Zobrazeno 1 - 10
of 16
pro vyhledávání: '"Dashyant Dhanak"'
Publikováno v:
Cell chemical biology. 24(9)
Advances in understanding the role and molecular mechanisms underlying immune surveillance and control of (pre)malignancies is revolutionizing clinical practice in the treatment of cancer. Presently, multiple biologic drugs targeting the immune check
Autor:
Martin Brandt, Caretha L. Creasy, Elsie Diaz, Benjamin Schwartz, Peter J. Tummino, Melissa B. Pappalardi, William H. Miller, Glenn S. Van Aller, Ryan G. Kruger, Sharad K. Verma, Heidi M. Ott, Dashyant Dhanak, Michael T. McCabe
Publikováno v:
ACS Chemical Biology. 9:622-629
EZH2/PRC2 catalyzes transcriptionally repressive methylation at lysine 27 of histone H3 and has been associated with numerous cancer types. Point mutations in EZH2 at Tyr641 and Ala677 identified in non-Hodgkin lymphomas alter substrate specificity a
Autor:
Octerloney B. McDonald, Carla A. Donatelli, William F. Huffman, Toshihiro Hamajima, Christine Thompson, Kelly E. Fisher, Martha A. Sarpong, Jamin C Wang, David Sutton, Dashyant Dhanak, Peter J. Tummino, Jun Tang, Ken A. Newlander, Zhihong V Lai, Hong Xiang, Kosuke Sasaki, Domingos J. Silva, Mary Ann Hardwicke, Jerry L. Adams, Cynthia A. Parrish, Schmidt Stanley J, Denis R. Patrick, Hiroko Nakamura, Jingsong Yang, Catherine A. Oleykowski, Robert A. Copeland, Amita M. Chaudhari, Ramona Plant, David H. Drewry, Kristin K Koretke-Brown, Nicholas D. Adams, Joelle Lorraine Burgess
Publikováno v:
Journal of Medicinal Chemistry. 53:3973-4001
The Aurora kinases play critical roles in the regulation of mitosis and are frequently overexpressed or amplified in human tumors. Selective inhibitors may provide a new therapy for the treatment of tumors with Aurora kinase amplification. Herein we
Autor:
Nannan Liu, Michael N. Zimmerman, Richard M. Keenan, Victor K. Johnston, Deping Chai, Rosanna Tedesco, Duke M. Fitch, Juili Lin-Goerke, Kenneth Wiggall, Antony N. Shaw, Nestor O. Concha, Ramesh Bambal, Michael G. Darcy, Robert T. Sarisky, Dashyant Dhanak, Kevin J. Duffy, Adam T. Gates
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:4350-4353
The synthesis and optimisation of HCV NS5B polymerase inhibitors with improved potency versus the existing compound 1 is described. Substitution in the benzothiadiazine portion of the molecule, furnishing improvement in potency in the high protein Re
Autor:
Steven D. Knight, Richard M. Keenan, James J. Foley, Diane Naselsky, Ralph A. Rivero, Kevin L. Salyers, Stephen A. Douglas, Anthony Sapienza, Nambi Aiyar, Ming An, Jian Jin, Dashyant Dhanak, Henry M. Sarau
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:3950-3954
SAR exploration of the central diamine, benzyl, and terminal aminoalkoxy regions of the N-cyclic azaalkyl benzamide series led to the identification of very potent human urotensin-II receptor antagonists such as 1a with a Ki of 4 nM. The synthesis an
Autor:
William F. Huffman, Ken A. Newlander, Amita M. Chaudhari, Shu-Yun Zhang, Michael L. Moore, Jeffrey T. Finer, Kevin J. Duffy, Antony N. Shaw, Melody Diamond, David Sutton, Robert A. Copeland, Michael N. Zimmerman, Chiu-Mei M Sung, Leo F. Faucette, Roman Sakowicz, Jeffrey R. Jackson, Lusong Luo, Kurt R. Auger, Kenneth W. Wood, Jeffrey D. Carson, Carla A. Donatelli, Cynthia A. Parrish, Erin D. Hugger, Steven D. Knight, Lance Ridgers, Nicholas D. Adams, Joelle Lorraine Burgess, Dashyant Dhanak
Publikováno v:
Journal of Medicinal Chemistry. 50:4939-4952
Kinesin spindle protein (KSP), an ATPase responsible for spindle pole separation during mitosis that is present only in proliferating cells, has become a novel and attractive anticancer target with potential for reduced side effects compared to curre
Autor:
Thomas J. Carr, Dashyant Dhanak, David Haigh, George Burton, Victor K. Johnson, Pia Thommes, Glenn A. Hofmann, Robert T. Sarisky, Martin John Slater, Juili Lin-Goerke, Thomas W. Ku, Nigel R. Parry, Terry Kiesow
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:1930-1933
The SAR development is described for a series of N -acyl pyrrolidine inhibitors of the Hepatitis C virus RNA-dependent RNA polymerase, NS5B, from tractable Δ21 enzyme inhibitors to an example with antiviral activity in a cellular assay (HCV replicon
Autor:
Chao Han, Warren W. Gerhardt, Dashyant Dhanak, Kevin J. Duffy, Nestor O. Concha, Adam T. Gates, Richard M. Keenan, Victor K. Johnston, Glenn A. Hofmann, Duke M. Fitch, Nannan Liu, Kenneth Wiggall, Antony N. Shaw, Dina L. Halegoua, Robert T. Sarisky, Michael N. Zimmerman, Ramesh Bambal, Michael G. Darcy, Arun C. Kaura, Juili Lin-Goerke, Deping Chai, Rosanna Tedesco
Publikováno v:
Journal of Medicinal Chemistry. 49:971-983
Recently, we disclosed a new class of HCV polymerase inhibitors discovered through high-throughput screening (HTS) of the GlaxoSmithKline proprietary compound collection. This interesting class of 3-(1,1-dioxo-2H-1,2,4-benzothiadiazin-3-yl)-4-hydroxy
Autor:
Jian Jin, Widdowson Katherine L, Dashyant Dhanak, Dulcie B. Schmidt, Henry M. Sarau, Nambi Aiyar, Richard M. Keenan, Stephen A. Douglas, Carl D. Bennett, Steven D. Knight, James J. Foley, Ralph A. Rivero, Diane Naselsky, Gregory L. Warren, Bing Wang, Michael L. Moore
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:3229-3232
High throughput screening of the corporate compound collection led to the discovery of a novel series of substituted aminoalkoxybenzyl pyrrolidines as human urotensin-II receptor antagonists. The synthesis, initial structure-activity relationships, a
Autor:
Henry M. Sarau, John R. White, Lisa T. Christmann, Dashyant Dhanak, Anthony J. Jurewicz, Widdowson Katherine L, Richard M. Keenan, Judithann M. Lee, Michael G. Darcy
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:1441-1444
The discovery of a series of phenylalanine derived CCR3 antagonists is reported. Parallel, solution-phase library synthesis has been utilized to delineate the structure–activity relationship leading to the synthesis of highly potent, CCR3-selective