Zobrazeno 1 - 10
of 35
pro vyhledávání: '"Ajit Jadhav"'
Autor:
Hongchao Zheng, Andrew L. McIver, Surendra Karavadhi, Adam Yasgar, William J. Moore, Li Liu, Zhuyin Li, Carleen Klumpp-Thomas, Ajit Jadhav, Natalia J. Martinez, Kyle R. Brimacombe, Mindy I. Davis, Wei Zhao, Daniel J. Urban, Stephen V. Frye, Anton Simeonov, Xiaodong Wang, Samarjit Patnaik, Rajan Pragani, Mark J. Henderson, Weihe Zhang, Melinda G. Hollingshead, Min Shen, Qingyang Liu, Gordon M. Stott, Tobie D. Lee, Sam Michael, Matthew B. Boxer, Jason M. Rohde, Matthew D. Hall, Yuhong Fang, Joseph M. Covey, Dorian M. Cheff
Publikováno v:
J Med Chem
Neomorphic mutations in isocitrate dehydrogenase 1 (IDH1) are oncogenic for a number of malignancies, primarily low-grade gliomas and acute myeloid leukemia (AML). We report a medicinal chemistry campaign around a 7,7-dimethyl-7,8-dihydro-2H-1λ(2)-q
Autor:
Anju Singh, Marc Ferrer, Xin Xu, Samarjit Patnaik, Thelma M. Escobar, Noel Southall, Myagmarjav Dashynam, Vanja Lazarevic, Ajit Jadhav, Bryan Chim, Juan J. Marugan, Xin Hu, Xiuhuai Liu, Stefan A. Muljo
Publikováno v:
Scientific Reports, Vol 11, Iss 1, Pp 1-14 (2021)
Scientific Reports
Scientific Reports
MicroRNA miR-155 is an important regulatory molecule in the immune system and is highly expressed and functional in Th17 cells, a subset of CD4+ T helper cells which are key players in autoimmune diseases. Small molecules that can modulate miR-155 ma
Autor:
Matthew D. Hall, David J. Maloney, Amy Wang, Jeffrey W. Strovel, Makoto Yoshioka, Daniel J. Urban, Xin Xu, Shyh-Ming Yang, Pranav Shah, Ajit Jadhav, Steven Fletcher, Xin Hu
Publikováno v:
Bioorg Med Chem Lett
A new series of quinazoline-based analogs as potent bromodomain-containing protein 4 (BRD4) inhibitors is described. The structure-activity relationships on 2- and 4-position of quinazoline ring, and the substitution at 6-position that mimic the acet
Autor:
Douglas R. Davies, Gloria A. Benavides, Xin Hu, Jeffrey P. Norenberg, Somnath Jana, Ganesha Rai, Pavan Muttil, Larry A. Sklar, Katherine Pohida, Daniel J. Urban, Kabir, David M. Dranow, Andrew J. Flint, Leonard M. Neckers, Giuseppe L. Squadrito, David J. Maloney, William J. Moore, Victor M. Darley-Usmar, Elias C. Padilha, Ajit Jadhav, Matthew D. Hall, Kyle R. Brimacombe, Dorian M. Cheff, Anton Simeonov, Nitesh K. Kunda, Plamen P. Christov, Pranav Shah, Tamara Anderson, Dingyin Tao, Hu Zhu, Murali Cherukuri, Yuhong Fang, Shyh-Ming Yang, Gary A. Sulikowski, Gordon M. Stott, Donna F. Kusewitt, Tobie D. Lee, Chi V. Dang, Alex G. Waterson, Mark J. Henderson, Bryan T. Mott, Kwangho Kim, Michelle S. Johnson, Helen J. Hathaway, Nobu Oshima
Publikováno v:
J Med Chem
Lactate dehydrogenase (LDH) catalyzes the conversion of pyruvate to lactate, with concomitant oxidation of reduced nicotinamide adenine dinucleotide as the final step in the glycolytic pathway. Glycolysis plays an important role in the metabolic plas
Autor:
David L. Williams, Elias S.J. Arnér, Francesco Angelucci, Paul R. Banta, Haining Lyu, Pavel A. Petukhov, Anton Simeonov, Gregory R. J. Thatcher, Wendy A. Lea, Ajit Jadhav, Qing Cheng
Publikováno v:
ACS Infect Dis
Schistosomiasis is a widespread human parasitic disease currently affecting over 200 million people. Chemotherapy for schistosomiasis relies exclusively on praziquantel. Although significant advances have been made in recent years to reduce the incid
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::48576000631706243cfd9ff4de5f05c3
http://hdl.handle.net/11697/141774
http://hdl.handle.net/11697/141774
Autor:
Ganesha Rai, Joseph Jackson, Dan Crooks, Giuseppe L. Squadrito, Shun Kishimoto, Leonard M. Neckers, Tamara Anderson, Akira Yuno, Min-Jung Lee, Didier Picard, William J. Moore, Daniel J. Urban, Helen H. Hathaway, Jeffrey R. Brender, David J. Maloney, Michael A. Moses, Victor M. Darley-Usmar, Nobu Oshima, Kristin Beebe, Michelle S. Johnson, Anton Simeonov, Ajit Jadhav, Ryo Ishida, Abhinav Joshi, Matthew D. Hall, Gloria A. Benavides, Alex G. Waterson, James Mitchell, Bryan T. Mott, Donna F. Kusewitt, Jane B. Trepel, Gordon M. Stott, Larry A. Sklar, Tobie D. Lee, W. Marston Linehan, Jonathan H. Shrimp, Xin Hu, Kazutoshi Yamamoto, Jeffrey P. Norenberg, Murali Krishna, Chi V. Dang
Publikováno v:
Cell Reports, Vol 30, Iss 6, Pp 1798-1810.e4 (2020)
Cell reports
Cell reports
SUMMARY The reliance of many cancers on aerobic glycolysis has stimulated efforts to develop lactate dehydrogenase (LDH) inhibitors. However, despite significant efforts, LDH inhibitors (LDHi) with sufficient specificity and in vivo activity to deter
Autor:
Myagmarjav Dashnyam, Stefan A. Muljo, Juan J. Marugan, Bryan Chim, Camille A. Spinner, Marc Ferrer, Andrés E. Dulcey, Prasanthi P. Koganti, Anju Singh, Vimal Selvaraj, Noel Southall, Vanja Lazarevic, Kelli M. Wilson, Ajit Jadhav, Xin Hu, Thelma M. Escobar, Xin Xu
Publikováno v:
Scientific Reports
Scientific Reports, Vol 10, Iss 1, Pp 1-14 (2020)
Scientific Reports, Vol 10, Iss 1, Pp 1-14 (2020)
Th17 cells are critical drivers of autoimmune diseases and immunopathology. There is an unmet need to develop therapies targeting pathogenic Th17 cells for the treatment of autoimmune disorders. Here, we report that anxiolytic FGIN-1-27 inhibits diff
Autor:
Diane L. Carlisle, Robert M. Friedlander, Anton Simeonov, Hongchun Li, Murat Can Cobanoglu, Fen Pei, Mark J. Henderson, Andrew M. Stern, Tongying Shun, Timothy R. Lezon, Seyed H Mousavi, D. Lansing Taylor, Steve Titus, Lee Apostle Mcdermott, Michael Fioravanti, Prema Iyer, Mark E. Schurdak, Ivet Bahar, Ajit Jadhav
Publikováno v:
Scientific Reports, Vol 7, Iss 1, Pp 1-16 (2017)
Scientific Reports
Scientific Reports
Quantitative Systems Pharmacology (QSP) is a drug discovery approach that integrates computational and experimental methods in an iterative way to gain a comprehensive, unbiased understanding of disease processes to inform effective therapeutic strat
Autor:
Eric J. Kuenstner, David M. Dranow, Victor M. Darley-Usmar, Gary A. Sulikowski, Douglas R. Davies, Hu Zhu, Ganesha Rai, William J. Moore, David J. Maloney, Anton Simeonov, Dorian M. Cheff, Ajit Jadhav, Chi V. Dang, Kyle R. Brimacombe, Shyh-Ming Yang, Andrew J. Flint, Leonard M. Neckers, Gordon M. Stott, Tobie D. Lee, Xin Hu, Katie Pohida, Christine Lukacs, Alex G. Waterson, Daniel J. Urban, Diane K. Luci, Bryan T. Mott, Gloria A. Benavides, Matthew D. Hall, Jennifer Kouznetsova
Publikováno v:
Journal of Medicinal Chemistry. 60:9184-9204
We report the discovery and medicinal chemistry optimization of a novel series of pyrazole-based inhibitors of human lactate dehydrogenase (LDH). Utilization of a quantitative high-throughput screening paradigm facilitated hit identification, while s
Autor:
Darren P. Wallace, Ajit Jadhav, Robert H. Weiss, Anton Simeonov, Ty C. Voss, Yuchi Chen, Alexey Zahkarov, Josephine F. Trott, Natalia J. Martinez, Carina Danchik, Rosita R. Asawa
Publikováno v:
Scientific Reports, Vol 10, Iss 1, Pp 1-12 (2020)
Scientific Reports
Scientific Reports
Autosomal dominant polycystic kidney disease (ADPKD) is one of the most common inherited monogenic disorders, characterized by a progressive decline in kidney function due in part to the formation of fluid-filled cysts. While there is one FDA-approve