Publications by authors named "George Sheppard"

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Discovery of -Ethyl-4-[2-(4-fluoro-2,6-dimethyl-phenoxy)-5-(1-hydroxy-1-methyl-ethyl)phenyl]-6-methyl-7-oxo-1-pyrrolo[2,3-]pyridine-2-carboxamide (ABBV-744), a BET Bromodomain Inhibitor with Selectivity for the Second Bromodomain.
George S Sheppard, Le Wang, Steven D Fidanze, Lisa A Hasvold, Dachun Liu

J Med Chem· May 2020

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Selective inhibition of the BD2 bromodomain of BET proteins in prostate cancer.
Emily J Faivre, Keith F McDaniel, Daniel H Albert, Srinivasa R Mantena, Joshua P Plotnik, George S Sheppard

Nature· February 2020

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Discovery and optimization of novel constrained pyrrolopyridone BET family inhibitors.
Steven D Fidanze, Dachun Liu, Robert A Mantei, Lisa A Hasvold, John K Pratt, George S Sheppard

Bioorg Med Chem Lett· June 2018

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Discovery of N-(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor.
Keith F McDaniel, Le Wang, Todd Soltwedel, Steven D Fidanze, Lisa A Hasvold, George S Sheppard

J Med Chem· October 2017

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Preclinical Characterization of BET Family Bromodomain Inhibitor ABBV-075 Suggests Combination Therapeutic Strategies.
Mai H Bui, Xiaoyu Lin, Daniel H Albert, Leiming Li, Lloyd T Lam, George S Sheppard

Cancer Res· June 2017

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Methylpyrrole inhibitors of BET bromodomains.
Lisa A Hasvold, George S Sheppard, Le Wang, Steven D Fidanze, Dachun Liu

Bioorg Med Chem Lett· May 2017

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Fragment-Based, Structure-Enabled Discovery of Novel Pyridones and Pyridone Macrocycles as Potent Bromodomain and Extra-Terminal Domain (BET) Family Bromodomain Inhibitors.
Le Wang, John K Pratt, Todd Soltwedel, George S Sheppard, Steven D Fidanze

J Med Chem· May 2017

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MCL-1 Is a Key Determinant of Breast Cancer Cell Survival: Validation of MCL-1 Dependency Utilizing a Highly Selective Small Molecule Inhibitor.
Yu Xiao, Paul Nimmer, George S Sheppard, Milan Bruncko, Paul Hessler

Mol Cancer Ther· August 2015

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Correction to Structure-Guided Design of a Series of MCL-1 Inhibitors with High Affinity and Selectivity.
Milan Bruncko, Le Wang, George S Sheppard, Darren C Phillips, Stephen K Tahir

J Med Chem· May 2015

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Structure-guided design of a series of MCL-1 inhibitors with high affinity and selectivity.
Milan Bruncko, Le Wang, George S Sheppard, Darren C Phillips, Stephen K Tahir

J Med Chem· March 2015

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Substituted 4-amino-1H-pyrazolo[3,4-d]pyrimidines as multi-targeted inhibitors of insulin-like growth factor-1 receptor (IGF1R) and members of ErbB-family receptor kinases.
Gary T Wang, Robert A Mantei, Robert D Hubbard, Julie L Wilsbacher, Qian Zhang, George S Sheppard

Bioorg Med Chem Lett· October 2010

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Imidazo[2,1-b]thiazoles: multitargeted inhibitors of both the insulin-like growth factor receptor and members of the epidermal growth factor family of receptor tyrosine kinases.
Steve D Fidanze, Scott A Erickson, Gary T Wang, Robert Mantei, Richard F Clark, George S Sheppard

Bioorg Med Chem Lett· April 2010

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Reversal of oncogene transformation and suppression of tumor growth by the novel IGF1R kinase inhibitor A-928605.
William N Pappano, Paul M Jung, Jonathan A Meulbroek, Yi-Chun Wang, Robert D Hubbard, George S Sheppard

BMC Cancer· September 2009

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Analyzing the binding of Co(II)-specific inhibitors to the methionyl aminopeptidases from Escherichia coli and Pyrococcus furiosus.
Sanghamitra Mitra, George Sheppard, Jieyi Wang, Brian Bennett, Richard C Holz

J Biol Inorg Chem· May 2009

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Development of multitargeted inhibitors of both the insulin-like growth factor receptor (IGF-IR) and members of the epidermal growth factor family of receptor tyrosine kinases.
Robert D Hubbard, Nwe Y Bamaung, Steve D Fidanze, Scott A Erickson, Fabio Palazzo, George S Sheppard

Bioorg Med Chem Lett· March 2009

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Discovery, identification, and characterization of candidate pharmacodynamic markers of methionine aminopeptidase-2 inhibition.
Scott E Warder, Lora A Tucker, Shaun M McLoughlin, Tamara J Strelitzer, Joseph L Meuth, George S Sheppard

J Proteome Res· November 2008

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Insulin-like growth factor-1 receptor and ErbB kinase inhibitor combinations block proliferation and induce apoptosis through cyclin D1 reduction and Bax activation.
Julie L Wilsbacher, Qian Zhang, Lora A Tucker, Robert D Hubbard, George S Sheppard

J Biol Chem· August 2008

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Correlation of tumor growth suppression and methionine aminopetidase-2 activity blockade using an orally active inhibitor.
Jieyi Wang, Lora A Tucker, Jason Stavropoulos, Qian Zhang, Yi-Chun Wang, George S Sheppard

Proc Natl Acad Sci U S A· February 2008

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Pyrazolo[3,4-d]pyrimidines as potent inhibitors of the insulin-like growth factor receptor (IGF-IR).
Robert D Hubbard, Nwe Y Bamaung, Fabio Palazzo, Qian Zhang, Peter Kovar, George S Sheppard

Bioorg Med Chem Lett· October 2007

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Lead optimization of methionine aminopeptidase-2 (MetAP2) inhibitors containing sulfonamides of 5,6-disubstituted anthranilic acids.
Gary T Wang, Robert A Mantei, Megumi Kawai, Jason S Tedrow, David M Barnes, George S Sheppard

Bioorg Med Chem Lett· May 2007

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Development of sulfonamide compounds as potent methionine aminopeptidase type II inhibitors with antiproliferative properties.
Megumi Kawai, Nwe Y BaMaung, Steve D Fidanze, Scott A Erickson, Jason S Tedrow, George S Sheppard

Bioorg Med Chem Lett· July 2006

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Discovery and optimization of anthranilic acid sulfonamides as inhibitors of methionine aminopeptidase-2: a structural basis for the reduction of albumin binding.
George S Sheppard, Jieyi Wang, Megumi Kawai, Steve D Fidanze, Nwe Y BaMaung

J Med Chem· June 2006

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Methionine aminopeptidase 2 inhibition is an effective treatment strategy for neuroblastoma in preclinical models.
Michael J Morowitz, Rosalind Barr, Qun Wang, Rebecca King, Nicholas Rhodin, George S Sheppard

Clin Cancer Res· April 2005

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3-Amino-2-hydroxyamides and related compounds as inhibitors of methionine aminopeptidase-2.
George S Sheppard, Jieyi Wang, Megumi Kawai, Nwe Y BaMaung, Richard A Craig

Bioorg Med Chem Lett· February 2004

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Lysyl 4-aminobenzoic acid derivatives as potent small molecule mimetics of plasminogen kringle 5.
George S Sheppard, Megumi Kawai, Richard A Craig, Donald J Davidson, Sandra M Majest

Bioorg Med Chem Lett· February 2004

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