Zobrazeno 1 - 10
of 11
pro vyhledávání: '"Lee T. Schaller"'
Autor:
Tony Y. Wang, Chiara Piubelli, Lee T. Schaller, Pierette Banker, Stefano Tacconi, Paula Selley, Todd W. Shearer, Robert A. Reid, Federico Faggioni, Daniel J. Price, Richard F. Cox, Shawn P. Williams, David H. Drewry, Michela Tessari, Richard G. Buckholz, Patrick R. Maloney, Paul R. Reid, Brian D. Thompson, Xi Liang, Jeffery L. Smith, Octerloney B. McDonald, Ilaria Sartori
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 28:1958-1963
Hypothalamic CAMKK2 represents a potential mechanism for chemically affecting satiety and promoting weight loss in clinically obese patients. Single-digit nanomolar inhibitors of CAMKK2 were identified in three related ATP-competitive series. Limited
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::77ef3d3a14b6690b03d61d51517e7124
https://doi.org/10.1016/j.bmcl.2018.03.034
https://doi.org/10.1016/j.bmcl.2018.03.034
Autor:
Chuck Poole, Alan R. Rendina, Andrew L. Larkin, Heather Hobbs, Helen F. Sneddon, Lee T. Schaller, Gordon Saxty, Jonathan P. Hutchinson, David N. Deaton, Jeffrey Guss, Young Do, Tianshun Xu, Karen Affleck, Simon Teanby Hodgson, Stephen A. Thomson, H. Fritz Kramer, Caterina Musetti, Peckham Gregory, Ian Edward David Smith, Melanie Leveridge, Harry Nicholls, Jason A. Holt, Don O. Somers, Ying Shen, J. Darren Stuart, Sorif Uddin, Anne Cleasby, Paul N. Mortenson, Caroline Richardson, Daniel J. Price, Lisa M. Shewchuk, Eugene L. Stewart, Michael R. Jeune, David Anders, Lisa A. Orband-Miller, Ashley Paul Hancock, Paris Ward, Joseph W. Wilson
Publikováno v:
Bioorganicmedicinal chemistry. 27(8)
With the goal of discovering more selective anti-inflammatory drugs, than COX inhibitors, to attenuate prostaglandin signaling, a fragment-based screen of hematopoietic prostaglandin D synthase was performed. The 76 crystallographic hits were sorted
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::19cd1125a360e08da732c75d2aa1d7f2
https://pubmed.ncbi.nlm.nih.gov/30858025
https://pubmed.ncbi.nlm.nih.gov/30858025
Autor:
Anthony L. Handlon, Lisa M. Leesnitzer, Joseph Wendell Wilson, Rodolfo Cadilla, Philip Stewart Turnbull, Chuck Poole, Raymond V. Merrihew, Lee T. Schaller, John C. Ulrich
Publikováno v:
ACS Medicinal Chemistry Letters. 7:83-88
A series of selective androgen receptor modulators (SARMs) containing the 1-(trifluoromethyl)benzyl alcohol core have been optimized for androgen receptor (AR) potency and drug-like properties. We have taken advantage of the lipophilic ligand efficie
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1948a5cc793f5e6af8fe972330e13665
https://doi.org/10.1021/acsmedchemlett.5b00377
https://doi.org/10.1021/acsmedchemlett.5b00377
Autor:
Edward P. Garvey, Brian A. Johns, Margaret J. Gartland, Scott A. Foster, Wayne H. Miller, Robert G. Ferris, Richard J. Hazen, Mark R. Underwood, Eric E. Boros, James B. Thompson, Jason G. Weatherhead, Cecilia S. Koble, Scott H. Allen, Lee T. Schaller, Ronald G. Sherrill, Tomokazu Yoshinaga, Masanori Kobayashi, Chiaki Wakasa-Morimoto, Shigeru Miki, Koichiro Nakahara, Takeshi Noshi, Akihiko Sato, Tamio Fujiwara
Publikováno v:
Antimicrobial Agents and Chemotherapy. 52:901-908
The naphthyridinone GSK364735 potently inhibited recombinant human immunodeficiency virus type 1 (HIV-1) integrase in a strand transfer assay (mean 50% inhibitory concentration ± standard deviation, 8 ± 2 nM). As expected based on the structure of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9f1ce24916536e22a701ee05912ccf1b
https://doi.org/10.1128/aac.01218-07
https://doi.org/10.1128/aac.01218-07
Autor:
Jeffrey H. Tidwell, George Andrew Freeman, Marty St. Clair, Robert G. Ferris, Lee T. Schaller, Dean W. Selleseth, Steven A. Short, Jill R. Cowan, Lawrence R. Boone, Kurt Weaver, G B Roberts, Joseph H. Chan, Richard J. Hazen, Kelly R. Moniri, Karen Rene Romines
Publikováno v:
Antimicrobial Agents and Chemotherapy. 49:4046-4051
The compound GW678248 is a novel benzophenone nonnucleoside reverse transcriptase inhibitor (NNRTI). Preclinical assessment of GW678248 indicates that this compound potently inhibits wild-type (WT) and mutant human immunodeficiency virus type 1 (HIV-
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4865655b25dbfbe07da6cb52e75ed9fb
https://doi.org/10.1128/aac.49.10.4046-4051.2005
https://doi.org/10.1128/aac.49.10.4046-4051.2005
Autor:
Yu Guo, Scott Howard Dickerson, Jeff Gobel, Dan Gillie, Lee T. Schaller, J. Patrick Condreay, Stephen A. Thomson, Boggs Sharon Davis, Curt D. Haffner
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(23)
We report the synthesis and in vitro activity of a series of novel N-{3-[(1,1-dioxido-1,2-benzothiazol-3-yl)(phenyl)amino]propyl}benzamide analogs. These analogs showed potent inhibitory activity against Kv1.3. Several compounds, including compound 8
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a870ef7f27f641a6b9a4e61ecee832f9
https://pubmed.ncbi.nlm.nih.gov/20971642
https://pubmed.ncbi.nlm.nih.gov/20971642
Autor:
Richard J. Hazen, George Andrew Freeman, Karen Rene Romines, Joseph H. Chan, Jill R. Cowan, Jeffrey H. Tidwell, Steven A. Short, Andrews Clarence Webster, Robert G. Ferris, Lee T. Schaller, David K. Stammers, Steve S. Gonzales, Lawrence R. Boone
Publikováno v:
J Med Chem. 49(2)
Despite the progress of the past two decades, there is still considerable need for safe, efficacious drugs that target human immunodeficiency virus (HIV). This is particularly true for the growing number of patients infected with virus resistant to c
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::405b85ab19f215dab48e2757a2d46a62
http://ora.ox.ac.uk/objects/uuid:3971cc78-77e5-4caf-ab76-51d0ac6e806d
http://ora.ox.ac.uk/objects/uuid:3971cc78-77e5-4caf-ab76-51d0ac6e806d
Autor:
George Andrew Freeman, Jill R. Cowan, Marty St. Clair, Karen Rene Romines, Robert J. Harvey, Lee T. Schaller, Robert G. Ferris, Steven A. Short, Lawrence R. Boone, Joseph H. Chan, Jeffrey H. Tidwell, Richard Hazen
Publikováno v:
Antimicrobial agents and chemotherapy. 49(11)
GW678248, a novel nonnucleoside reverse transcriptase inhibitor, has been evaluated for anti-human immunodeficiency virus activity in a variety of in vitro assays against laboratory strains and clinical isolates. When GW678248 was tested in combinati
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::aeb82d8484dcb9799dc0729602a6161f
https://pubmed.ncbi.nlm.nih.gov/16251284
https://pubmed.ncbi.nlm.nih.gov/16251284
Autor:
Jeffrey H. Tidwell, David J. Reynolds, Lee T. Schaller, George Andrew Freeman, Rob Ferris, Marty St. Clair, G B Roberts, Richard J. Hazen, Joseph H. Chan, Lawrence R. Boone, Kurt Weaver, Gina S. Lowell, Steven A. Short, Andrews Clarence Webster, Steve S. Gonzales, Katrina L. Creech, Jill R. Cowan, George W. Koszalka, Karen Rene Romines
Publikováno v:
Journal of medicinal chemistry. 47(5)
GW4511, GW4751, and GW3011 showed IC50 values ≤2 nM against wild type HIV-1 and
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8e87ff312ea730b47c6c0b635ec73882
https://pubmed.ncbi.nlm.nih.gov/14971897
https://pubmed.ncbi.nlm.nih.gov/14971897
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