Zobrazeno 1 - 10
of 31
pro vyhledávání: '"Lisa M, Kopcho"'
Autor:
Joelle M. Onorato, Ching-Hsuen Chu, Zhengping Ma, Lisa M. Kopcho, Hannguang J. Chao, R.Michael Lawrence, Dong Cheng
Publikováno v:
Journal of Lipid Research, Vol 56, Iss 3, Pp 747-753 (2015)
To demonstrate monoacylglycerol acyltransferase 2 (MGAT2)-mediated enzyme activity in a cellular context, cells of the murine secretin tumor cell-1 line of enteroendocrine origin were used to construct human MGAT2-expressing recombinant cell lines. L
Externí odkaz:
https://doaj.org/article/d164256204b843b0ad2be9f52d8848a8
Autor:
Shu Chang, Anthony V. Azzara, Yi-Xin Li, Marta Dabros, James Kempson, Reshma Panemangelor, Huji Turdi, Kimberly A. Foster, William J. Keim, Jean M. Whaley, Jeffrey A. Robl, Fang Moore, Luping Chen, Mary Jane Cullen, Xiaoping Hou, Atsu Apedo, R. Michael Lawrence, Arvind Mathur, David G. Harden, Wei Meng, Kevin O'Malley, Mary Ann Pelleymounter, Hannguang Chao, Pratik Devasthale, Jon J. Hangeland, Zhengping Ma, Dauh-Rurng Wu, Robert Paul Brigance, Guohua Zhao, Lynn M. Abell, Qi Gao, Susan Harvey, Lisa M. Kopcho, Dong Cheng, Elizabeth A. Dierks, Ching-Hsuen Chu, Suzanne Rooney, Xiang-Yang Ye, Saleem Ahmad, Wei Wang
Publikováno v:
Journal of Medicinal Chemistry. 64:14773-14792
MGAT2 inhibition is a potential therapeutic approach for the treatment of metabolic disorders. High-throughput screening of the BMS internal compound collection identified the aryl dihydropyridinone compound 1 (hMGAT2 IC50 = 175 nM) as a hit. Compoun
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::40e90999a2854f1a395c0459b5cd876d
https://doi.org/10.1021/acs.jmedchem.1c01356
https://doi.org/10.1021/acs.jmedchem.1c01356
Autor:
Mark Fereshteh, Xiao Zhu, Tai-An Lin, Prabhakar Rajanna, Cherney Emily Charlotte, Aravind Anandam, Xin Li, Derrick Maley, Liping Zhang, Gopal Dhar, Aaron Balog, Robert M. Borzilleri, Johnni Gullo-Brown, T. Thanga Mariappan, Kathy Johnston-Allegretto, Christine Huang, Venkata Murali, John T. Hunt, Sandeep Mahankali, Gregory D. Vite, Lisa M. Kopcho, Shweta Padmanabhan, Sarah C. Traeger
Publikováno v:
ACS Med Chem Lett
[Image: see text] Indoleamine 2,3-dioxygenase 1 (IDO1) has been identified as a target for small-molecule immunotherapy for the treatment of a variety of cancers including renal cell carcinoma and metastatic melanoma. This work focuses on the identif
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c69bf6be584624b416a38e3f63d582b0
https://doi.org/10.1021/acsmedchemlett.1c00014
https://doi.org/10.1021/acsmedchemlett.1c00014
Autor:
Mian Gao, David J. Shuster, Hai-Yun Xiao, Christine B. Goldstine, Jing Chen, Zhonghui Lu, Victor R. Guarino, Khehyong Ngu, Lisa M. Kopcho, Deepa Calambur, Kurt R. Gregor, Andrew J. Tebben, Jingwu Duan, Luisa Salter-Cid, Hao Lu, Joseph A. Tino, Ning Li, John Hynes, James R. Burke, Joseph Yanchunas, John E. Macor, Steven Sheriff, Dauh-Rurng Wu, Bin Jiang, Patrick J. Shaw, ChiehYing Y. Chang, Jenny Xie, Vojkan Susulic, T. G. Murali Dhar
Publikováno v:
Journal of Medicinal Chemistry. 63:15050-15071
Scaffold hopping and structure-based drug design were employed to identify substituted 4-aminoquinolines and 4-aminonaphthyridines as potent, small molecule inhibitors of tumor necrosis factor alpha (TNFα). Structure-activity relationships in both t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4023f6e8b3a6052dbeee946d81173312
https://doi.org/10.1021/acs.jmedchem.0c01732
https://doi.org/10.1021/acs.jmedchem.0c01732
Autor:
Dong Cheng, Bradley A. Zinker, Yi Luo, Petia Shipkova, Claudia H. De Oliveira, Gopal Krishna, Elizabeth A. Brown, Stephanie L. Boehm, Giridhar S. Tirucherai, Huidong Gu, Zhengping Ma, Ching-Hsuen Chu, Joelle M. Onorato, Lisa M. Kopcho, Ron Ammar, Julia Smith, Pratik Devasthale, R. Michael Lawrence, Steven A. Stryker, Elizabeth A. Dierks, Anthony V. Azzara, Leon Carayannopoulos, Edgar D. Charles, Kimberley A. Lentz, David A. Gordon
Publikováno v:
Cell metabolism. 34(11)
Monoacylglycerol acyltransferase 2 (MGAT2) is an important enzyme highly expressed in the human small intestine and liver for the regulation of triglyceride absorption and homeostasis. We report that treatment with BMS-963272, a potent and selective
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::394387e9e73eae85eafb5bf7ab1908f8
https://pubmed.ncbi.nlm.nih.gov/36323235
https://pubmed.ncbi.nlm.nih.gov/36323235
Autor:
Lisa M. Kopcho, Johnni Gullo-Brown, Shweta Padmanabhan, Pattasseri Shabeerali, Arvind Mathur, Prabhakar Rajanna, Lorell Discenza, Liping Zhang, Zhenqiu Hong, Sarah C. Traeger, Zheng Yang, Cherney Emily Charlotte, Richard Rampulla, David K. Williams, Gopal Dhar, Kimberly A. Foster, James Kempson, Derrick Maley, Mary F. Grubb, Xiao Zhu, Xin Li, Weifang Shan, Robert M. Borzilleri, Diane Delpy, Kevin Stefanski, T. Thanga Mariappan, Gregory D. Vite, Kathy A. Johnston, Audris Huang, Asoka Ranasinghe, Mark Fereshteh, Aravind Anandam, Steven P. Seitz, John T. Hunt, Aaron Balog, Celia D’Arienzo, Anuradha Gupta, Tai-An Lin, Roshan Y. Nimje, Weiwei Guo, Christine Huang, Venkata Murali, Sandeep Mahankali
Publikováno v:
ACS Med Chem Lett
[Image: see text] IDO1 inhibitors have shown promise as immunotherapies for the treatment of a variety of cancers, including metastatic melanoma and renal cell carcinoma. We recently reported the identification of several novel heme-displacing IDO1 i
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f0f0d7f8a891846e7ad07844b139d549
https://europepmc.org/articles/PMC8274105/
https://europepmc.org/articles/PMC8274105/
Autor:
Steven P. Seitz, Gregory D. Vite, John T. Hunt, Mark Fereshteh, Cherney Emily Charlotte, Joseph Fargnoli, Lorell Discenza, Liping Zhang, Jennifer Brown, Xin Li, Kevin Stefanski, Christine Huang, Asoka Ranasinghe, Lisa M. Kopcho, Xiao Zhu, Aaron Balog, Diane Delpy, Sarah C. Traeger, Jesse Swanson, Mary F. Grubb, Zheng Yang, Theresa Ziemba, Kathy A. Johnston, Kimberly A. Foster, Johnni Gullo-Brown, Celia D’Arienzo, Susheel Jethanand Nara, Robert M. Borzilleri, Derrick Maley, Tai-An Lin
Publikováno v:
ACS Med Chem Lett
[Image: see text] Indoleamine 2,3-dioxygenase 1 (IDO1) is a heme-containing dioxygenase enzyme implicated in cancer immune response. This account details the discovery of BMS-986242, a novel IDO1 inhibitor designed for the treatment of a variety of c
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b01df4e45b608d7e7f9d0a0d2c59445e
https://pubmed.ncbi.nlm.nih.gov/33603977
https://pubmed.ncbi.nlm.nih.gov/33603977
Autor:
Arathi Krishnakumar, Lisa M. Kopcho, Michael Basso, Benjamin P. Vokits, Glenn H. Cantor, Sutjano Jusuf, Lei Zhao, Lynn M. Abell, Ashok Dongre, Javed Khan, Steven A. Spronk, Gregory A. Locke, Gerald J. Duke, Andrew Quoc Viet, Scott A. Shaw, Franck Duclos, Ellen K. Kick, Joelle M. Onorato, Charles G. Clark, Ruth R. Wexler, Dilger Andrew K, Ji Gao
Publikováno v:
Bioorganicmedicinal chemistry. 28(22)
Myeloperoxidase (MPO) is a heme peroxidase found in neutrophils, monocytes and macrophages that efficiently catalyzes the oxidation of endogenous chloride into hypochlorous acid for antimicrobial activity. Chronic MPO activation can lead to indiscrim
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::30388866645cc723c34668c20055fd32
https://pubmed.ncbi.nlm.nih.gov/33007547
https://pubmed.ncbi.nlm.nih.gov/33007547
Autor:
Leonard P. Adam, Wei Meng, Ruth R. Wexler, Lisa M. Kopcho, Heather Finlay, Richard Yang, Xiaohong Yin, Kamelia Behnia, David S. Taylor, Gregory A. Locke, Lei Zhao
Publikováno v:
Bioorganicmedicinal chemistry letters. 29(20)
A series of benzothiazoles with a cyano group was synthesized and evaluated as endothelial lipase (EL) inhibitors for the potential treatment of cardiovascular diseases. Efforts to reduce molecular weight and polarity in the series led to improved ph
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d066a528718e06e53e431b6fbfee1443
https://pubmed.ncbi.nlm.nih.gov/31519373
https://pubmed.ncbi.nlm.nih.gov/31519373
Autor:
Matt Soars, Lisa M. Kopcho, Carolyn A. Weigelt, Shilpa Demes, Gregory D. Vite, Mary J. Harner, Rohit Malik, Guo Li, David G. Harden, Charles F. Voliva, Kevin O’Malley, Zheming Ruan, Lan-Ying Qin, Brian J. Arey, Peter K. Park, Jennifer Price, Steven Sheriff, Gerald J. Duke, Ashvinikumar V. Gavai, JIngjing Deng, Brian E. Fink, Christopher M. Barbieri, Max Ruzanov, Muge Celiktas, Mark R. Witmer, Yuval Blat, William D. Schmitz, Joseph G. Naglich, Iyoncy Rodrigo
Publikováno v:
Cancer Research. 81:1140-1140
The chromosome 9p21 (chr9p21) locus is deleted in almost 10% of all cancer types. This locus includes the CDKN2A gene that encodes the critical tumor suppressors p19-ARF and p16-INK4a. Methylthioadenosine phosphorylase (MTAP), a gene proximal to CDKN
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::769a298e5dedd6469a5cf85008a3a619
https://doi.org/10.1158/1538-7445.am2021-1140
https://doi.org/10.1158/1538-7445.am2021-1140