K. Maegley

发表

Dihydroxylphenyl amides as inhibitors of the Hsp90 molecular chaperone.

L. Funk, P. Kung, J. Meng, 2008, Bioorganic & medicinal chemistry letters.

Design strategies to target crystallographic waters applied to the Hsp90 molecular chaperone.

K. Gajiwala, M. Hickey, P. Kung, 2011, Bioorganic & medicinal chemistry letters.

Discovery of a Novel and Selective Indoleamine 2,3-Dioxygenase (IDO-1) Inhibitor 3-(5-Fluoro-1H-indol-3-yl)pyrrolidine-2,5-dione (EOS200271/PF-06840003) and Its Characterization as a Potential Clinical Candidate.

S. Kaiser, M. Kraus, A. Stewart, 2017, Journal of medicinal chemistry.

31st Annual Meeting and Associated Programs of the Society for Immunotherapy of Cancer (SITC 2016): part two

Manish R. Patel, Charles J. Vaske, Joe Y. Chang, 2016, Journal for Immunotherapy of Cancer.

Targeting Divalent Metal Ions at the Active Site of the HIV-1 RNase H Domain: NMR Studies on the Interactions of Divalent Metal Ions with RNase H and Its Inhibitors

Jiangli Yan, K. Maegley, O. Brodsky, 2011 .

Structure of HIV-1 reverse transcriptase with the inhibitor beta-Thujaplicinol bound at the RNase H active site.

A. D. Clark, S. Hughes, E. Arnold, 2009, Structure.

Potentiation of cytotoxic drug activity in human tumour cell lines, by amine-substituted 2-arylbenzimidazole-4-carboxamide PARP-1 inhibitors.

N. Curtin, R. Griffin, B. Golding, 2004, Bioorganic & medicinal chemistry letters.

Synthesis and Biological Properties of Benzimidazole Inhibitors of the DNA Repair Enzyme Poly ( ADP-ribose ) Polymerase

N. Curtin, R. Griffin, B. Golding, 2022 .

Tricyclic benzimidazoles as potent poly(ADP-ribose) polymerase-1 inhibitors.

N. Curtin, R. Griffin, B. Golding, 2003, Journal of medicinal chemistry.

A fluorescence polarization assay for screening inhibitors against the ribonuclease H activity of HIV-1 reverse transcriptase.

K. Maegley, P. Bingham, G. Nakayama, 2006, Analytical biochemistry.

Characterization of the Selective Indoleamine 2,3-Dioxygenase-1 (IDO1) Catalytic Inhibitor EOS200271/PF-06840003 Supports IDO1 as a Critical Resistance Mechanism to PD-(L)1 Blockade Therapy

C. Dillon, Xianxian Zheng, M. Kraus, 2018, Molecular Cancer Therapeutics.

Design, synthesis, and evaluation of 3,4-dihydro-2H-[1,4]diazepino[6,7,1-hi]indol-1-ones as inhibitors of poly(ADP-ribose) polymerase.

N. Curtin, R. Griffin, B. Golding, 2004, Journal of medicinal chemistry.

Anticancer chemosensitization and radiosensitization by the novel poly(ADP-ribose) polymerase-1 inhibitor AG14361.

Robert Almassy, Kaye J Williams, N. Curtin, 2004, Journal of the National Cancer Institute.

Design, synthesis, and biological evaluation of novel human 5'-deoxy-5'-methylthioadenosine phosphorylase (MTAP) substrates.

L. Kuhn, P. W. Rose, P. Kung, 2005, Bioorganic & Medicinal Chemistry Letters.

Polycomb repressive complex 2 structure with inhibitor reveals a mechanism of activation and drug resistance

K. Gajiwala, P. Kung, A. Brooun, 2016, Nature Communications.

Optimization of Orally Bioavailable Enhancer of Zeste Homolog 2 (EZH2) Inhibitors Using Ligand and Property-Based Design Strategies: Identification of Development Candidate (R)-5,8-Dichloro-7-(methoxy(oxetan-3-yl)methyl)-2-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3,4-dihydroisoquin

K. Gajiwala, N. Sach, P. Kung, 2017, Journal of medicinal chemistry.

Design and Synthesis of Pyridone-Containing 3,4-Dihydroisoquinoline-1(2H)-ones as a Novel Class of Enhancer of Zeste Homolog 2 (EZH2) Inhibitors.

P. Kung, S. Yamazaki, M. Edwards, 2016, Journal of medicinal chemistry.

Design and Synthesis of Pyridone-Containing 3 , 4-Dihydroisoquinoline-1 ( 2 H ) ‐ ones as a Novel Class of Enhancer of Zeste Homolog 2 ( EZH 2 ) Inhibitors

P. Kung, S. Yamazaki, M. Edwards, 2016 .

SAH derived potent and selective EZH2 inhibitors.

K. Gajiwala, P. Kung, K. Maegley, 2015, Bioorganic & medicinal chemistry letters.

SAM-Competitive PRMT5 Inhibitor PF-06939999 Demonstrates Antitumor Activity in Splicing Dysregulated NSCLC with Decreased Liability of Drug Resistance

M. Tran-Dube, M. McTigue, S. Yamazaki, 2021, Molecular Cancer Therapeutics.

Preclinical selection of a novel poly(ADP-ribose) polymerase inhibitor for clinical trial

N. Curtin, D. Newell, Lan Z. Wang, 2007, Molecular Cancer Therapeutics.

Ras-catalyzed hydrolysis of GTP: a new perspective from model studies.

D. Herschlag, K. Maegley, S. J. Admiraal, 1996, Proceedings of the National Academy of Sciences of the United States of America.

Development of hepatitis C virus chimeric replicons for identifying broad spectrum NS3 protease inhibitors.

A. Patick, K. Maegley, R. Love, 2007, Antiviral research.

Conserved RNA-binding specificity of polycomb repressive complex 2 is achieved by dispersed amino acid patches in EZH2

T. Cech, K. Gajiwala, A. Gooding, 2017, eLife.

Ack1: Activation and Regulation by Allostery

K. Gajiwala, R. Ferre, K. Maegley, 2013, PloS one.

Novel tricyclic poly(ADP-ribose) polymerase-1 inhibitors with potent anticancer chemopotentiating activity: design, synthesis, and X-ray cocrystal structure.

N. Curtin, R. Griffin, B. Golding, 2002, Journal of medicinal chemistry.

Characterization of Specific N-α-Acetyltransferase 50 (Naa50) Inhibitors Identified Using a DNA Encoded Library.

W. K. Sonnenburg, P. Kung, Sergei L Timofeevski, 2020, ACS medicinal chemistry letters.

The crystal structure of the RNA-dependent RNA polymerase from human rhinovirus: a dual function target for common cold antiviral therapy.

P. Dragovich, H. Parge, R. Ferre, 2004, Structure.

DNA Bending by EcoRI DNA Methyltransferase Accelerates Base Flipping but Compromises Specificity*

J. Beechem, N. Reich, J. Mort, 1999, The Journal of Biological Chemistry.

Strategies employed for the development of PARP inhibitors.

N. Curtin, K. Maegley, Stacie Canan, 2011, Methods in molecular biology.

All PARP inhibitors are not equal: An in vitro mechanistic comparison of PF-01367338 to iniparib.

K. Maegley, P. Bingham, H. Thomas, 2011, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.

Identification of potent nontoxic poly(ADP-Ribose) polymerase-1 inhibitors: chemopotentiation and pharmacological studies.

N. Curtin, B. Durkacz, D. Newell, 2003, Clinical cancer research : an official journal of the American Association for Cancer Research.

Anti-cancer chemosensitization in vitro and in vivo by a novel potent poly(ADP-ribose) polymerase (PARP1) inhibitor, TBI-361.

N. Curtin, S. Barton, R. Griffin, 2001 .

Structural and functional analysis of EcoRI DNA methyltransferase by proteolysis.

D. Shoemaker, N. Reich, K. Maegley, 1991, Biochemistry.

Correction to Design and Synthesis of Pyridone-Containing 3,4-Dihydroisoquinoline-1(2H)-ones as a Novel Class of Enhancer of Zeste Homolog 2 (EZH2) Inhibitors.

P. Kung, S. Yamazaki, M. Edwards, 2016, Journal of Medicinal Chemistry.

Optimization of potent, selective, and orally bioavailable pyrrolodinopyrimidine-containing inhibitors of heat shock protein 90. Identification of development candidate 2-amino-4-{4-chloro-2-[2-(4-fluoro-1H-pyrazol-1-yl)ethoxy]-6-methylphenyl}-N-(2,2-difluoropropyl)-5,7-dihydro-6H-pyrrolo[3,4-d]pyri

K. Gajiwala, M. Hickey, P. Kung, 2011, Journal of medicinal chemistry.

Comparison of a High-Throughput Mass Spectrometry Method and Radioactive Filter Binding to Assay the Protein Methyltransferase PRMT5.

A. Brooun, K. Maegley, P. Bingham, 2015, Assay and drug development technologies.

Discovery of 2-((1H-benzo[d]imidazol-1-yl)methyl)-4H-pyrido[1,2-a]pyrimidin-4-ones as novel PKM2 activators.

M. Hickey, M. Pairish, S. Greasley, 2013, Bioorganic & medicinal chemistry letters.

Discovery of a highly potent, selective, orally bioavailable inhibitor of KAT6A/B histone acetyltransferases with efficacy against KAT6A-high ER+ breast cancer.

Chin Wee Tan, Dharmesh D. Bhuva, Eric C Greenwald, 2023, Cell chemical biology.

Abstract 4863: PF-06840003: a highly selective IDO-1 inhibitor that shows good in vivo efficacy in combination with immune checkpoint inhibitors

Paolo Vicini, Deepak Dalvie, Chad Ray, 2016 .

31st Annual Meeting and Associated Programs of the Society for Immunotherapy of Cancer (SITC 2016): part two

Charles J. Vaske, Joe Y. Chang, Scott R. Presnell, 2016, Journal for ImmunoTherapy of Cancer.

Characterization of Specific N-α-Acetyltransferase 50 (Naa50) Inhibitors Identified Using a DNA Encoded Library.

W. K. Sonnenburg, P. Kung, M. Gehring, 2020, ACS medicinal chemistry letters.