PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 33589424-6 2021 We experimentally validated that the SMAC mimetic birinapant upregulates MHC-I, sensitizes cancer cells to T-cell-dependent killing, and adds to ICB efficacy. birinapant 50-60 diablo IAP-binding mitochondrial protein Homo sapiens 37-41 33108350-4 2020 Here, we show that knockdown of CASP8 renders HNSCCs susceptible to necroptosis by a second mitochondria-derived activator of caspase (SMAC) mimetic, Birinapant, in combination with pan-caspase inhibitors zVAD FMK or Emricasan and radiation. birinapant 150-160 diablo IAP-binding mitochondrial protein Homo sapiens 85-133 34050412-1 2021 We studied the effects of birinapant, a mimetic of the second mitochondria-derived activator of caspase (SMAC), on invasion and proliferation of MGC-803 gastric cancer cells and the molecular mechanisms underlying these processes. birinapant 26-36 diablo IAP-binding mitochondrial protein Homo sapiens 105-109 33334024-2 2020 Birinapant, a synthetic second mitochondrial activator of caspases (SMAC) mimetic, suppresses the functions of IAP proteins in order to enhance apoptotic pathways and facilitate tumor death. birinapant 0-10 diablo IAP-binding mitochondrial protein Homo sapiens 68-72 33097020-2 2020 Standard-of-care paclitaxel (PTX), combined with birinapant (BRP), a bivalent mimetic of the apoptosis antagonist SMAC (second mitochondria-derived activator of caspases), exerts synergistic killing of PANC-1 human pancreatic adenocarcinoma cells. birinapant 49-59 diablo IAP-binding mitochondrial protein Homo sapiens 114-118 33097020-2 2020 Standard-of-care paclitaxel (PTX), combined with birinapant (BRP), a bivalent mimetic of the apoptosis antagonist SMAC (second mitochondria-derived activator of caspases), exerts synergistic killing of PANC-1 human pancreatic adenocarcinoma cells. birinapant 49-59 diablo IAP-binding mitochondrial protein Homo sapiens 120-169 26944210-2 2016 Here, we report that small-molecule Smac mimetics (i.e. BV6, LCL161, birinapant) that neutralize x-linked IAP (XIAP), cellular IAP (cIAP)1 and cIAP2 cooperate with demethylating agents (i.e. 5-azacytidine (5AC) or 5-aza-2"-deoxycytidine (DAC)) to induce cell death in ALL cells. birinapant 69-79 diablo IAP-binding mitochondrial protein Homo sapiens 36-40 30344003-4 2018 We found that DIABLO/SMAC mimetics (birinapant, GDC-0152, and embelin) selectively kill HIV-TCM without increasing virus production or targeting uninfected TCM. birinapant 36-46 diablo IAP-binding mitochondrial protein Homo sapiens 14-20 30344003-4 2018 We found that DIABLO/SMAC mimetics (birinapant, GDC-0152, and embelin) selectively kill HIV-TCM without increasing virus production or targeting uninfected TCM. birinapant 36-46 diablo IAP-binding mitochondrial protein Homo sapiens 21-25 29467909-2 2018 Using SMAC mimetic compounds, including birinapant, to degrade and/or inhibit these proteins and sensitize apoptosis may enhance therapies in HNSCC. birinapant 40-50 diablo IAP-binding mitochondrial protein Homo sapiens 6-10 29467909-4 2018 These cell lines were treated with Fas ligand-Fc (FasL) and birinapant, a bivalent SMAC mimetic, in mono and combination therapies. birinapant 60-70 diablo IAP-binding mitochondrial protein Homo sapiens 83-87 28460471-3 2017 We here showed that Norcantharidin, a drug that is currently being used in cancer treatment, significantly enhanced SMAC mimetic Birinapant-mediated cell viability inhibition and robustly promoted apoptosis in established breast carcinoma cell lines, as well as in primary breast carcinoma cells. birinapant 129-139 diablo IAP-binding mitochondrial protein Homo sapiens 116-120 27469115-0 2016 SMAC Mimetic Birinapant plus Radiation Eradicates Human Head and Neck Cancers with Genomic Amplifications of Cell Death Genes FADD and BIRC2. birinapant 13-23 diablo IAP-binding mitochondrial protein Homo sapiens 0-4 27469115-4 2016 Birinapant, a novel SMAC mimetic, sensitized multiple HNSCC lines to cell death by agonists TNFalpha or TRAIL and inhibited cIAP1>XIAP>IAP2. birinapant 0-10 diablo IAP-binding mitochondrial protein Homo sapiens 20-24 27469115-8 2016 In vivo, birinapant inhibited tumor growth and enhanced radiation-induced TNFalpha, tumor responses, and host survival in UM-SCC-46 and -11B xenograft models displaying amplification and overexpression of FADD+/- BIRC2 These findings suggest that combination of SMAC mimetics such as birinapant plus radiation may be particularly active in HNSCC, which harbor frequent FADD/BIRC2 genomic alterations. birinapant 9-19 diablo IAP-binding mitochondrial protein Homo sapiens 262-266 32341449-0 2020 Targeting triple-negative breast cancers with the Smac-mimetic birinapant. birinapant 63-73 diablo IAP-binding mitochondrial protein Homo sapiens 50-54 27302164-0 2016 Acute Sensitivity of Ph-like Acute Lymphoblastic Leukemia to the SMAC-Mimetic Birinapant. birinapant 78-88 diablo IAP-binding mitochondrial protein Homo sapiens 65-69 27302164-2 2016 In this study, we evaluated the efficacy of birinapant, a small-molecule mimetic of the apoptotic regulator SMAC, against a diverse set of ALL subtypes. birinapant 44-54 diablo IAP-binding mitochondrial protein Homo sapiens 108-112 27302164-8 2016 In combination therapy, birinapant enhanced the in vivo efficacy of an induction-type regimen of vincristine, dexamethasone, and L-asparaginase against Ph-like ALL xenografts, offering a preclinical rationale to further evaluate this SMAC mimetic for BCP-ALL treatment. birinapant 24-34 diablo IAP-binding mitochondrial protein Homo sapiens 234-238 27194727-0 2016 The caspase-8 inhibitor emricasan combines with the SMAC mimetic birinapant to induce necroptosis and treat acute myeloid leukemia. birinapant 65-75 diablo IAP-binding mitochondrial protein Homo sapiens 52-56 27194727-2 2016 Birinapant, a clinical SMAC mimetic, had been designed to mimic the interaction between inhibitor of apoptosis proteins (IAPs) and SMAC/Diablo, thereby relieving IAP-mediated caspase inhibition and promoting apoptosis of cancer cells. birinapant 0-10 diablo IAP-binding mitochondrial protein Homo sapiens 23-27 27194727-2 2016 Birinapant, a clinical SMAC mimetic, had been designed to mimic the interaction between inhibitor of apoptosis proteins (IAPs) and SMAC/Diablo, thereby relieving IAP-mediated caspase inhibition and promoting apoptosis of cancer cells. birinapant 0-10 diablo IAP-binding mitochondrial protein Homo sapiens 131-135 27194727-2 2016 Birinapant, a clinical SMAC mimetic, had been designed to mimic the interaction between inhibitor of apoptosis proteins (IAPs) and SMAC/Diablo, thereby relieving IAP-mediated caspase inhibition and promoting apoptosis of cancer cells. birinapant 0-10 diablo IAP-binding mitochondrial protein Homo sapiens 136-142 26567362-4 2015 Currently, several Smac mimetics are under evaluation in early clinical trials as monotherapy or in rational combinations (i.e., GDC-0917/CUDC-427, LCL161, AT-406/Debio1143, HGS1029, and TL32711/birinapant). birinapant 187-194 diablo IAP-binding mitochondrial protein Homo sapiens 19-23 26566079-0 2016 Pharmacodynamic markers and clinical results from the phase 2 study of the SMAC mimetic birinapant in women with relapsed platinum-resistant or -refractory epithelial ovarian cancer. birinapant 88-98 diablo IAP-binding mitochondrial protein Homo sapiens 75-79 26446940-0 2016 Effect of a Smac Mimetic (TL32711, Birinapant) on the Apoptotic Program and Apoptosis Biomarkers Examined with Validated Multiplex Immunoassays Fit for Clinical Use. birinapant 26-33 diablo IAP-binding mitochondrial protein Homo sapiens 12-16 26446940-0 2016 Effect of a Smac Mimetic (TL32711, Birinapant) on the Apoptotic Program and Apoptosis Biomarkers Examined with Validated Multiplex Immunoassays Fit for Clinical Use. birinapant 35-45 diablo IAP-binding mitochondrial protein Homo sapiens 12-16 26446940-1 2016 PURPOSE: To support clinical pharmacodynamic evaluation of the Smac mimetic TL32711 (birinapant) and other apoptosis-targeting drugs, we describe the development, validation, and application of novel immunoassays for 15 cytosolic and membrane-associated proteins indicative of the induction, onset, and commitment to apoptosis in human tumors. birinapant 76-83 diablo IAP-binding mitochondrial protein Homo sapiens 63-67 26446940-1 2016 PURPOSE: To support clinical pharmacodynamic evaluation of the Smac mimetic TL32711 (birinapant) and other apoptosis-targeting drugs, we describe the development, validation, and application of novel immunoassays for 15 cytosolic and membrane-associated proteins indicative of the induction, onset, and commitment to apoptosis in human tumors. birinapant 85-95 diablo IAP-binding mitochondrial protein Homo sapiens 63-67 26859455-1 2016 Birinapant is a smac-mimetic (SM) in clinical trials for treating cancer. birinapant 0-10 diablo IAP-binding mitochondrial protein Homo sapiens 16-20 26985322-1 2016 Birinapant/TL32711 (1) is a bivalent antagonist of the inhibitor of apoptosis (IAP) family of proteins and was designed to mimic AVPI, the N-terminal tetrapeptide of the second mitochondria-derived activator of caspases (Smac/DIABLO). birinapant 0-10 diablo IAP-binding mitochondrial protein Homo sapiens 221-225 26985322-1 2016 Birinapant/TL32711 (1) is a bivalent antagonist of the inhibitor of apoptosis (IAP) family of proteins and was designed to mimic AVPI, the N-terminal tetrapeptide of the second mitochondria-derived activator of caspases (Smac/DIABLO). birinapant 0-10 diablo IAP-binding mitochondrial protein Homo sapiens 226-232 26985322-1 2016 Birinapant/TL32711 (1) is a bivalent antagonist of the inhibitor of apoptosis (IAP) family of proteins and was designed to mimic AVPI, the N-terminal tetrapeptide of the second mitochondria-derived activator of caspases (Smac/DIABLO). birinapant 11-18 diablo IAP-binding mitochondrial protein Homo sapiens 221-225 26985322-1 2016 Birinapant/TL32711 (1) is a bivalent antagonist of the inhibitor of apoptosis (IAP) family of proteins and was designed to mimic AVPI, the N-terminal tetrapeptide of the second mitochondria-derived activator of caspases (Smac/DIABLO). birinapant 11-18 diablo IAP-binding mitochondrial protein Homo sapiens 226-232 26567362-4 2015 Currently, several Smac mimetics are under evaluation in early clinical trials as monotherapy or in rational combinations (i.e., GDC-0917/CUDC-427, LCL161, AT-406/Debio1143, HGS1029, and TL32711/birinapant). birinapant 195-205 diablo IAP-binding mitochondrial protein Homo sapiens 19-23 26095377-2 2015 Recent advances in the development of novel Smac-derived peptidomimetics and non-peptidic molecules with improved anti-IAPs activity and resistance to proteolytic cleavage have been reported and led to a number of candidates that are currently in clinical trials including LCL-161, SM-406/AT-406, GDC-0512/GDC-0917, and birinapant. birinapant 320-330 diablo IAP-binding mitochondrial protein Homo sapiens 44-48 26333381-0 2015 A Phase I Study of the SMAC-Mimetic Birinapant in Adults with Refractory Solid Tumors or Lymphoma. birinapant 36-46 diablo IAP-binding mitochondrial protein Homo sapiens 23-27 26333381-3 2015 Here, we report a first-in-human trial designed to determine the maximum tolerated dose (MTD), safety, and pharmacokinetics/pharmacodynamics (PK/PD) of birinapant, a novel SMAC mimetic. birinapant 152-162 diablo IAP-binding mitochondrial protein Homo sapiens 172-176 25902530-5 2015 Here, we show using an immunocompetent mouse model of chronic HBV infection that birinapant and other Smac mimetics are able to rapidly reduce serum HBV DNA and serum HBV surface antigen, and they promote the elimination of hepatocytes containing HBV core antigen. birinapant 81-91 diablo IAP-binding mitochondrial protein Homo sapiens 102-106 24684347-0 2014 Birinapant, a smac-mimetic with improved tolerability for the treatment of solid tumors and hematological malignancies. birinapant 0-10 diablo IAP-binding mitochondrial protein Homo sapiens 14-18 24563541-0 2014 Birinapant (TL32711), a bivalent SMAC mimetic, targets TRAF2-associated cIAPs, abrogates TNF-induced NF-kappaB activation, and is active in patient-derived xenograft models. birinapant 0-10 diablo IAP-binding mitochondrial protein Homo sapiens 33-37 24563541-0 2014 Birinapant (TL32711), a bivalent SMAC mimetic, targets TRAF2-associated cIAPs, abrogates TNF-induced NF-kappaB activation, and is active in patient-derived xenograft models. birinapant 12-19 diablo IAP-binding mitochondrial protein Homo sapiens 33-37 24563541-6 2014 Here, we report the preclinical characterization of birinapant (TL32711), a bivalent SMAC-mimetic compound currently in clinical trials for the treatment of cancer. birinapant 52-62 diablo IAP-binding mitochondrial protein Homo sapiens 85-89 24563541-6 2014 Here, we report the preclinical characterization of birinapant (TL32711), a bivalent SMAC-mimetic compound currently in clinical trials for the treatment of cancer. birinapant 64-71 diablo IAP-binding mitochondrial protein Homo sapiens 85-89 23403634-0 2013 The novel SMAC mimetic birinapant exhibits potent activity against human melanoma cells. birinapant 23-33 diablo IAP-binding mitochondrial protein Homo sapiens 10-14 23225169-3 2013 Here, we report for the first time that bivalent Smac mimetic Birinapant induces cell death as a single agent in TRAIL-insensitive SUM190 (ErbB2-overexpressing) cells and significantly increases potency of TRAIL-induced apoptosis in TRAIL-sensitive SUM149 (triple-negative, EGFR-activated) cells, two patient tumor-derived IBC models. birinapant 62-72 diablo IAP-binding mitochondrial protein Homo sapiens 49-53 24526787-2 2014 Here, we identify deregulated apoptotic components in AML stem/progenitor cells and investigate the individual and combinatorial effects of the novel inhibitor of apoptosis (IAP) protein antagonist and second mitochondrial-derived activator of caspases (SMAC) mimetic birinapant and demethylating epigenetic modulators. birinapant 268-278 diablo IAP-binding mitochondrial protein Homo sapiens 202-252 23225169-0 2013 Smac mimetic Birinapant induces apoptosis and enhances TRAIL potency in inflammatory breast cancer cells in an IAP-dependent and TNF-alpha-independent mechanism. birinapant 13-23 diablo IAP-binding mitochondrial protein Homo sapiens 0-4