Discovery of BMS-641988, a novel and potent inhibitor of androgen receptor signaling for the treatment of prostate cancer.

PubWeight™: 0.99‹?› | Rank: Top 15%

🔗 View Article (PMID 19654297)

Published in Cancer Res on August 04, 2009

Authors

Ricardo M Attar1, Maria Jure-Kunkel, Aaron Balog, Mary Ellen Cvijic, Janet Dell-John, Cheryl A Rizzo, Liang Schweizer, Thomas E Spires, J Suso Platero, Mary Obermeier, Weifang Shan, Mark E Salvati, William R Foster, Joseph Dinchuk, Shen-Jue Chen, Gregory Vite, Robert Kramer, Marco M Gottardis

Author Affiliations

1: Bristol-Myers Squibb Company, Princeton, New Jersey, USA. rattar1@its.jnj.com

Articles by these authors

Safety, activity, and immune correlates of anti-PD-1 antibody in cancer. N Engl J Med (2012) 52.99

An immune-active tumor microenvironment favors clinical response to ipilimumab. Cancer Immunol Immunother (2011) 4.02

Wnt signals across the plasma membrane to activate the beta-catenin pathway by forming oligomers containing its receptors, Frizzled and LRP. Development (2004) 2.84

Insulin-mediated acceleration of breast cancer development and progression in a nonobese model of type 2 diabetes. Cancer Res (2010) 2.13

Challenges in meeting fellowship procedural guidelines in pediatric therapeutic endoscopy and liver biopsy. J Pediatr Gastroenterol Nutr (2014) 2.12

The HIF-1α hypoxia response in tumor-infiltrating T lymphocytes induces functional CD137 (4-1BB) for immunotherapy. Cancer Discov (2012) 1.95

Constitutively active type I insulin-like growth factor receptor causes transformation and xenograft growth of immortalized mammary epithelial cells and is accompanied by an epithelial-to-mesenchymal transition mediated by NF-kappaB and snail. Mol Cell Biol (2007) 1.89

Management of ingested magnets in children. J Pediatr Gastroenterol Nutr (2012) 1.78

The mechanisms of differential sensitivity to an insulin-like growth factor-1 receptor inhibitor (BMS-536924) and rationale for combining with EGFR/HER2 inhibitors. Cancer Res (2009) 1.78

Castration-resistant prostate cancer: locking up the molecular escape routes. Clin Cancer Res (2009) 1.72

BMS-754807, a small molecule inhibitor of insulin-like growth factor-1R/IR. Mol Cancer Ther (2009) 1.62

Dasatinib (BMS-354825) pharmacokinetics and pharmacodynamic biomarkers in animal models predict optimal clinical exposure. Clin Cancer Res (2006) 1.61

Drug safety is a barrier to the discovery and development of new androgen receptor antagonists. Prostate (2010) 1.54

Preclinical efficacy spectrum and pharmacokinetics of ixabepilone. Cancer Chemother Pharmacol (2008) 1.53

Casein kinase Iepsilon modulates the signaling specificities of dishevelled. Mol Cell Biol (2004) 1.41

HER receptor signaling confers resistance to the insulin-like growth factor-I receptor inhibitor, BMS-536924. Mol Cancer Ther (2008) 1.40

N-(cycloalkylamino)acyl-2-aminothiazole inhibitors of cyclin-dependent kinase 2. N-[5-[[[5-(1,1-dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]-4- piperidinecarboxamide (BMS-387032), a highly efficacious and selective antitumor agent. J Med Chem (2004) 1.39

Reinventing the wheel of cyclic AMP: novel mechanisms of cAMP signaling. Ann N Y Acad Sci (2002) 1.26

Agonist anti-CD137 mAb act on tumor endothelial cells to enhance recruitment of activated T lymphocytes. Cancer Res (2011) 1.23

Differential mechanisms of acquired resistance to insulin-like growth factor-i receptor antibody therapy or to a small-molecule inhibitor, BMS-754807, in a human rhabdomyosarcoma model. Cancer Res (2010) 1.22

The androgen receptor can signal through Wnt/beta-Catenin in prostate cancer cells as an adaptation mechanism to castration levels of androgens. BMC Cell Biol (2008) 1.21

High IGF-IR activity in triple-negative breast cancer cell lines and tumorgrafts correlates with sensitivity to anti-IGF-IR therapy. Clin Cancer Res (2010) 1.20

Preclinical discovery of ixabepilone, a highly active antineoplastic agent. Cancer Chemother Pharmacol (2008) 1.19

Established B16 tumors are rejected following treatment with GM-CSF-secreting tumor cell immunotherapy in combination with anti-4-1BB mAb. Clin Immunol (2007) 1.19

Discovery of aminothiazole inhibitors of cyclin-dependent kinase 2: synthesis, X-ray crystallographic analysis, and biological activities. J Med Chem (2002) 1.18

Treatment with anti-CD137 mAbs causes intense accumulations of liver T cells without selective antitumor immunotherapeutic effects in this organ. Cancer Immunol Immunother (2010) 1.15

Requirement for a nuclear function of beta-catenin in Wnt signaling. Mol Cell Biol (2003) 1.14

Quality indicators increase the reliability of microarray data. Genomics (2002) 1.14

Eosinophilic esophagitis: the newest esophageal inflammatory disease. Nat Rev Gastroenterol Hepatol (2009) 1.09

Synthetic lethality screens reveal RPS6 and MST1R as modifiers of insulin-like growth factor-1 receptor inhibitor activity in childhood sarcomas. Cancer Res (2010) 1.08

Discovery and validation of biomarkers that respond to treatment with brivanib alaninate, a small-molecule VEGFR-2/FGFR-1 antagonist. Cancer Res (2007) 1.08

Combined immunostimulatory monoclonal antibodies extend survival in an aggressive transgenic hepatocellular carcinoma mouse model. Clin Cancer Res (2013) 1.05

Dual IGF-1R/InsR inhibitor BMS-754807 synergizes with hormonal agents in treatment of estrogen-dependent breast cancer. Cancer Res (2011) 1.04

Synergistic antitumor activity of ixabepilone (BMS-247550) plus bevacizumab in multiple in vivo tumor models. Clin Cancer Res (2008) 1.02

ETV6-NTRK3-mediated breast epithelial cell transformation is blocked by targeting the IGF1R signaling pathway. Cancer Res (2010) 1.02

IGFBP ratio confers resistance to IGF targeting and correlates with increased invasion and poor outcome in breast tumors. Clin Cancer Res (2012) 1.01

Discovery of a 2,4-disubstituted pyrrolo[1,2-f][1,2,4]triazine inhibitor (BMS-754807) of insulin-like growth factor receptor (IGF-1R) kinase in clinical development. J Med Chem (2009) 0.98

Identification of a novel class of androgen receptor antagonists based on the bicyclic-1H-isoindole-1,3(2H)-dione nucleus. Bioorg Med Chem Lett (2005) 0.98

BMS-536924 reverses IGF-IR-induced transformation of mammary epithelial cells and causes growth inhibition and polarization of MCF7 cells. Clin Cancer Res (2009) 0.97

2-Arylbenzoxazoles as novel cholesteryl ester transfer protein inhibitors: optimization via array synthesis. Bioorg Med Chem Lett (2008) 0.97

Interlaboratory evaluation of genomic signatures for predicting carcinogenicity in the rat. Toxicol Sci (2008) 0.96

Targeting epigenetic regulators for cancer therapy. Ann N Y Acad Sci (2014) 0.95

GREB1 is a novel androgen-regulated gene required for prostate cancer growth. Prostate (2006) 0.94

Identification and optimization of a novel series of [2.2.1]-oxabicyclo imide-based androgen receptor antagonists. Bioorg Med Chem Lett (2008) 0.94

Molecular markers for novel therapies in neuroendocrine (carcinoid) tumors. Endocr Relat Cancer (2010) 0.94

Bin3 deletion causes cataracts and increased susceptibility to lymphoma during aging. Cancer Res (2008) 0.93

A fibronectin scaffold approach to bispecific inhibitors of epidermal growth factor receptor and insulin-like growth factor-I receptor. MAbs (2011) 0.92

Synergistic activity of ixabepilone plus other anticancer agents: preclinical and clinical evidence. Ther Adv Med Oncol (2011) 0.92

Drug-induced perturbations of the bile acid pool, cholestasis, and hepatotoxicity: mechanistic considerations beyond the direct inhibition of the bile salt export pump. Drug Metab Dispos (2013) 0.92

A retrospective analysis of toxicogenomics in the safety assessment of drug candidates. Toxicol Pathol (2007) 0.92

Acridone-based inhibitors of inosine 5'-monophosphate dehydrogenase: discovery and SAR leading to the identification of N-(2-(6-(4-ethylpiperazin-1-yl)pyridin-3-yl)propan-2-yl)-2- fluoro-9-oxo-9,10-dihydroacridine-3-carboxamide (BMS-566419). J Med Chem (2007) 0.91

Radiotherapy enhances antitumor effect of anti-CD137 therapy in a mouse Glioma model. Radiat Res (2010) 0.91

Discovery of the pyrrolo[2,1-f][1,2,4]triazine nucleus as a new kinase inhibitor template. J Med Chem (2004) 0.90

Inhibition of proliferation and estrogen receptor signaling by peroxisome proliferator-activated receptor gamma ligands in uterine leiomyoma. Cancer Res (2003) 0.90

Chemically synthesized molecules with the targeting and effector functions of antibodies. J Am Chem Soc (2014) 0.89

Design and synthesis of 4-[3,5-dioxo-11-oxa-4,9-diazatricyclo[5.3.1.0(2,6)]undec-4-yl]-2-trifluoromethyl-benzonitriles as androgen receptor antagonists. Bioorg Med Chem Lett (2010) 0.89

Drug efflux by breast cancer resistance protein is a mechanism of resistance to the benzimidazole insulin-like growth factor receptor/insulin receptor inhibitor, BMS-536924. Mol Cancer Ther (2011) 0.88

gamma-Lactams as glycinamide replacements in cyclohexane-based CC chemokine receptor 2 (CCR2) antagonists. Bioorg Med Chem Lett (2010) 0.88

Pyrrolopyridazine MEK inhibitors. Bioorg Med Chem Lett (2005) 0.88

Combined Inhibition of IGF-1R/IR and Src family kinases enhances antitumor effects in prostate cancer by decreasing activated survival pathways. PLoS One (2012) 0.88

BMS-536924 sensitizes human epithelial ovarian cancer cells to the PARP inhibitor, 3-aminobenzamide. Gynecol Oncol (2009) 0.85

Gene expression profiling of whole blood in ipilimumab-treated patients for identification of potential biomarkers of immune-related gastrointestinal adverse events. J Transl Med (2013) 0.85

T cell costimulation with anti-CD137 monoclonal antibodies is mediated by K63-polyubiquitin-dependent signals from endosomes. J Immunol (2013) 0.84

IGF signaling contributes to malignant transformation of hematopoietic progenitors by the MLL-AF9 oncoprotein. Exp Hematol (2012) 0.84

Structure based approach to the design of bicyclic-1H-isoindole-1,3(2H)-dione based androgen receptor antagonists. Bioorg Med Chem Lett (2005) 0.84

Development and evaluation of a genomic signature for the prediction and mechanistic assessment of nongenotoxic hepatocarcinogens in the rat. Toxicol Sci (2011) 0.83

Discovery of potent, orally-active, and muscle-selective androgen receptor modulators based on an N-aryl-hydroxybicyclohydantoin scaffold. J Med Chem (2006) 0.83

Discovery of a small molecule antagonist of the parathyroid hormone receptor by using an N-terminal parathyroid hormone peptide probe. Proc Natl Acad Sci U S A (2007) 0.83

A high-content glucocorticoid receptor translocation assay for compound mechanism-of-action evaluation. J Biomol Screen (2007) 0.83