P
Paul Hessler
Researcher at AbbVie
Publications - 23
Citations - 1477
Paul Hessler is an academic researcher from AbbVie. The author has contributed to research in topics: Cancer & Bromodomain. The author has an hindex of 12, co-authored 23 publications receiving 1100 citations.
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Journal ArticleDOI
Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours.
Loren M. Lasko,Clarissa G. Jakob,Rohinton Edalji,Wei Qiu,Debra Montgomery,Enrico L. Digiammarino,T. Matt Hansen,Roberto M. Risi,Robin R. Frey,Vlasios Manaves,Bailin Shaw,Mikkel Algire,Paul Hessler,Lloyd T. Lam,Tamar Uziel,Emily J. Faivre,Debra Ferguson,Fritz G. Buchanan,Ruth L. Martin,Maricel Torrent,Gary G. Chiang,Kannan R. Karukurichi,J. William Langston,Brian T. Weinert,Chunaram Choudhary,Peter de Vries,John H. Van Drie,David L. McElligott,Kesicki Edward A,Ronen Marmorstein,Chaohong Sun,Philip A. Cole,Saul H. Rosenberg,Michael R. Michaelides,Albert Lai,Kenneth D. Bromberg +35 more
TL;DR: The results demonstrate the feasibility of using small molecule inhibitors to selectively target the catalytic activity of histone acetyltransferases, which may provide effective treatments for transcriptional activator-driven malignancies and diseases.
Journal ArticleDOI
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,Denise Wilcox,Lu Zhang,Mai H. Bui,George S. Sheppard,Le Wang,Vasudha Sehgal,Xiaoyu Lin,Xiaoli Huang,Xin Lu,Tamar Uziel,Paul Hessler,Lloyd T. Lam,Richard J. Bellin,Gaurav Mehta,Steve D. Fidanze,John K. Pratt,Dachun Liu,Lisa A. Hasvold,Chaohong Sun,Sanjay C. Panchal,John J. Nicolette,Stacey Fossey,Chang H. Park,Kenton L. Longenecker,Lance J Bigelow,Maricel Torrent,Saul H. Rosenberg,Warren M. Kati,Yu Shen +33 more
TL;DR: ABBV-744, a selective inhibitor of the BD2 domains of BET family proteins, is effective against prostate cancer in mouse xenograft models, with lower toxicities than the dual-bromodomain BET inhibitor ABBV -075 and underscores the potential value of selectively targeting theBD2 domain of BETfamily proteins for cancer therapy.
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Protein tyrosine phosphatase 1B negatively regulates leptin signaling in a hypothalamic cell line
Wiweka Kaszubska,H. Douglas Falls,Verlyn G. Schaefer,Deanna L. Haasch,Leigh Frost,Paul Hessler,Paul E. Kroeger,David White,Michael R. Jirousek,James M. Trevillyan +9 more
TL;DR: It is suggested that PTP1B inhibitors might be efficacious in the treatment of obesity by increasing leptin sensitivity and indicating that P TP1B is a negative regulator of leptin signaling.
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Potential mechanisms of resistance to venetoclax and strategies to circumvent it
Stephen K. Tahir,Morey L. Smith,Paul Hessler,Lisa Roberts Rapp,Kenneth B. Idler,Chang H. Park,Joel D. Leverson,Lloyd T. Lam +7 more
TL;DR: This study identified numerous changes in multiple resistant lines; the changes were neither mutually exclusive nor universal across the cell lines tested, thus exemplifying the complexity and heterogeneity of potential resistance mechanisms.
Journal ArticleDOI
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,Xin Lu,Lisa Roberts-Rapp,William N. Pappano,Steven W. Elmore,Andrew J. Souers,Joel D. Leverson,Darren C. Phillips +11 more
TL;DR: It is demonstrated that apoptosis resulting from a loss in MCL-1 function requires expression of the proapoptotic protein BAK, and substantial synergy is demonstrated between navitoclax and Mcl-1 siRNA, the direct M CL-1 inhibitor A-1210477, or the indirect MCL -1 inhibitor flavopiridol, highlighting the therapeutic potential for inhibiting BCL-XL and MCL,1 in breast cancer.