Zobrazeno 1 - 10
of 13
pro vyhledávání: '"M. Anthony Leesnitzer"'
Autor:
Erich W. Baum, Brian Wilson, Jason L. Rowand, David E. Uehling, James Michael Salovich, Kelly Anderson, Ganesh S. Moorthy, Stephon C. Smith, M. Anthony Leesnitzer, Robert A. Mook, Kristen Elizabeth Nailor, Kirk L. Stevens, Arthur Groy, Rakesh Kumar, Mui Cheung, Scott Howard Dickerson, Anne M. Hassell, Jingsong Yang, Lisa M. Shewchuk, Roseanne Gerding, Holly Kathleen Emerson, Charity Atkins, Kevin Wayne Kuntz, Peter Sabbatini, Kyle A. Emmitte
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:1004-1008
The optimization of imidazo[1,2-a]pyridine inhibitors as potent and selective inhibitors of IGF-1R is presented. Further optimization of oral exposure in mice is also discussed. Detailed selectivity, in vitro activity, and in vivo PK profiles of an o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::40ce4aa8f8f52a234e5ce06f2469921a
https://doi.org/10.1016/j.bmcl.2008.11.058
https://doi.org/10.1016/j.bmcl.2008.11.058
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::e9c38b38823234fe10e050a50c9a3d7a
https://doi.org/10.2174/1386207054020840
https://doi.org/10.2174/1386207054020840
Autor:
James M. Way, Vincent Rash, Jon L. Collins, Dana P. Danger, M. Anthony Leesnitzer, Channa K Jayawickreme, David Moncol, David C McCoy, Xi Liang, Sean Ross, Thomas J. Rimele, Grace Chen, Padmaja Vulimiri, Stephen Jenkinson, Dock Steven Thomas, Patrick R. Maloney, Steven M. Sparks, Christopher P. Laudeman
Publikováno v:
Bioorganicmedicinal chemistry letters. 24(14)
The exploration of a diarylsulfonamide series of free fatty acid receptor 4 (FFA4/GPR120) agonists is described. This work led to the identification of selective FFA4 agonist 8 (GSK137647A) and selective FFA4 antagonist 39. The in vitro profile of co
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4a248d91a368ece66d7901b7b21e9d6e
https://pubmed.ncbi.nlm.nih.gov/24881566
https://pubmed.ncbi.nlm.nih.gov/24881566
Autor:
Huangshu Lei, Anne M. Hassell, Rakesh Kumar, M. Anthony Leesnitzer, Toshihiro Hamajima, Felix Deanda, Hiroko Nakamura, Stanley D. Chamberlain, J. Brad Shotwell, Jun Tang, Roseanne Gerding, Samarjit Patnaik, Lisa M. Shewchuck, Kirk L. Stevens
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(11)
Exploration of the SAR around a series of 3,5-disubstituted-1H-pyrrolo[2,3-b]pyridines led to the discovery of novel pyrrolopyridine inhibitors of the IGF-1R tyrosine kinase. Several compounds demonstrated nanomolar potency in enzyme and cellular mec
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::701863fa69f3d183d14561c2ba78ff87
https://pubmed.ncbi.nlm.nih.gov/19394223
https://pubmed.ncbi.nlm.nih.gov/19394223
Autor:
Peter Sabbatini, Roseanne Gerding, Bin Yang, J. Brad Shotwell, Charity Atkins, Robert A. Mook, Lisa M. Shewchuk, Arthur Groy, Huangshu Lei, Rakesh Kumar, Anikó M. Redman, Anne M. Hassell, Kirk L. Stevens, Joseph W. Wilson, M. Anthony Leesnitzer, Jason L. Rowand, Felix Deanda, Stanley D. Chamberlain, Ganesh S. Moorthy, Samarjit Patnaik
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(2)
The evaluation of a series of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidines as inhibitors of the IGF-1R (IGF-IR) receptor tyrosine kinase is reported. Examples demonstrate nanomolar potencies in in vitro enzyme and mechanistic cellular assays as well
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::81af07a50099480b583f1fb5e7b95ef6
https://pubmed.ncbi.nlm.nih.gov/19056263
https://pubmed.ncbi.nlm.nih.gov/19056263
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::993edb682148101da04f2a40507a6ade
https://pubmed.ncbi.nlm.nih.gov/16101009
https://pubmed.ncbi.nlm.nih.gov/16101009
Autor:
Neil Broadway, Millard H. Lambert, M. Anthony Leesnitzer, J. David Becherer, Andreas Ludwig, Christian Hundhausen, Robert Andrews, D. Mark Bickett
Publikováno v:
Combinatorial chemistryhigh throughput screening. 8(2)
The transmembrane metzinkin-proteases of the ADAM (a disintegrin and a metalloproteinase)-family ADAM10 and ADAM 17 are both implicated in the ectodomain shedding of various cell surface molecules including the IL6-receptor and the transmembrane chem
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9d75b7d53a912a8c81a33e4992bf6259
https://pubmed.ncbi.nlm.nih.gov/15777180
https://pubmed.ncbi.nlm.nih.gov/15777180
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e45088b93c91fa2f5b7cc63b35d439d5
https://pubmed.ncbi.nlm.nih.gov/11514157
https://pubmed.ncbi.nlm.nih.gov/11514157
Publikováno v:
High Throughput Screening for Novel Anti-Inflammatories ISBN: 9783034895781
Tumor necrosis factor-α (TNFα) has been implicated in cancer and inflammatory diseases since it was first characterized and eventually identified by researchers in several laboratories in the mid-1980s [1-5]. However, only recently has the patho-lo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::2de5bea4a860ef97df46e52820414e4b
https://doi.org/10.1007/978-3-0348-8462-4_5
https://doi.org/10.1007/978-3-0348-8462-4_5
Autor:
M. Anthony Leesnitzer, Daniel F. Hassler, Justin L. Mitchell, Laurie K. Overton, John R. Didsbury, Wen-Ji Chen, J. David Becherer, Gerard McGeehan, Philip McCauley, Marcos E. Milla, S.-L. Catherine Jin, Jui-Lan Su, Thomas A. Kost, Christine R. Hoffman, Janet Warner, Theresa D. Seaton, H. Luke Carter, Mary Pat Moyer, Marcia L. Moss, Gregory Pahel, Warren J. Rocque, William Burkhart, Frank J Schoenen, William C. Clay, Millard H. Lambert, Derril H. Willard
Publikováno v:
Nature. 385(6618)
Tumour-necrosis factor-alpha (TNF-alpha) is a cytokine that contributes to a variety of inflammatory disease states. The protein exists as a membrane-bound precursor of relative molecular mass 26K which can be processed by a TNF-alpha-converting enzy
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::69260f1d8e755327cff416b9b4e34799
https://pubmed.ncbi.nlm.nih.gov/9034191
https://pubmed.ncbi.nlm.nih.gov/9034191