Zobrazeno 1 - 10
of 10
pro vyhledávání: '"Sarkiz D Issakani"'
Autor:
Yonchu Jenkins, Tian-Qiang Sun, Vadim Markovtsov, Marc Foretz, Wei Li, Henry Nguyen, Yingwu Li, Alison Pan, Gerald Uy, Lisa Gross, Kristen Baltgalvis, Stephanie L Yung, Tarikere Gururaja, Taisei Kinoshita, Alexander Owyang, Ira J Smith, Kelly McCaughey, Kathy White, Guillermo Godinez, Raniel Alcantara, Carmen Choy, Hong Ren, Rachel Basile, David J Sweeny, Xiang Xu, Sarkiz D Issakani, David C Carroll, Dane A Goff, Simon J Shaw, Rajinder Singh, Laszlo G Boros, Marc-André Laplante, Bruno Marcotte, Rita Kohen, Benoit Viollet, André Marette, Donald G Payan, Todd M Kinsella, Yasumichi Hitoshi
Publikováno v:
PLoS ONE, Vol 8, Iss 12, p e81870 (2013)
Modulation of mitochondrial function through inhibiting respiratory complex I activates a key sensor of cellular energy status, the 5'-AMP-activated protein kinase (AMPK). Activation of AMPK results in the mobilization of nutrient uptake and cataboli
Externí odkaz:
https://doaj.org/article/9f3bbe0f39b0498d932c53dbf27c0985
Autor:
Simon J. Shaw, Dane A. Goff, David C. Carroll, Rajinder Singh, David J. Sweeny, Gary Park, Yonchu Jenkins, Vadim Markovtsov, Tian-Qiang Sun, Sarkiz D. Issakani, Yasumichi Hitoshi, Donald G. Payan
Publikováno v:
Bioorganicmedicinal chemistry. 71
Using an in-cell AMPK activation assay, we have developed structure-activity relationships around a hit pyridine dicarboxamide 5 that resulted in 40 (R419). A particular focus was to retain the on-target potency while also improving microsomal stabil
Autor:
David C. Carroll, Xiulan Zhou, John McLaughlin, Julie Sheung, Rajinder Singh, Sarkiz D. Issakani, Simon J. Shaw, Lyuben Tsvetkov, Arvinder Sran, Donald G. Payan, Jianing Huang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:5199-5202
Structure-activity relationships have been developed around 5-bromo-8-toluylsulfonamidoquinoline 1 a hit compound in an assay for the interaction of the E3 ligase Skp2 with Cks1, part of the SCF ligase complex. Disruption of this protein-protein inte
Autor:
H. Henry Lu, Rao Kolluri, Dane Goff, Peiyong Huang, Hui Hong, Ann Yen, Ning Sheng, Donald G. Payan, Emily Stauffer, Scott Crowder, Xiang Xu, Rajinder Singh, Anthony Martinez, Emily Anderson, Qi Huang, Eileen Goldstein, Todd Kinsella, Kunbin Qu, Philip Achacoso, Ihab S. Darwish, Sarkiz D. Issakani
Publikováno v:
Antimicrobial Agents and Chemotherapy. 52:1419-1429
Hepatitis C virus (HCV) infection is one of the major causes of viral hepatitis, with a great propensity to induce chronicity (21). Liver inflammation can persist for decades in chronic HCV infection and eventually leads to cirrhosis, end-stage liver
Autor:
Alexander B. Rossi, Hui Li, Donald G. Payan, Jeffrey Clough, Ankush Argade, Somasekhar Bhamidipati, Esteban Masuda, Rajinder Singh, Christina Coquilla, Holger Keim, Catherine Sylvain, Sarkiz D. Issakani, David Carroll
Publikováno v:
Bioorganicmedicinal chemistry letters. 25(10)
Here we report the optimization of small molecule inhibitors of human mast cell degranulation via anti-IgE-mediated tryptase release following cross-linking and activation of IgE-loaded FceR1 receptors. The compounds are selective upstream inhibitors
Autor:
Somasekhar Bhamidipati, Sarkiz D. Issakani, David Carroll, Donald G. Payan, Vanessa Taylor, Catherine Sylvain, Holger Keim, Rajinder Singh, Hui Li, Jeffrey Clough, Ellen Herlaar, Brian Wong, Sylvia Braselmann, Esteban Masuda, Ankush Argade, Haoran Zhao
Publikováno v:
Bioorganicmedicinal chemistry letters. 25(10)
Using cultured human mast cells (CHMC) the optimization of 2,4-diaminopyrimidine compounds leading to 22, R406 is described. Compound 22 is a potent upstream inhibitor of mast cell degranulation and its mechanism of action is via inhibition of Syk ki
Autor:
Stacey Huynh, Roy Frances, Vanessa Taylor, Alexander B. Rossi, Ellen Herlaar, Ankush Argade, Esteban Masuda, Donald G. Payan, Sylvia Braselmann, Rajinder Singh, Sarkiz D. Issakani
Publikováno v:
Journal of Allergy and Clinical Immunology. 118:749-755
Background Activation of the IgE receptor, FcɛRI, in mast cells is the key mechanism initiating and propagating pathophysiological responses in allergic rhinitis. Objective Identify and characterize a small molecule inhibitor of IgE-dependent mast c
Autor:
Rajinder Singh, Yonchu Jenkins, Rita Kohen, Gerald Uy, Rachel Basile, Benoit Viollet, Bruno Marcotte, Kristen A. Baltgalvis, Ira J. Smith, Yasumichi Hitoshi, Alexander Owyang, Wei Li, Vadim Markovtsov, Dane Goff, Marc Foretz, David C. Carroll, André Marette, Raniel Alcantara, Carmen Choy, Laszlo G. Boros, Guillermo Godinez, Xiang Xu, Kelly McCaughey, Alison Pan, Tarikere Gururaja, Lisa Gross, Yingwu Li, Kathy White, Todd Kinsella, Donald G. Payan, Hong Ren, Tian-Qiang Sun, Henry Nguyen, Taisei Kinoshita, Simon J. Shaw, Stephanie Yung, David J. Sweeny, Sarkiz D. Issakani, Marc-André Laplante
Publikováno v:
PLoS ONE
PLoS ONE, Vol 8, Iss 12, p e81870 (2013)
PLoS ONE, Vol 8, Iss 12, p e81870 (2013)
Modulation of mitochondrial function through inhibiting respiratory complex I activates a key sensor of cellular energy status, the 5'-AMP-activated protein kinase (AMPK). Activation of AMPK results in the mobilization of nutrient uptake and cataboli
Autor:
Donald G. Payan, Yonchu Jenkins, Sarkiz D. Issakani, Nan Lin, Yingwu Li, Dane Goff, Simon J. Shaw, Jianing Huang, Yasumichi Hitoshi, Xiang Xu, Guodong Dong, Rajinder Singh, Luke Boralsky, Elmer Sampang
Publikováno v:
Cancer Research. 76:3021-3021
5’-AMP-activated protein kinase (AMPK) is a key sensor of cellular energy status and is critical for maintaining energy homeostasis under conditions of nutrient stress. During cellular transformation, metabolic reprogramming enables the aberrant gr
Autor:
Brian R Wong, Susan M. Molineaux, Susan Demo, Todd R. Pray, Mark K. Bennett, Sarkiz D. Issakani, Jianing Huang, Donald G. Payan, Francesco Parlati
Publikováno v:
Drug resistance updates : reviews and commentaries in antimicrobial and anticancer chemotherapy. 5(6)
Disregulation of the cell cycle and proliferation play key roles in cellular transformation and tumorigenesis. Such processes are intimately tied to the concentration, localization and activity of enzymes, adapters, receptors, and structural proteins