Zobrazeno 1 - 10
of 39
pro vyhledávání: '"Yingqing Ran"'
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:
Zhiyu Huang, Yingqing Ran, Le An, Alberto Gobbi, Jonathan Maher, Claire Emson, Naomi S. Rajapaksa, Edna F. Choo, Yongsheng Chen, Steven Do, Aleksandr Kolesnikov, Ali A. Zarrin, Christine Yu, Marian C. Bryan, Joy Drobnick, Swathi Sujatha-Bhaskar, Hans Brightbill, James R. Kiefer, Jun Liang, Brent S. McKenzie, Ross Francis, John S. Wai, Patrick J. Lupardus, Kevin DeMent
Publikováno v:
ACS Med Chem Lett
[Image: see text] IRAK4 kinase activity transduces signaling from multiple IL-1Rs and TLRs to regulate cytokines and chemokines implicated in inflammatory diseases. As such, there is high interest in identifying selective IRAK4 inhibitors for the tre
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3c741d6c5a8d5445e4411ce0bee8e8c5
https://europepmc.org/articles/PMC7073891/
https://europepmc.org/articles/PMC7073891/
Publikováno v:
Journal of Pharmaceutical Sciences. 107:327-333
The oral bioavailability of a drug candidate is influenced by its permeability, metabolism, and physicochemical properties. Among the physicochemical properties, solubility and dissolution rate often are the most critical factors affecting the oral b
Autor:
Le An, Jonathan Maher, Yingqing Ran, Ryan E. Morgan, Lisa Wong, Laurent Salphati, Leah Schutt, Xiaolin Zhang, David Potter, Steven Cepa, Jacqueline M. Tarrant, Jodie Pang, Roxanne Andaya
Publikováno v:
Toxicology and Applied Pharmacology. 338:204-213
Drug-induced liver injury (DILI) has been the most frequent cause of post-marketing drug withdrawals in the last 50years. The multifactorial nature of events that precede severe liver injury in human patients is difficult to model in rodents due to a
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:
Yichin Liu, Peter S. Dragovich, Daniel F. Ortwine, Birong Zhang, Richard D. Cummings, Jun Liang, Yingqing Ran, Marie Classon, Sharada Labadie, Tommy Lai, Weifeng Mao, Victor S. Gehling, Bianca M. Liederer, Erica Van der Porten, Jean-Christophe Harmange, Till Mauer, Le An, Xiaoping Zheng, Jiangpeng Liao, James R. Kiefer, Maia Vinogradova, Snahel Patel, Patrick Trojer, Gauri Deshmukh, Amy Gustafson, Lesley J. Murray
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 27:2974-2981
A high-throughput screening (HTS) of the Genentech/Roche library identified a novel, uncharged scaffold as a KDM5A inhibitor. Lacking insight into the binding mode, initial attempts to improve inhibitor potency failed to improve potency, and synthesi
Autor:
Patrick J. Lupardus, Yongsheng Chen, Naomi S. Rajapaksa, John S. Wai, Kevin DeMent, Edna F. Choo, Brent S. McKenzie, Ross Francis, Joy Drobnick, Hans Brightbill, James R. Kiefer, Willy M. Chang, Chudi Ndubaku, Alberto Gobbi, Antonio G. DiPasquale, Aleksandr Kolesnikov, Jonathan Maher, Jianwen Feng, Claire Emson, Le An, Ali A. Zarrin, Zhiyu Huang, Christine Yu, Yingqing Ran, Marian C. Bryan, Swathi Sujatha-Bhaskar
Publikováno v:
Journal of medicinal chemistry. 62(13)
A series of pyrazolopyrimidine inhibitors of IRAK4 were developed from a high-throughput screen (HTS). Modification of an HTS hit led to a series of bicyclic heterocycles with improved potency and kinase selectivity but lacking sufficient solubility
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:
Jane L. Grogan, Ruina Li, Edna F. Choo, Sarah M. Bronner, Maureen Beresini, Jonathan Maher, Patrick Cyr, Yingjie Li, Thomas Hunsaker, Brian K. Albrecht, Colin Masui, Kevin R Clark, Yingqing Ran, Jeremy Murray, Terry Crawford, Xiaorong Liang, Fei Wang, F. Anthony Romero, Xiaocang Wei, Alexander M. Taylor, Georgia Hatzivassiliou, Kyle Clagg, Kwong Wah Lai, Karen E. Gascoigne, Le An, Steven Magnuson, Mark Merchant, John S. Wai, Zhongguo Chen, Jiangpeng Liao, Vickie Tsui, Emily Chan, Kevin X. Chen, Wenfeng Liu, Wei Huang, Dong Yu, Stefan G. Koenig, Susan Kaufman, Xiaoyu Zhu, Gladys de Leon Boenig, Justin Ly, Denise E. de Almeida Nagata, Bing-Yan Zhu
Publikováno v:
Journal of medicinal chemistry. 60(22)
Inhibition of the bromodomain of the transcriptional regulator CBP/P300 is an especially interesting new therapeutic approach in oncology. We recently disclosed in vivo chemical tool 1 (GNE-272) for the bromodomain of CBP that was moderately potent a