Zobrazeno 1 - 10
of 40
pro vyhledávání: '"Yingqing, Ran"'
Autor:
Ernie Yulyaningsih, Jung H Suh, Melania Fanok, Roni Chau, Hilda Solanoy, Ryan Takahashi, Anna I Bakardjiev, Isabel Becerra, N Butch Benitez, Chi-Lu Chiu, Sonnet S Davis, William E Dowdle, Timothy Earr, Anthony A Estrada, Audrey Gill, Connie Ha, Patrick CG Haddick, Kirk R Henne, Martin Larhammar, Amy W-S Leung, Romeo Maciuca, Bahram Memarzadeh, Hoang N Nguyen, Alicia A Nugent, Maksim Osipov, Yingqing Ran, Kevin Rebadulla, Elysia Roche, Thomas Sandmann, Jing Wang, Joseph W Lewcock, Kimberly Scearce-Levie, Lesley A Kane, Pascal E Sanchez
Publikováno v:
eLife, Vol 12 (2024)
The integrated stress response (ISR) is a conserved pathway in eukaryotic cells that is activated in response to multiple sources of cellular stress. Although acute activation of this pathway restores cellular homeostasis, intense or prolonged ISR ac
Externí odkaz:
https://doaj.org/article/6521500dd1424027bebffc6920eba56b
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fe42f6062f9f361a3f700a527fd2a8dc
https://doi.org/10.1021/acsmedchemlett.0c00224
https://doi.org/10.1021/acsmedchemlett.0c00224
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ee86fe3f8068fbb2ff9647a59eadb710
https://pubmed.ncbi.nlm.nih.gov/34251202
https://pubmed.ncbi.nlm.nih.gov/34251202
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2dfb3be0c2fc847902111285ced5e8d1
https://doi.org/10.1016/j.xphs.2017.09.023
https://doi.org/10.1016/j.xphs.2017.09.023
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8004fdf2e2913eead1e9740f774a2c2b
https://doi.org/10.1016/j.taap.2017.11.007
https://doi.org/10.1016/j.taap.2017.11.007
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5c4ca868520e02822732a1114f5f125c
https://doi.org/10.1016/j.bmcl.2021.128335
https://doi.org/10.1016/j.bmcl.2021.128335
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e55347996293ce1a7c7b826ca989d0ef
https://doi.org/10.1016/j.bmcl.2017.05.016
https://doi.org/10.1016/j.bmcl.2017.05.016
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/
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e0004b792a5f5c3e407829d184818a26
https://pubmed.ncbi.nlm.nih.gov/31082230
https://pubmed.ncbi.nlm.nih.gov/31082230
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::44d8d5a978c93dfa3b1dcd947097b508
https://pubmed.ncbi.nlm.nih.gov/30732944
https://pubmed.ncbi.nlm.nih.gov/30732944