Susan Kaufman

发表

Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637).

Y. Leblanc, H. Jayaram, R. Sims, 2016, ACS medicinal chemistry letters.

Imidazo[1,2-a]pyridin-6-yl-benzamide analogs as potent RAF inhibitors.

K. Shoemaker, Z. Ni, S. Cowan-Jacob, 2017, Bioorganic & medicinal chemistry letters.

Activation of the IRE1 RNase through remodeling of the kinase front pocket by ATP-competitive ligands

Peter S Liu, A. Ashkenazi, E. Day, 2020, Nature Communications.

A Unique Approach to Design Potent and Selective Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP) Inhibitors.

Fei Wang, H. Jayaram, F. A. Romero, 2017, Journal of medicinal chemistry.

Antibody Conjugation of a Chimeric BET Degrader Enables in vivo Activity

Melinda M. Mulvihill, Karen E Gascoigne, R. Rowntree, 2020, ChemMedChem.

Discovery of 2-pyrimidyl-5-amidothiophenes as potent inhibitors for AKT: synthesis and SAR studies.

E. Fang, Sylvia Ma, J. Murray, 2006, Bioorganic & medicinal chemistry letters.

Design and synthesis of a biaryl series as inhibitors for the bromodomains of CBP/P300.

Fei Wang, F. A. Romero, E. Choo, 2018, Bioorganic & medicinal chemistry letters.

Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300.

Karen E Gascoigne, Fei Wang, S. Kharbanda, 2016, Journal of medicinal chemistry.

Abstract 3790: Preclinical profile of LGX818: A potent and selective RAF kinase inhibitor

G. Caponigro, Nanxin Li, Edward G. Lorenzana, 2012 .

Identification of NVP-BKM120 as a Potent, Selective, Orally Bioavailable Class I PI3 Kinase Inhibitor for Treating Cancer.

Simon Ng, Yanchen Zhang, Kenneth Crawford, 2011, ACS medicinal chemistry letters.

Structural resemblances and comparisons of the relative pharmacological properties of imatinib and nilotinib.

Nikolaus Stiefl, J. Mestan, N. Stiefl, 2010, Bioorganic & medicinal chemistry.

Identification and structure-activity relationship of 2-morpholino 6-(3-hydroxyphenyl) pyrimidines, a class of potent and selective PI3 kinase inhibitors.

K. Shoemaker, M. Wiesmann, W. Fantl, 2010, Bioorganic & medicinal chemistry letters.

Single-cell dissection of cellular components and interactions shaping the tumor immune phenotypes in ovarian cancer.

R. Bourgon, Yulei N. Wang, A. Daemen, 2021, Cancer cell.

Discovery of imidazo[1,2-a]-pyridine inhibitors of pan-PI3 kinases that are efficacious in a mouse xenograft model.

Yongjin Xu, Z. Ni, C. Voliva, 2016, Bioorganic & medicinal chemistry letters.

Therapeutic Targeting of the CBP/p300 Bromodomain Blocks the Growth of Castration-Resistant Prostate Cancer.

Karen E Gascoigne, Z. Modrušan, S. Kharbanda, 2017, Cancer research.

Disruption of IRE1α through its kinase domain attenuates multiple myeloma

M. Amiot, D. Lawrence, P. Walter, 2018, Proceedings of the National Academy of Sciences.

Structure guided optimization of a fragment hit to imidazopyridine inhibitors of PI3K.

Z. Ni, M. Wiesmann, C. Voliva, 2013, Bioorganic & medicinal chemistry letters.

GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP).

Karen E Gascoigne, Y. Ran, G. Hatzivassiliou, 2017, Journal of medicinal chemistry.

Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 1: Exploration of Antibody Linker, Payload Loading, and Payload Molecular Properties.

Melinda M. Mulvihill, Karen E Gascoigne, R. Rowntree, 2021, Journal of medicinal chemistry.

Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 2: Improvement of In Vitro Antiproliferation Activity and In Vivo Antitumor Efficacy.

Melinda M. Mulvihill, R. Rowntree, Wentao Wei, 2021, Journal of medicinal chemistry.

Identification of BRaf-Sparing Amino-Thienopyrimidines with Potent IRE1α Inhibitory Activity.

S. Srivastava, C. Ly, A. Ashkenazi, 2020, ACS medicinal chemistry letters.