Zobrazeno 1 - 10
of 27
pro vyhledávání: '"Jamal Carlos Saeh"'
Autor:
Jamal Carlos Saeh, Justin Cidado, Lisa Drew, Stephen Fawell, Michelle Min Wu, Neeraj Kumar Aryal, Gareth P. Gregory, Maureen Hattersley, Wenlin Shao, Theresa Proia, Maryann San Martin, Ricky W. Johnstone, Scott Boiko
Publikováno v:
Blood
BH3 mimetics like venetoclax target prosurvival Bcl-2 family proteins and are important therapeutics in the treatment of hematological malignancies. We demonstrate that endogenous Bfl-1 expression can render preclinical lymphoma tumor models insensit
Autor:
Shenghua Wen, Srividya B. Balachander, Francis D. Gibbons, Michael Zinda, William McCoull, Nancy Su, Barry R. Davies, Stephen E. Kurtz, Terry MacIntyre, Edward J. Hennessy, Martin Wild, Paula Lewis, Ricky W. Johnstone, Jamal Carlos Saeh, Kathleen A. Burke, Omid Tavana, Andrea Newbold, Elizabeth A. Coker, Alwin Schuller, Justin Cidado, Diebold R Bruce, Tristan J. Lubinski, Steven Criscione, J. Paul Secrist, Kate Byth, Gareth P. Gregory, Deborah Lawson, Ammar Adam, Shannon K. McWeeney, Stephen Fawell, Thomas Gero, Jeffrey G. Varnes, Eric Gangl, Patricia Jaaks, Jeffrey W. Tyner, Mathew J. Garnett, Areya Tabatabai, Stephanos Ioannidis
Publikováno v:
Clinical Cancer Research. 26:6535-6549
Purpose: Targeting Bcl-2 family members upregulated in multiple cancers has emerged as an important area of cancer therapeutics. While venetoclax, a Bcl-2–selective inhibitor, has had success in the clinic, another family member, Bcl-xL, has also e
Publikováno v:
Cancer Research. 79:P4-13
Estrogen receptor α-positive (ER+) breast cancer is routinely treated with therapies targeting the ER axis. However, de novo and acquired resistance to the standard-of-care treatment occur in a significant subset of patients. Multiple mechanisms hav
Autor:
Ammar Adam, David J. Owen, Justin Cidado, Claire Patterson, Matthew Skinner, Stuart Purbrick, Lorraine Graham, Petar Pop-Damkov, Michael Giannis, Srividya B. Balachander, Francis D. Gibbons, William McCoull, Marianne Ashford, Hill Kathryn Jane, Martin Wild, Eric Gangl, Stephen Fawell, Corinne Reimer, Sean Redmond, Paul D. Kemmitt, Barry R. Davies, Jamal Carlos Saeh, Shenghua Wen, J. Paul Secrist, Alwin Schuller, Edward J. Hennessy, Sonya Gales, Iain Grant, Alexander R. Harmer, Jeremy S. Parker, Brian Kelly
Publikováno v:
Communications Biology
Communications Biology, Vol 4, Iss 1, Pp 1-14 (2021)
Communications Biology, Vol 4, Iss 1, Pp 1-14 (2021)
Dual Bcl-2/Bcl-xL inhibitors are expected to deliver therapeutic benefit in many haematological and solid malignancies, however, their use is limited by tolerability issues. AZD4320, a potent dual Bcl-2/Bcl-xL inhibitor, has shown good efficacy howev
Autor:
Chandra Sekhar Reddy Chilamakuri, Clive D'Santos, Stephen Fawell, Michael Zinda, David M. Weinstock, Nancy Su, Valar Nila Roamio Franklin, Petar Pop-Damkov, Jamal Carlos Saeh, Raphael Koch, Wenlin Shao, Steven Criscione, Justin Cidado, Scott Boiko, Lisa Drew, Maryann San Martin, Theresa Proia, Douglas Ferguson
Publikováno v:
Clinical cancer research : an official journal of the American Association for Cancer Research. 26(4)
Purpose: Cyclin-dependent kinase 9 (CDK9) is a transcriptional regulator and potential therapeutic target for many cancers. Multiple nonselective CDK9 inhibitors have progressed clinically but were limited by a narrow therapeutic window. This work de
Autor:
Amanda L. Christie, Courtney L. Andersen, Alan Rosen, Kim Maratea, Edwin Clark, Maureen Hattersley, Corinne Reimer, Jerome T. Mettetal, Sai Pulukuri, Jon Travers, Jamal Carlos Saeh, Justin Cidado
Publikováno v:
Blood. 134:1273-1273
Acute myeloid leukemia (AML) is an aggressive, heterogeneous malignancy. AML patients whose disease relapses on chemotherapy or are unfit for aggressive induction regimens have limited therapeutic options. Many patients benefit from the combination o
Autor:
Jamal Carlos Saeh, Vibha Oza, Kate Byth, Michael T. Rooney, Lucienne Ronco, Paul Lyne, Danyang Li, Qibin Su, Gurmit Grewal, Victor Kamhi, Edward J. Hennessy
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:2041-2045
We have discovered a novel class of heterocyclic sulfonamides that act as antagonists of the S1P1 receptor. While members of this series identified from a high-throughput screen showed promising levels of potency in a cell-based assay measuring the i
Autor:
Suqin He, Jeffrey L. Brown, Gary Hattersley, Ziyang Yu, Hitisha K. Patel, Dannie Wang, Jamal Carlos Saeh, Chris Miller
Publikováno v:
Clinical cancer research : an official journal of the American Association for Cancer Research. 23(24)
Purpose: Steroidal androgens suppress androgen receptor and estrogen receptor positive (AR/ER+) breast cancer cells and were used to treat breast cancer, eliciting favorable response. The current study evaluates the activity and efficacy of the oral
Autor:
Kate Byth, Daniel John Russell, Jamal Carlos Saeh, Terry MacIntyre, Stephanos Ioannidis, Thomas Gero, Diebold R Bruce, Galina Repik, Paul T. Grover, Ogoe Claude Afona, Mei Su, Jeffrey G. Varnes, Prasenjit Mukherjee, Shan Huang, Keith Dillman
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:3026-3033
Structural modifications of the left-hand side of compound 1 were identified which retained or improved potent binding to Bcl-2 and Bcl-xL in in vitro biochemical assays and had strong activity in an RS4;11 apoptotic cellular assay. For example, sulf
Autor:
Terry MacIntyre, Brian Aquila, Edward J. Hennessy, Naomi Laing, Vibha Oza, David Whitston, Victor Kamhi, Jamal Carlos Saeh, Lillian Castriotta, Li Sha, Troy Patterson, Christopher Huntington, Danyang Li, Haiyun Wang, Charles A. Omer, Alexander Hird, Melissa Vasbinder, Donald J. Cook, Michael T. Rooney, Galina Repik, Maureen Hattersley, Ammar Adam
Publikováno v:
Journal of Medicinal Chemistry. 56:9897-9919
A series of dimeric compounds based on the AVPI motif of Smac were designed and prepared as antagonists of the inhibitor of apoptosis proteins (IAPs). Optimization of cellular potency, physical properties, and pharmacokinetic parameters led to the id