Zobrazeno 1 - 10
of 73
pro vyhledávání: '"John S. Wai"'
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1eaea12dee6f95904b15f4c9e925d0b1
https://doi.org/10.1021/acs.jmedchem.0c01845
https://doi.org/10.1021/acs.jmedchem.0c01845
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
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::519ca8bb4de4ed4b24ce14fe281e518e
https://pubmed.ncbi.nlm.nih.gov/33596073
https://pubmed.ncbi.nlm.nih.gov/33596073
Autor:
Peter S. Dragovich, Jun Guo, Josefa dela Cruz-Chuh, Guangmin Li, Binqing Wei, Zijin Xu, Leanna Staben, Geoff Del Rosario, Shang-Fan Yu, Thomas H. Pillow, Katherine R. Kozak, Mary Ann Go, Jinhua Chen, Rebecca K. Rowntree, John S. Wai, Carl Ng, Keyang Xu, Donglu Zhang, S. Cyrus Khojasteh, Gail Lewis Phillips
Publikováno v:
Journal of medicinal chemistry. 63(17)
Cytotoxic pyrrolobenzodiazepine (PBD)-dimer molecules are frequently utilized as payloads for antibody-drug conjugates (ADCs), and many examples are currently in clinical development. In order to further explore this ADC payload class, the physicoche
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1f05642a14801d439bd63d27f4c631bb
https://pubmed.ncbi.nlm.nih.gov/32787101
https://pubmed.ncbi.nlm.nih.gov/32787101
Autor:
Chris Frantz, Keyang Xu, Katherine R. Kozak, Thomas H. Pillow, Zijin Xu, Geoffrey Del Rosario, Pragya Adhikari, Douglas D. Leipold, Andrew Polson, Jinhua Chen, Shang-Fan Yu, Mary Ann T. Go, Breanna S. Vollmar, Josefa dela Cruz-Chuh, Peter S. Dragovich, Amrita V. Kamath, Hans Erickson, Fiona Zhong, John S. Wai, Carl Ng, Melissa Schutten
Publikováno v:
Molecular cancer therapeutics. 20(6)
Calicheamicin antibody–drug conjugates (ADCs) are effective therapeutics for leukemias with two recently approved in the United States: Mylotarg (gemtuzumab ozogamicin) targeting CD33 for acute myeloid leukemia and Besponsa (inotuzumab ozogamicin)
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::13ea774d110d9f3fb9ee986f88f4881a
https://pubmed.ncbi.nlm.nih.gov/33722856
https://pubmed.ncbi.nlm.nih.gov/33722856
Autor:
Yuan Chen, Matthew R. Durk, Lionel Rouge, Peter A. S. Smith, Man-Wah Tan, John S. Wai, Jacob Schwarz, Tucker C. Roberts, Jing Kang, Donghong Yan, Hany S. Girgis, Summer Park, John G. Quinn, Min Xu, Prasuna Paraselli, Christopher E. Heise, Jeremy Murray, Wilson Phung, Yongsheng Chen, James J. Crawford, Robert I. Higuchi, Zhiyong Yu, Michael F. T. Koehler, Elizabeth Skippington, Hua Zhang
Publikováno v:
Nature. 561:189-194
Multidrug-resistant bacteria are spreading at alarming rates, and despite extensive efforts no new class of antibiotic with activity against Gram-negative bacteria has been approved in over fifty years. Natural products and their derivatives have a k
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::51ec234ca5fb6e9853f7b3be3f183058
https://doi.org/10.1038/s41586-018-0483-6
https://doi.org/10.1038/s41586-018-0483-6
Autor:
Peter S. Dragovich, Sheila Ulufatu, John S. Wai, James Lee, Reginald Delarosa, Carl Ng, Zijin Xu, Chunjiao Chen, Shang-Fan Yu, S. Cyrus Khojasteh, Gail Lewis Phillips, Rebecca K. Rowntree, Keyang Xu, Aimee Fourie-O'Donohue, Zhonghua Pei, Isabel Figueroa, Liling Liu, Josefa dela Cruz-Chuh, Jiawei Lu, Jun Guo, Weiwei Jin, Jing Wang, Jinhua Chen, Eva Lin, Nicola J. Stagg, David Stokoe, Scott E. Martin, Trung Nguyen, Donglu Zhang, Hui Yao, Guangmin Li, Rachana Ohri, Thomas H. Pillow, Katherine R. Kozak, Brandon Latifi, Yuzhong Deng, Vishal Verma
Publikováno v:
Molecular Pharmaceutics. 15:3979-3996
A number of cytotoxic pyrrolobenzodiazepine (PBD) monomers containing various disulfide-based prodrugs were evaluated for their ability to undergo activation (disulfide cleavage) in vitro in the presence of either glutathione (GSH) or cysteine (Cys).
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::137e6f9931e607d2a0302bf2150b678d
https://doi.org/10.1021/acs.molpharmaceut.8b00431
https://doi.org/10.1021/acs.molpharmaceut.8b00431
Autor:
Maureen Beresini, Vickie Tsui, John S. Wai, F. Anthony Romero, Gladys de Leon Boenig, Patrick Cyr, Xiaoyu Zhu, Kevin X. Chen, Jiangpeng Liao, Edna F. Choo, Susan Kaufman, Fei Wang, Kwong Wah Lai, Caicai Zhu, Zhongguo Chen, Terry Crawford, Weichao Shen, Wenfeng Liu, Jeremy Murray, Yingjie Li, Sarah M. Bronner, Steven Magnuson, Justin Ly
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 28:15-23
A novel, potent, and orally bioavailable inhibitor of the bromodomain of CBP, compound 35 (GNE-207), has been identified through SAR investigations focused on optimizing al bicyclic heteroarene to replace the aniline present in the published GNE-272
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a093625fe16457098a0a0b8d624a6c4e
https://doi.org/10.1016/j.bmcl.2017.11.025
https://doi.org/10.1016/j.bmcl.2017.11.025
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