated activity of the two receptors. ritetronium 0-6 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 88-93 10418981-13 1999 EM-652 was also found to block the recruitment of SRC-1 at AF1 of ER beta, this ligand-independent activation of AF1 being closely related to phosphorylation of the steroid receptors by protein kinase. ritetronium 0-6 SRC proto-oncogene, non-receptor tyrosine kinase Homo sapiens 50-55 10418981-13 1999 EM-652 was also found to block the recruitment of SRC-1 at AF1 of ER beta, this ligand-independent activation of AF1 being closely related to phosphorylation of the steroid receptors by protein kinase. ritetronium 0-6 interferon gamma receptor 2 Homo sapiens 59-62 10418981-13 1999 EM-652 was also found to block the recruitment of SRC-1 at AF1 of ER beta, this ligand-independent activation of AF1 being closely related to phosphorylation of the steroid receptors by protein kinase. ritetronium 0-6 estrogen receptor 2 Homo sapiens 66-73 10418981-13 1999 EM-652 was also found to block the recruitment of SRC-1 at AF1 of ER beta, this ligand-independent activation of AF1 being closely related to phosphorylation of the steroid receptors by protein kinase. ritetronium 0-6 interferon gamma receptor 2 Homo sapiens 113-116 9421405-5 1998 EM-652 is also very effective in abrogating E2-stimulated ER alpha and ER beta trans-activation of the pS2 promoter in HeLa cells. ritetronium 0-6 estrogen receptor 1 Homo sapiens 58-66 9421405-5 1998 EM-652 is also very effective in abrogating E2-stimulated ER alpha and ER beta trans-activation of the pS2 promoter in HeLa cells. ritetronium 0-6 estrogen receptor 2 Homo sapiens 71-78 9421405-5 1998 EM-652 is also very effective in abrogating E2-stimulated ER alpha and ER beta trans-activation of the pS2 promoter in HeLa cells. ritetronium 0-6 trefoil factor 1 Homo sapiens 103-106