Paul E. Erdman
Celgene
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Publication
Featured researches published by Paul E. Erdman.
Bioorganic & Medicinal Chemistry Letters | 2002
Moorthy S.S. Palanki; Leah M. Gayo-Fung; Graziella I. Shevlin; Paul E. Erdman; Mark Sato; Mark Goldman; Lynn J. Ransone; Cheryl Spooner
Several analogues of ethyl 2-[(3-methyl-2,5-dioxo(3-pyrrolinyl))amino]-4-(trifluoromethyl)pyrimidine-5-carboxylate (1) were synthesized and tested as inhibitors of AP-1 and NF-κB mediated transcriptional activation in Jurkat T cells. From our SAR work, ethyl 2-[(3-methyl-2,5-dioxo(3-pyrrolinyl))-N-methylamino]-4-(trifluoromethyl)-pyrimidine-5-carboxylate was identified as a novel and potent inhibitor.
Bioorganic & Medicinal Chemistry Letters | 2012
Garrick Packard; Patrick Papa; Jennifer Riggs; Paul E. Erdman; Lida Tehrani; Dale Robinson; Roy Harris; Graziella I. Shevlin; Sophie Perrin-Ninkovic; Robert Hilgraf; Margaret A. McCarrick; Tam Tran; Yuedi W. Fleming; April Bai; Samantha J. Richardson; Jason Katz; Yang Tang; Jim Leisten; Mehran F. Moghaddam; Brian E. Cathers; Dan Zhu; Steven T. Sakata
The serine/threonine specific protein kinase B-Raf is part of the MAPK pathway and is an interesting oncology target. We have identified thieno[2,3-d]pyrimidines as a core scaffold of small molecule B-Raf inhibitors. The SAR of analogs in this series will be described.
Journal of Medicinal Chemistry | 2017
Jennifer Riggs; Mark A. Nagy; Jan Elsner; Paul E. Erdman; Dan Cashion; Dale Robinson; Roy Harris; Dehua Huang; Lida Tehrani; Gordafaried Deyanat-Yazdi; Rama Krishna Narla; Xiaohui Peng; Tam Tran; Leo Barnes; Terra Miller; Jason Katz; Yang Tang; Ming Chen; Mehran F. Moghaddam; Sogole Bahmanyar; Barbra Pagarigan; Silvia L Delker; Laurie LeBrun; Philip Chamberlain; Andrew Antony Calabrese; Stacie S. Canan; Katerina Leftheris; Dan Zhu; John Boylan
Triple negative breast cancer (TNBC) remains a serious unmet medical need with discouragingly high relapse rates. We report here the synthesis and structure-activity relationship (SAR) of a novel series of 2,4,5-trisubstituted-7H-pyrrolo[2,3-d]pyrimidines with potent activity against TNBC tumor cell lines. These compounds were discovered from a TNBC phenotypic screen and possess a unique dual inhibition profile targeting TTK (mitotic exit) and CLK2 (mRNA splicing). Design and optimization, driven with a TNBC tumor cell assay, identified potent and selective compounds with favorable in vitro and in vivo activity profiles and good iv PK properties. This cell-based driven SAR produced compounds with strong single agent in vivo efficacy in multiple TNBC xenograft models without significant body weight loss. These data supported the nomination of CC-671 into IND-enabling studies as a single agent TNBC therapy.
Cell | 2018
Waleed Minzel; Avanthika Venkatachalam; Avner Fink; Eric Hung; Guy Brachya; Ido Burstain; Maya Shaham; Amitai Rivlin; Itay Omer; Adar Zinger; Shlomo Elias; Eitan Winter; Paul E. Erdman; Robert Sullivan; Leah Fung; Frank Mercurio; Dansu Li; Joseph Vacca; Nathali Kaushansky; Liran I. Shlush; Moshe Oren; Ross L. Levine; Eli Pikarsky; Irit Snir-Alkalay; Yinon Ben-Neriah
CKIα ablation induces p53 activation, and CKIα degradation underlies the therapeutic effect of lenalidomide in a pre-leukemia syndrome. Here we describe the development of CKIα inhibitors, which co-target the transcriptional kinases CDK7 and CDK9, thereby augmenting CKIα-induced p53 activation and its anti-leukemic activity. Oncogene-driving super-enhancers (SEs) are highly sensitive to CDK7/9 inhibition. We identified multiple newly gained SEs in primary mouse acute myeloid leukemia (AML) cells and demonstrate that the inhibitors abolish many SEs and preferentially suppress the transcription elongation of SE-driven oncogenes. We show that blocking CKIα together with CDK7 and/or CDK9 synergistically stabilize p53, deprive leukemia cells of survival and proliferation-maintaining SE-driven oncogenes, and induce apoptosis. Leukemia progenitors are selectively eliminated by the inhibitors, explaining their therapeutic efficacy with preserved hematopoiesis and leukemia cure potential; they eradicate leukemia in MLL-AF9 and Tet2-/-;Flt3ITD AML mouse models and in several patient-derived AML xenograft models, supporting their potential efficacy in curing human leukemia.
Archive | 2001
Adam Kois; Karen J Macfarlane; Yoshitaka Satoh; Shripad S. Bhagwat; Jason S. Parnes; Moorthy S. S. Palanki; Paul E. Erdman
Archive | 2009
Sogole Bahmanyar; R.J. Bates; Kate Blease; Andrew Antony Calabrese; Thomas Oran Daniel; Mercedes Delgado; Jan Elsner; Paul E. Erdman; Bruce Fahr; Gregory D. Ferguson; Branden Lee; Lisa Nadolny; Garrick Packard; Patrick Papa; Veronique Plantevin-Krenitsky; Jennifer Riggs; Patricia Rohane; Sabita Sankar; John Sapienza; Yoshitaka Satoh; Victor S. Sloan; Randall Stevens; Lida Tehrani; Jayashree Tikhe; Eduardo Torres; Andrew Wallace; Brandon Wade Whitefield; Jingjing Zhao
Journal of Medicinal Chemistry | 2000
Moorthy S. S. Palanki; Paul E. Erdman; Leah M. Gayo-Fung; Graziella I. Shevlin; Robert Sullivan; Mark E. Goldman; Lynn J. Ransone; Brydon L. Bennett; Anthony M. Manning; Mark J. Suto
Journal of Medicinal Chemistry | 1998
Robert Sullivan; Colin G. Bigam; Paul E. Erdman; Moorthy S. S. Palanki; David W. Anderson; Mark E. Goldman; Lynn J. Ransone; Mark J. Suto
Bioorganic & Medicinal Chemistry Letters | 2003
Moorthy S.S. Palanki; Paul E. Erdman; Minghuan Ren; Mark J. Suto; Brydon L. Bennett; Anthony M. Manning; Lynn J. Ransone; Cheryl Spooner; Sonal Desai; Arnie Ow; Ryuichi Totsuka; Peter W. Tsao; Wataru Toriumi
Bioorganic & Medicinal Chemistry Letters | 2000
Moorthy S. S. Palanki; Paul E. Erdman; Anthony M. Manning; Arnold Ow; Lynn J. Ransone; Cheryl Spooner; Carla Suto; Mark J. Suto