Zobrazeno 1 - 10
of 12
pro vyhledávání: '"Michael D. Gaul"'
Autor:
Guozhang Xu, Zhijie Liu, Xinkang Wang, Tianbao Lu, Renee L. DesJarlais, Tho Thieu, Jing Zhang, Zheng Huang Devine, Fuyong Du, Qiu Li, Cynthia M. Milligan, Paul Shaffer, Peder E. Cedervall, John C. Spurlino, Christopher F. Stratton, Beth Pietrak, Lawrence M. Szewczuk, Victoria Wong, Ruth A. Steele, Wouter Bruinzeel, Madhu Chintala, Jose Silva, Michael D. Gaul, Mark J. Macielag, Ravi Nargund
Publikováno v:
Journal of medicinal chemistry. 65(15)
Activated factor XI (FXIa) inhibitors are promising novel anticoagulants with low bleeding risk compared with current anticoagulants. The discovery of potent FXIa inhibitors with good oral bioavailability has been challenging. Herein, we describe our
Autor:
Shyh-Ming, Yang, Yuting, Tang, Rui, Zhang, Huajun, Lu, Gee-Hong, Kuo, Michael D, Gaul, Yaxin, Li, George, Ho, James G, Conway, Yin, Liang, James M, Lenhard, Keith T, Demarest, William V, Murray
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:6773-6776
A new series of urea-based, 4-bicyclic heteroaryl-piperidine derivatives as potent SCD1 inhibitors is described. The structure-activity relationships focused on bicyclic heteroarenes and aminothiazole-urea portions are discussed. A trend of dose-depe
Autor:
Jeremy M. Travins, Carl Crysler, Hufnagel Heather Rae, Karen DiLoreto, Norman Huebert, Michael X. Kolpak, Nalin L. Subasinghe, Jennifer Kirkpatrick, Stephen H. Eisennagel, Bruce E. Tomczuk, Wenxi Pan, Christopher J. Molloy, Ehab Khalil, Nisha S. Ninan, Shelley K. Ballentine, Kristi A. Leonard, Roger F. Bone, Richard Soll, Farah Ali, Michael D. Gaul
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:5303-5307
Complement C1s protease inhibitors have potential utility in the treatment of diseases associated with activation of the classical complement pathway such as humorally mediated graft rejection, ischemia-reperfusion injury (IRI), vascular leak syndrom
Autor:
Kimberly G. Petrov, Thomas R. Caferro, Octerloney B. McDonald, David W. Rusnak, Dana E. Vanderwall, Kelly Horne Donaldson, Tara Renae Rheault, David E. Uehling, Lisa M. Shewchuk, Scott Howard Dickerson, Robert J. Mullin, Michael D. Gaul, Aaron S. Goetz, Glenn M. Spehar, Anne T. Truesdale, Edgar R. Wood
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:817-820
Two new series of potent and selective dual EGFR/ErbB-2 kinase inhibitors derived from novel thienopyrimidine cores have been identified. Isomeric thienopyrimidine cores were evaluated as isosteres for a 4-anilinoquinazoline core and several analogs
Autor:
M. Anthony Leesnitzer, Kimberly G. Petrov, Marcia L. Moss, Darryl Lynn Mcdougald, J. David Becherer, David J. Cowan, Robert W. Wiethe, Millard H. Lambert, David Lee Musso, Robert Andrews, D. Mark Bickett, Jennifer Gabriel Badiang, Michael D. Gaul, Andersen Marc W, Daniel B. Kassel, Michael H. Rabinowitz, R. Kevin Blackburn, Janet Warner, Daniel S. Kinder, Theresa D. Seaton
Publikováno v:
Combinatorial Chemistry & High Throughput Screening. 8:327-339
We report a systematic analysis of the P1' and P2' substrate specificity of TNF-alpha converting enzyme (TACE) using a peptide library and a novel analytical method, and we use the substrate specificity information to design novel reverse hydroxamate
Autor:
Sarva M. Tadepalli, Alex G. Waterson, Perry Scott Brignola, Scott Howard Dickerson, Robert J. Mullin, Thomas R. Caferro, Craig D. Wagner, Hamilton D. Dickson, Dana E. Vanderwall, Kimberly G. Petrov, John C. Ulrich, Michael D. Gaul, Lisa M. Shewchuk, Anne M. Hassell, Kelly Horne Donaldson, Edgar R. Wood, David E. Uehling, Jon D. Williams, Ronald L. Brashear, Barry R. Keith, Wendy L. White, David W. Rusnak, Byron Ellis, Robert J. Griffin, Michael J. Reno
Analysis of the x-ray crystal structure of mono-substituted acetylenic thienopyrimidine 6 complexed with the ErbB family enzyme ErbB-4 revealed a covalent bond between the terminal carbon of the acetylene moiety and the sulfhydryl group of Cys-803 at
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4ee325f04de0f7f4e5e90c473b3e261b
https://europepmc.org/articles/PMC2268535/
https://europepmc.org/articles/PMC2268535/
Autor:
Millard H, Lambert, R Kevin, Blackburn, Theresa D, Seaton, Daniel B, Kassel, Daniel S, Kinder, M Anthony, Leesnitzer, D Mark, Bickett, Janet R, Warner, Marc W, Andersen, Jennifer G, Badiang, David J, Cowan, Michael D, Gaul, Kimberly G, Petrov, Michael H, Rabinowitz, Robert W, Wiethe, J David, Becherer, Darryl L, McDougald, David L, Musso, Robert C, Andrews, Marcia L, Moss
Publikováno v:
Combinatorial chemistryhigh throughput screening. 8(4)
We report a systematic analysis of the P1' and P2' substrate specificity of TNF-alpha converting enzyme (TACE) using a peptide library and a novel analytical method, and we use the substrate specificity information to design novel reverse hydroxamate
Autor:
Marcia L. Moss, David J. Cowan, Bubacz Dulce Garrido, Timothy K. Tippin, Stanford Jennifer Badiang, Michele C. Rizzolio, Robert W. Wiethe, Darryl Lynn Mcdougald, Lee T. Schaller, Joseph H. Chan, James G. Conway, Millard H. Lambert, Justin L. Mitchell, Robert Carl Andrews, M. Anthony Leesnitzer, David Lee Musso, Janet Warner, Andersen Marc W, Michael H. Rabinowitz, J. David Becherer, Kimberly C. Glennon, D. Mark Bickett, Michael D. Gaul, L.Graham Whitesell, Elizabeth J. Beaudet, Richard Austin, Kevin M. Hedeen
Publikováno v:
Bioorganicmedicinal chemistry letters. 11(16)
N -Hydroxyformamide-class metalloprotease inhibitors were designed and synthesized, which have potent broad-spectrum activity versus matrix metalloproteases and TNF-α converting enzyme (TACE). Compound 13c possesses good oral and intravenous pharmac
Publikováno v:
Journal of the American Chemical Society. 114:2258-2260
Publikováno v:
Environmental Science & Technology. 21:777-784
The ozonolyses of 1- and 2-methylnaphthalene and 1,2-, 1,3-, 1,4-, and 2,3-dimethylnaphthalene were performed in dilute aqueous solution, and the resulting nonperoxidic products were extracted, concentrated, and identified. Identification of the ozon