Zobrazeno 1 - 10
of 20
pro vyhledávání: '"Steven J. Hartman"'
Autor:
Ishita Mostafa, Matthew C. Hibberd, Steven J. Hartman, Md Hasan Hafizur Rahman, Mustafa Mahfuz, S.M. Tafsir Hasan, Per Ashorn, Michael J. Barratt, Tahmeed Ahmed, Jeffrey I. Gordon
Publikováno v:
EBioMedicine, Vol 104, Iss , Pp 105166- (2024)
Summary: Background: Globally, stunting affects ∼150 million children under five, while wasting affects nearly 50 million. Current interventions have had limited effectiveness in ameliorating long-term sequelae of undernutrition including stunting,
Externí odkaz:
https://doaj.org/article/949c0bae794e4d999df60dc817a0cab5
Autor:
Peter S. Dragovich, Mingtao He, Leanna Staben, Hongyan Zhang, Melinda M. Mulvihill, Catherine Wilson, Hao Zhou, Tracy Kleinheinz, Binqing Wei, Jianfeng Xin, Nicole Blaquiere, Fanwei Meng, John S. Wai, Susan Kaufman, Liang Liu, Rebecca K. Rowntree, Steven T. Staben, Jing Wang, Katherine R. Kozak, Josefa dela Cruz-Chuh, Zijin Xu, Steven J. Hartman, Robert A. Blake, Xiaoyu Zhu, Sunil Bhakta, Donglu Zhang, Hui Yao, Aimee O'Donohue, Jack Sadowsky, Qi Liu, Pragya Adhikari, Liling Liu, Ying Lu, Thomas H. Pillow, Jinhua Chen, Emel Adaligil, Karen E. Gascoigne
Publikováno v:
Journal of Medicinal Chemistry. 64:2534-2575
The biological and medicinal impacts of proteolysis-targeting chimeras (PROTACs) and related chimeric molecules that effect intracellular degradation of target proteins via ubiquitin ligase-mediated ubiquitination continue to grow. However, these chi
Autor:
Kuen Yeap, John S. Wai, Maia Vinogradova, Yu Zhong, Lori Friedman, Xiaojing Wang, Daniel Otwine, Jiangpeng Liao, Nick Ray, James R. Kiefer, Vidhi Mody, Jun Li, Fabien Roussel, Deepak Sampath, Simon Charles Goodacre, Jun Liang, Michelle Nannini, Sharada Labadie, Xiaoping Zheng, Ellen Ingalla, Steven J. Hartman, Birong Zhang, Jae H. Chang, Tao Wang, Yingqing Ran, Jason R. Zbieg, Amy Sambrone, Kwong Wah Lai, Amy Young, Ciara Metcalfe, Neville James Mclean, Robert A. Blake, Tracy Kleinheinz
Publikováno v:
ACS Med Chem Lett
[Image: see text] Estrogen receptor alpha (ERα) is a well-validated drug target for ER-positive (ER+) breast cancer. Fulvestrant is FDA-approved to treat ER+ breast cancer and works through two mechanisms—as a full antagonist and selective estroge
Autor:
Martin O'Rourke, Nicholas Charles Ray, Thomas Gelzleichter, Leah Schutt, Ellen Ingalla, Neville James Mclean, Xiaojing Wang, Stephen Daly, Yingqing Ran, Jiangpeng Liao, Tommy Lai, Yu Zhong, Jun Liang, Sharada Labadie, Lori Friedman, Amy Sambrone, Jun Li, Robert A. Blake, Tao Wang, Liu Zhiguo, Birong Zhang, Steven J. Hartman, Jae H. Chang, Wei Zhou, Jane Guan, Vidhi Mody, Jonathan White, Fabien Roussel, Antonio G. DiPasquale, Jason R. Zbieg, Daniel F. Ortwine, Amy Young, James R. Kiefer, Maia Vinogradova, Simon Charles Goodacre, Deepak Sampath, Tracy Kleinheinz, Xiaoping Zheng, Jennifer M. Giltnane, Lorn Kategaya, Ingrid E. Wertz, Matthew Gill, Ciara Metcalfe, Siew Kuen Yeap, John S. Wai, Jason Oeh, Michelle Nannini
Publikováno v:
Journal of medicinal chemistry. 64(16)
Breast cancer remains a leading cause of cancer death in women, representing a significant unmet medical need. Here, we disclose our discovery efforts culminating in a clinical candidate, 35 (GDC-9545 or giredestrant). 35 is an efficient and potent s
Autor:
Steven J. Hartman, Ying Lu, Wentao Wei, Hao Zhou, Geoffrey Del Rosario, Robert A. Blake, Xiaoyu Zhu, Nicholas Corr, Aaron Fullerton, Shang-Fan Yu, Peter S. Dragovich, Jing Wang, Rebecca K. Rowntree, Donglu Zhang, Hui Yao, Emel Adaligil, Fan Jiang, Hongyan Zhang, Jack Sadowsky, John S. Wai, Jinhua Chen, Thomas H. Pillow, Susan Kaufman, Zijin Xu, Katherine R. Kozak, Jeremy Murray, Shenhua Zhang, Leanna Staben, Josefa dela Cruz-Chuh, Pragya Adhikari, Aimee O'Donohue, Tracy Kleinheinz, Liling Liu, Melinda M. Mulvihill, William S. Sawyer, Yongxin Zhao, Binqing Wei
Publikováno v:
Journal of medicinal chemistry. 64(5)
Heterobifunctional compounds that direct the ubiquitination of intracellular proteins in a targeted manner via co-opted ubiquitin ligases have enormous potential to transform the field of medicinal chemistry. These chimeric molecules, often termed pr
Autor:
Kuen Yeap, Birong Zhang, Jae H. Chang, Lori Friedman, Nick Ray, Jiangpeng Liao, Xiaojing Wang, Amy Sambrone, Jun Li, Yu Zhong, Ellen Ingalla, Jason R. Zbieg, Daniel F. Ortwine, Vidhi Mody, John S. Wai, Tao Wang, Maia Vinogradova, Sharada Labadie, Steven J. Hartman, Tracy Kleinheinz, Nev McLean, Tommy Lai, Simon Charles Goodacre, Deepak Sampath, Jun Liang, Fabien Roussel, James R. Kiefer, Ciara Metcalfe, Xiaoping Zheng, Yingqing Ran, Michelle Nannini, Robert A. Blake
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 50:128335
Fulvestrant is an FDA-approved drug with a dual mechanism of action (MOA), acting as a full antagonist and degrader of the estrogen receptor protein. A significant limitation of fulvestrant is the dosing regimen required for efficacy. Due to its high
Autor:
Mingtao He, Chun Sing Li, Yongxin Zhao, Deepak Sampath, Leanna Staben, Ingrid E. Wertz, Hao Zhou, Rebecca K. Rowntree, Ellen Ingalla, Xinxin Wang, Richard Zang, Ying Lu, Qi Liu, Jiawei Lu, Gail Lewis Phillips, Binqing Wei, Fanwei Meng, Nicole Blaquiere, Yun-Xing Cheng, Steven T. Staben, Keyang Xu, Jinping Han, Tommy Lai, Kaishan Peng, Kunpeng Wan, Peter S. Dragovich, Lingyao Meng, Tracy Kleinheinz, Jinhua Chen, Amrita V. Kamath, John S. Wai, Carl Ng, Pragya Adhikari, Steven J. Hartman, Jianfeng Xin, Jintang He, Douglas D. Leipold, Thomas H. Pillow, Donglu Zhang, Hui Yao, Jack Sadowsky, Robert A. Blake, Willem den Besten
Publikováno v:
Bioorganicmedicinal chemistry letters. 30(4)
Chimeric molecules which effect intracellular degradation of target proteins via E3 ligase-mediated ubiquitination (e.g., PROTACs) are currently of high interest in medicinal chemistry. However, these entities are relatively large compounds that ofte
Autor:
Sharada S. Labadie, Jun Li, Robert A. Blake, Jae H. Chang, Simon Goodacre, Steven J. Hartman, Weiling Liang, James R. Kiefer, Tracy Kleinheinz, Tommy Lai, Jiangpeng Liao, Daniel F. Ortwine, Vidhi Mody, Nicholas C. Ray, Fabien Roussel, Maia Vinogradova, Siew Kuen Yeap, Birong Zhang, Xiaoping Zheng, Jason R. Zbieg, Jun Liang, Xiaojing Wang
Publikováno v:
Bioorganicmedicinal chemistry letters. 29(16)
Phenolic groups are responsible for the high clearance and low oral bioavailability of the estrogen receptor alpha (ERα) clinical candidate GDC-0927. An exhaustive search for a backup molecule with improved pharmacokinetic (PK) properties identified
Autor:
Tommy Lai, Maia Vinogradova, Jun Liang, Yu Zhong, Birong Zhang, Jae H. Chang, Xiaojing Wang, Yingqing Ran, Hai Chen, Deepak Sampath, Robert A. Blake, Ellen Ingalla, Jerome C. Nwachukwu, James R. Kiefer, Daniel F. Ortwine, Jiangpeng Liao, Tracy Kleinheinz, Amy Sambrone, Xiaoping Zheng, Kendall W. Nettles, Steven J. Hartman, Vidhi Mody, Michelle Nannini
Publikováno v:
Bioorganicmedicinal chemistry letters. 29(7)
Despite tremendous progress made in the understanding of the ERα signaling pathway and the approval of many therapeutic agents, ER+ breast cancer continues to be a leading cause of cancer death in women. We set out to discover compounds with a dual
Autor:
Peter S. Dragovich, Keyang Xu, John S. Wai, Jason Oeh, Willem den Besten, Yong Ma, Richard Vandlen, Ellen Ingalla, Fang Fan, Ingrid E. Wertz, Chunjiao Chen, Steven R. Leong, Deepak Sampath, Jiawei Lu, Donglu Zhang, Katherine R. Kozak, Thomas H. Pillow, Steven J. Hartman, Breanna S. Vollmar, Changrong He, Zijin Xu, Robert A. Blake, Gail Lewis Phillips, Josefa Chuh, Rebecca K. Rowntree, Jinhua Chen, Michelle Nannini, Rachana Ohri, Jintang He, Aimee Fourie, Lingyao Meng
Publikováno v:
Chemistry (Weinheim an der Bergstrasse, Germany). 24(19)
A novel strategy to attach indole-containing payloads to antibodies through a carbamate moiety and a self-immolating, disulfide-based linker is described. This new strategy was employed to connect a selective estrogen receptor down-regulator (SERD) t