Zobrazeno 1 - 9
of 9
pro vyhledávání: '"Manjiri, Ghate"'
Autor:
Elbert Chin, Francisco Xavier Talamas, Jim Li, Kristen Lynn Mccaleb, Manjiri Ghate, Javier de Vicente, Ryan Craig Schoenfeld, Ken A. Brameld, Beihan Wang, Isabel Najera, Vincent Leveque, James Patrick Dunn, Sharada Labadie, Gloria Ao-Ieong, Anthony M. Giannetti, Alfred S-T. Lui, April Wong, Seth F. Harris
Publikováno v:
Journal of Medicinal Chemistry. 56:3115-3119
The use of fragments with low binding affinity for their targets as starting points has received much attention recently. Screening of fragment libraries has been the most common method to find attractive starting points. Herein, we describe a unique
Autor:
Mcintosh Joel, Andreas Kuglstatter, Paul Weller, Sarah C. Abbot, David C. Swinney, Brad Loe, Tobias Gabriel, Roland J. Billedeau, Martin Stahl, Hasim Zecic, Nidhi Arora, Eva Papp, Humberto Bartolome Arzeno, Brian Wong, Allassan Abubakari, Nolan James Dewdney, David Michael Goldstein, Man-Ling Sung, Rebecca T Suttman, Michael Soth, Jaehyeon Park, Kieran Durkin, Fujun Li, Manjiri Ghate, Kristen Lynn Mccaleb, Sandra Frauchiger, Ronald J. Hill
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:3452-3456
Learnings from previous Roche p38-selective inhibitors were applied to a new fragment hit, which was optimized to a potent, exquisitely selective preclinical lead with a good pharmacokinetic profile.
Autor:
Jaehyeon Park, Harlan F Reese, Yun-Chou Tan, Hasim Zecic, Martin Stahl, Keshab Sarma, Renee Litman, Alejandra Trejo, William Bingenheimer, Michael Soth, David Michael Goldstein, Mary Welch, Eric Brian Sjogren, Man-Ling Sung, Sandra Frauchiger, Nolan James Dewdney, Bong San Pablo, Eva Papp, Daniel McWeeney, Ronald J. Hill, Paul Weller, Manjiri Ghate, JoAnn La Fargue, Brian Wong, Stacie A. Dalrymple, James Patrick Dunn, David Mark Rotstein, Richard T. Roberts, Bradford Graves, Rebecca T Suttman, Mcintosh Joel, Farrell Robert P, Andreas Kuglstatter, Chen Jian Jeffrey, Fujun Li, Humberto Bartolome Arzeno, Brad Loe, Tobias Gabriel
Publikováno v:
Journal of Medicinal Chemistry. 54:2255-2265
The development of a new series of p38α inhibitors resulted in the identification of two clinical candidates, one of which was advanced into a phase 2 clinical study for rheumatoid arthritis. The original lead, an lck inhibitor that also potently in
Autor:
Elbert Chin, Manjiri Ghate, Vincent Leveque, Sonal Rajyaguru, Bill Fitch, Jahari Laurant Tracy, Michael Brandl, Steve A. de Keczer, Ramona Hilgenkamp, Fell Jay Bradford, Tatyana Voronin, Isabel Najera, Gloria Ao-Ieong, Javier de Vicente, Shao-Yong Wu, Beihan Wang, Stacey Renee Spencer, Stengel Peter J, Peter Mohr, Mohammad R. Masjedizadeh, James F. Blake, Robert Than Hendricks, Todd R. Elworthy, David Bernard Smith, Junping Zhao, Ludmila Alexandrova, Robinson John E, Al Lui, John P. Fischer, Seth F. Harris, Jim Li, Connie Oshiro, Calvin Yee, Sophie Le Pogam
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:5648-5651
Benzothiazine-substituted tetramic acids were discovered as highly potent non-nucleoside inhibitors of HCV NS5B polymerase. X-ray crystallography studies confirmed the binding mode of these inhibitors with HCV NS5B polymerase. Rational optimization o
Autor:
Ludmila Alexandrova, Connie Oshiro, Ramona Hilgenkamp, Stengel Peter J, Isabel Najera, Peter Mohr, Jahari Laurant Tracy, Susan Larrabee, James F. Blake, David Bernard Smith, Bamberg Joe Timothy, George Adjabeng, Vincent Leveque, Andrew J. Briggs, Brian Xu, Seth F. Harris, Rebecca A. Stephenson, Sonal Rajyaguru, Manjiri Ghate, Beihan Wang, John P. Fischer, Stacey Renee Spencer, Calvin Yee, Sophie Le Pogam, Elbert Chin, Michael Brandl, Fell Jay Bradford, Gloria Ao-Ieong, Sunil Sukhtankar, Robert Than Hendricks, Jim Li, Robinson John E, Todd R. Elworthy, Farrell Robert P, Javier de Vicente
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:3642-3646
A new series of benzothiazine-substituted quinolinediones were evaluated as inhibitors of HCV polymerase NS5B. SAR studies on this series revealed a methyl sulfonamide group as a high affinity feature. Analogues with this group showed submicromolar p
Autor:
David M, Goldstein, Michael, Soth, Tobias, Gabriel, Nolan, Dewdney, Andreas, Kuglstatter, Humberto, Arzeno, Jeffrey, Chen, William, Bingenheimer, Stacie A, Dalrymple, James, Dunn, Robert, Farrell, Sandra, Frauchiger, JoAnn, La Fargue, Manjiri, Ghate, Bradford, Graves, Ronald J, Hill, Fujun, Li, Renee, Litman, Brad, Loe, Joel, McIntosh, Daniel, McWeeney, Eva, Papp, Jaehyeon, Park, Harlan F, Reese, Richard T, Roberts, David, Rotstein, Bong, San Pablo, Keshab, Sarma, Martin, Stahl, Man-Ling, Sung, Rebecca T, Suttman, Eric B, Sjogren, Yunchou, Tan, Alejandra, Trejo, Mary, Welch, Paul, Weller, Brian R, Wong, Hasim, Zecic
Publikováno v:
Journal of medicinal chemistry. 54(7)
The development of a new series of p38α inhibitors resulted in the identification of two clinical candidates, one of which was advanced into a phase 2 clinical study for rheumatoid arthritis. The original lead, an lck inhibitor that also potently in
Autor:
Manjiri Ghate, David E. Shaw, Armando G. Villaseñor, Stan Tsing, Jim W. Barnett, Michelle F. Browner, Andreas Kuglstatter
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(17)
JNK2 and p38alpha are closely related mitogen-activated protein kinases that regulate various cellular activities and are considered drug targets for inflammatory diseases. We have determined the X-ray crystal structure of the clinical phase II p38al
Autor:
David Sperandio, Bradley A. Katz, Paul A. Sprengeler, Kyle Mortara, Hedy Chan, Manjiri Ghate, William D. Shrader, Joseph D. Ho, John R. Somoza, Christine Luong, Mary E. McGrath
Publikováno v:
Structure (London, England : 1993). 11(9)
Hepsin is an integral membrane protein that may participate in cell growth and in maintaining proper cell morphology and is overexpressed in a number of primary tumors. We have determined the 1.75 A resolution structure of the extracellular component