Zobrazeno 1 - 10
of 15
pro vyhledávání: '"Deborah D. Jeanfavre"'
Autor:
Michael P. Winters, Renee L. DesJarlais, Mark Bobko, John P. Wolak, Ho Yin Lo, Steven S. Pullen, Deborah D. Jeanfavre, Hnin Hnin Khine, Rosemarie H. Sallati, Ernest L. Raymond, Mohammed A. Kashem, Lei Qiao, Gregory P. Roth, Declan Ryan, Joseph R. Woska, Kevin J. Moriarty, Darius Robinson, Hidenori Takahashi, B. Tomczuk, Wilson Matthew Allan, Ronald L. Magolda, Peter Allen Nemoto, Andre White, Brian Nicholas Cook
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:5545-5549
A series of novel potent benzimidazole based inhibitors of interleukin-2 T-cell kinase (Itk) were prepared. In this report, we discuss the structure-activity relationship (SAR), selectivity, and cell-based activity for the series. We also discuss the
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::77216c0a135ce0c04945949b146cd09c
https://doi.org/10.1016/j.bmcl.2008.09.015
https://doi.org/10.1016/j.bmcl.2008.09.015
Autor:
Kathy O’Shea, Denice M. Spero, Ronald L. Magolda, Mario G. Cardozo, Lisa H. Liu, Hanbo Hu, Derek Cogan, Heather Grbic, Thomas M. Farrell, John P. Wolak, John D. Ginn, Della White, Deborah D. Jeanfavre, Mohammed A. Kashem, Maryanne L. Brown, Anthony S. Prokopowicz, Carol Ann Homon, Erick R. R. Young, Joseph R. Woska, Paul Kaplita, Darren Disalvo, Georg Dahmann, Charles L. Cywin
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:225-230
An uHTS campaign was performed to identify selective inhibitors of PKC-theta. Initial triaging of the hit set based on selectivity and historical analysis led to the identification of 2,4-diamino-5-nitropyrimidines as potent and selective PKC-theta i
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6a34c352960493e0ce0044cbad949680
https://doi.org/10.1016/j.bmcl.2006.09.056
https://doi.org/10.1016/j.bmcl.2006.09.056
Autor:
Sudha Desai, Patricia L. Reilly, Deborah D. Jeanfavre, Gerald Nabozny, Terence A. Kelly, Lemieux Rene M, Maret Panzenbeck
Publikováno v:
European Journal of Pharmacology. 534:233-240
Compound I, a novel small molecule antagonist (Kd=6 nM) of human lymphocyte function-associated antigen-1 (LFA-1, CD11a/CD18) was tested for activity in a humanized mouse model of delayed-type hypersensitivity (trans vivo delayed-type hypersensitivit
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1749fd551f64ce34e2ef8ba2e12717f1
https://doi.org/10.1016/j.ejphar.2006.01.004
https://doi.org/10.1016/j.ejphar.2006.01.004
Autor:
Patricia L. Reilly, Charles Kennedy, Joseph R. Woska, Barbara-Jean Bormann, Christopher Pargellis, Jay Prendergast, Deborah D. Jeanfavre, Carol Stearns, Randall W. Barton
Publikováno v:
Biochemical Pharmacology. 52:1757-1765
CD26 and ecto-adenosine deaminase (ADA) are found associated on the plasma membrane of T lymphocytes and each possess distinct catalytic activities. CD26 has a proteolytic activity identical to dipep-tidylpeptidase IV (DPPIV; E.C. 3.4.14.5), and ecto
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a9e21fb6bb0700ce826e7f390569d276
https://doi.org/10.1016/s0006-2952(96)00597-7
https://doi.org/10.1016/s0006-2952(96)00597-7
Autor:
Stanley Kugler, Mohammed A. Kashem, Ernest L. Raymond, Hidenori Takahashi, Steven S. Pullen, Leslie Martin, Gabriel Labissiere, Jennifer Ahlberg, Jennifer A. Kowalski, Hnin Hnin Khine, Joseph R. Woska, Stéphane De Lombaert, Donna Skow, David S. Thomson, Kathy O’Shea, Brian Nicholas Cook, Renee Zindell, Deborah D. Jeanfavre, Doris Riether, Jörg Bentzien, Kerry L. M. Ralph, Rosemarie Sellati
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(6)
Benzamide 1 demonstrated good potency as a selective ITK inhibitor, however the amide moiety was found to be hydrolytically labile in vivo, resulting in low oral exposure and the generation of mutagenic aromatic amine metabolites. Replacing the benza
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a1df8326828e0236a2add4a210c4153e
https://pubmed.ncbi.nlm.nih.gov/19246196
https://pubmed.ncbi.nlm.nih.gov/19246196
Autor:
Vincent J. Merluzzi, Ronald B. Faanes, Kathleen Last-Barney, Deborah D. Jeanfavre, Eugene J. McNally, Steven D. Marlin, Carol Cahill
Publikováno v:
Journal of Virological Methods. 35:255-264
Soluble intercellular adhesion molecule-1 (sICAM-1) was shown to be the receptor for the major subgroup of rhinoviruses. It was demonstrated that this molecule can inhibit the binding and subsequent infection of target cells by rhinoviruses belonging
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::92006dde1cb6e0c579a0017308b1d64f
https://doi.org/10.1016/0166-0934(91)90067-a
https://doi.org/10.1016/0166-0934(91)90067-a
Autor:
Gary O. Caviness, Mark E. Labadia, Maurice M. Morelock, Joseph R. Woska, Deborah D. Jeanfavre, Kathleen Last-Barney, Patricia Giblin
Publikováno v:
Biochemical pharmacology. 74(1)
Molecular K(d) and k(off) parameters are often used to define the molecular potency of drugs. These constants, however, are determined on purified target proteins, and their relationship to in vivo binding phenomena is poorly understood. Herein, we r
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7d97526b2ffe97d7079f7c65a5284156
https://pubmed.ncbi.nlm.nih.gov/17482579
https://pubmed.ncbi.nlm.nih.gov/17482579
Autor:
Ian Potocki, Shirlynn Chen, Rosemarie Sellati, Patricia L. Reilly, Kei Kishimoto, Emeigh Jonathan Emilian, Gerald Nabozny, Robert Rothlein, Donghong A. Gao, Miao Clara K, Daniel R. Goldberg, Sorcek Ronald J, Daniel Kuzmich, Terence A. Kelly, Drané O'Brien, Deborah D. Jeanfavre, Charline Peng, and Stephen H. Norris, Kevin Chungeng Qian, Elizabeth Mainolfi, Wu Jiang-Ping, Joseph R. Woska, Jocelyn A. Gunn
Publikováno v:
Journal of medicinal chemistry. 47(22)
A novel class of lymphocyte function-associated antigen-1 (LFA-1) inhibitors is described. Discovered during the process to improve the physicochemical and metabolic properties of BIRT377 (1, Figure 1), a previously reported hydantoin-based LFA-1 inh
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fe9a79e4c0fcd3c81b9d9548fd038228
https://pubmed.ncbi.nlm.nih.gov/15481974
https://pubmed.ncbi.nlm.nih.gov/15481974
Autor:
Robert Rothlein, Maret Panzenbeck, Elizabeth Mainolfi, Terence A. Kelly, Rachel R. Kroe, Gary O. Caviness, Kathleen Last-Barney, Joseph R. Woska, Deborah D. Jeanfavre, Patricia Giblin, Steven E. Fogal, Patricia L. Reilly, Takashi Kei Kishimoto
Publikováno v:
Journal of immunological methods. 277(1-2)
The beta(2) integrin LFA-1 (CD11a/CD18) is a leukocyte-specific adhesion molecule that mediates leukocyte extravasation, antigen presentation, and T-cell-mediated cytolysis through its interaction with its counter-receptors, ICAM-1, ICAM-2, and ICAM-
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::142e86ff3ea13b2e8037e20a330cce80
https://pubmed.ncbi.nlm.nih.gov/12799043
https://pubmed.ncbi.nlm.nih.gov/12799043
Autor:
Walter Davidson, Jerry L. Hopkins, Deborah D. Jeanfavre, Kathleen Last Barney, Terence A. Kelly, Christine A. Grygon
Publikováno v:
Journal of the American Society for Mass Spectrometry. 14(1)
The allosteric inhibition of the lymphocyte function associated antigen-1/intercellullar adhesion molecule (LFA-1/ICAM-1) interaction, by a class of small molecules, is characterized by a battery of mass spectrometric techniques. Binding of hydantoin
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::605d9cb10f4c15995f5397b0ad975b07
https://pubmed.ncbi.nlm.nih.gov/12504329
https://pubmed.ncbi.nlm.nih.gov/12504329