Zobrazeno 1 - 10
of 11
pro vyhledávání: '"Nancy, Contel"'
Autor:
Colin, Zhang, Meizhong, Xu, Chunhong, He, Jincong, Zhuo, David M, Burns, Ding-Quan, Qian, Qiyan, Lin, Yun-Long, Li, Lihua, Chen, Eric, Shi, Costas, Agrios, Linkai, Weng, Vaqar, Sharief, Ravi, Jalluri, Yanlong, Li, Peggy, Scherle, Sharon, Diamond, Deborah, Hunter, Maryanne, Covington, Cindy, Marando, Richard, Wynn, Kamna, Katiyar, Nancy, Contel, Kris, Vaddi, Swamy, Yeleswaram, Gregory, Hollis, Reid, Huber, Steve, Friedman, Brian, Metcalf, Wenqing, Yao
Publikováno v:
SSRN Electronic Journal.
11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) has been identified as the primary enzyme responsible for the activation of hepatic cortisone to cortisol in specific peripheral tissues resulting in the concomitant antagonism of insulin action within
Autor:
Brian Metcalf, Sharon Diamond, Taisheng Huang, Lixin Shao, Swamy Yeleswaram, D. Joseph Rogier, Greg Hollis, Michael Xia, Ke Zhang, Ganfeng Cao, Nancy Contel, Lingquan Kong, Peggy Scherle, Maryanne Covington, Tom Emm, Robert Hughes, Joseph Glenn, Robert C. Newton, Kris Vaddi, Changsheng Zheng, Lou Storace, Chu-Biao Xue, Rajan Anand, Hao Feng, Meloni David, Anlai Wang, Mei Li, Philip A. Morton, Robinson Darius J, Qi Han, Rajesh V. Devraj, Yingxin Zhang
Publikováno v:
ACS Medicinal Chemistry Letters. 2:913-918
We report the discovery of a new (S)-3-aminopyrrolidine series of CCR2 antagonists. Structure-activity relationship studies on this new series led to the identification of 17 (INCB8761/PF-4136309) that exhibited potent CCR2 antagonistic activity, hig
Autor:
Beth Thomas, Gregory Hollis, Patrick J. Haley, Brian Metcalf, Kris Vaddi, Claire L. Neilan, Jack G. Shi, Paul Collier, Nancy Contel, Steven Friedman, Swamy Yeleswaram, Jordan S. Fridman, Denise Hertel, Robert Collins, Stacey Shepard, Peggy Scherle, Timothy Burn, Robert C. Newton, James D. Rodgers
Publikováno v:
Journal of Investigative Dermatology. 131:1838-1844
JAKs are required for signaling initiated by several cytokines (e.g., IL-4, IL-12, IL-23, thymic stromal lymphopoietin (TSLP), and IFNγ) implicated in the pathogenesis of inflammatory skin diseases such as psoriasis and atopic dermatitis (AD). Direc
Autor:
Francesco Passamonti, Bijoyesh Mookerjee, Nancy Contel, Mario Cazzola, Hagop M. Kantarjian, Srdan Verstovsek, Victor Sandor, Peter Rosen, Elisa Rumi, Tiziano Barbui, Alessandro Rambaldi, Giovanni Barosi, Alessandro M. Vannucchi, Lisa Pieri, Chiara Elena, Elisabetta Gattoni, Paola Guglielmelli, Shui He
Publikováno v:
Cancer
BACKGROUND Polycythemia vera (PV) is a myeloproliferative neoplasm associated with somatic gain-of-function mutations of Janus kinase-2 (JAK2). Therapeutic options are limited in patients with advanced disease. Ruxolitinib, an oral JAK1/JAK2 inhibito
Autor:
Frédéric Baribaud, Philip L Liu, Peggy Scherle, Brian Metcalf, Maryanne B. Covington, Gregory Hollis, Steve Friedman, Timothy Burn, Niu Shin, Philip Czerniak, Susan Erickson-Viitanen, Kris Vaddi, Nancy Contel, Kathy Wang, Robert Newton, Naiming Zhou, Swamy Yeleswaram, Yanlong Li, Chu-Biao Xue, Vasudha Garlapati, Kim Solomon, Beth Thomas
Publikováno v:
The Journal of pharmacology and experimental therapeutics. 338(1)
C-C chemokine receptor 5 (CCR5) is a clinically proven target for inhibition of HIV-1 infection and a potential target for various inflammatory diseases. In this article, we describe 5-[(4-{(3S)-4-[(1R,2R)-2-ethoxy-5-(trifluoromethyl)-2,3-dihydro-1H-
Autor:
Greg Hollis, Changsheng Zheng, Hao Feng, Mei Li, Peggy Scherle, Taisheng Huang, Joseph Glenn, Chu-Biao Xue, Kris Vaddi, Lixin Shao, Brian Metcalf, Tom Emm, Nancy Contel, Ke Zhang, Ganfeng Cao, Dilip P. Modi, Lou Storace, Anlai Wang, Sharon Diamond, Robert C. Newton, Chen Lihua, Steven Friedman, Rajan Anand, Vaqar Sharief, Lingquan Kong, Hiroyuki Tanaka, Meloni David, Maryanne Covington, Michael Xia, Laurine G. Galya, Robinson Darius J, Qi Han, Swamy Yeleswaram, Yingxin Zhang
Publikováno v:
ACS medicinal chemistry letters. 2(6)
We report the identification of 13 (INCB3284) as a potent human CCR2 (hCCR2) antagonist. INCB3284 exhibited an IC50 of 3.7 nM in antagonism of monocyte chemoattractant protein-1 binding to hCCR2, an IC50 of 4.7 nM in antagonism of chemotaxis activity
Autor:
Gregory Hollis, Tom Emm, Joseph Glenn, Kris Vaddi, Rajan Anand, Brian Metcalf, Douglas Keller, Peggy Scherle, Chen Lihua, Ke Zhang, Ganfeng Cao, Taisheng Huang, Sharon Diamond, Kim Solomon, Robert C. Newton, Chu-Biao Xue, Jiacheng Zhou, Meloni David, Steven Friedman, Nancy Contel, Anlai Wang, Changsheng Zheng, Bitao Zhao, Swamy Yeleswaram, Hao Feng, Ling Kong, Laurine G. Galya, Fredric Baribaud, Michael Xia, Niu Shin, Mei Li
To identify a CCR5 antagonist as an HIV-1 entry inhibitor, we designed a novel series of indane derivatives based on conformational considerations. Modification on the indane ring led to the discovery of compound 22a (INCB9471) that exhibited high af
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0734e1759782a0457a497299b8c836bd
https://europepmc.org/articles/PMC4007949/
https://europepmc.org/articles/PMC4007949/
Autor:
Bijoyesh Mookerjee, Peter Rosen, Giovanni Barosi, Tiziano Barbui, Elisabetta Gattoni, Lisa Pieri, Mario Cazzola, Francesco Passamonti, Nancy Contel, Elisa Rumi, Alessandro Rambaldi, Hagop M. Kantarjian, Alessandro M. Vannucchi, Shui He, Srdan Verstovsek
Publikováno v:
Blood. 120:804-804
Abstract 804 Background: Polycythemia vera (PV) is characterized by increased erythrocyte production resulting in an increased red blood cell mass. White blood cell (WBC) and platelet counts are also elevated and patients have increased thrombotic ri
Autor:
Lisa Pieri, Srdan Verstovsek, Enrico Tagliarico, Roberta Zini, Nancy Contel, Alberto Bosi, Ruggiero Norfo, Paola Guglielmelli, Alessandro M. Vannucchi, Timothy Burn, Kris Vaddi, Rossella Manfredini
Publikováno v:
ResearcherID
Abstract 3852 Protocol #18424-256 is a Phase 2 study of the JAK1 and JAK2 inhibitor ruxolitinib (INCB01842) in patients with advanced polycythemia vera (PV) and essential thrombocythemia (ET) refractory to hydroxyurea; preliminary results have been r
Autor:
Alessandro M. Vannucchi, Kris Vaddi, Lee P. Schacter, Tiziano Barbui, Elisa Rumi, Reid Huber, Elisabetta Gattoni, Richard S. Levy, Elisabetta Antonioli, Nancy Contel, Lisa Pieri, Srdan Verstovsek, Edward C Bradley, Giovanni Barosi, Francesco Passamonti, William M. Garrett, Alessandro Rambaldi, Mario Cazzola, Peter J. Rosen, Hagop M. Kantarjian, Victor Sandor
Publikováno v:
Blood. 116:313-313
Abstract 313 Background: While advanced PV and ET patients at high thrombotic risk are managed primarily with HU, patients who are intolerant or refractory to HU have limited therapeutic options. Identification of a dominant gain-of-function mutation