J
Joel R. Huff
Researcher at United States Military Academy
Publications - 114
Citations - 4252
Joel R. Huff is an academic researcher from United States Military Academy. The author has contributed to research in topics: Protease & HIV-1 protease. The author has an hindex of 28, co-authored 114 publications receiving 4163 citations. Previous affiliations of Joel R. Huff include Duke University & Merck & Co..
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Journal ArticleDOI
Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors.
Craig W. Lindsley,Zhijian Zhao,William H. Leister,Ronald G. Robinson,Stanley F. Barnett,Deborah Defeo-Jones,Raymond E. Jones,George D. Hartman,Joel R. Huff,Hans E. Huber,Mark E. Duggan +10 more
TL;DR: An iterative analog library synthesis approach quickly provided a highly selective Akt1/Akt2 inhibitor that induces apoptosis in tumor cells and inhibits Akt phosphorylation in vivo.
Journal ArticleDOI
L-743, 726 (DMP-266): a novel, highly potent nonnucleoside inhibitor of the human immunodeficiency virus type 1 reverse transcriptase.
Steven D. Young,Susan F. Britcher,Tran Lekhanh O,Payne Linda S,William C. Lumma,Terry A. Lyle,Joel R. Huff,P. S. Anderson,David B. Olsen,S S Carroll +9 more
TL;DR: A new class of NNRTIs, the 1, 4-dihydro-2H-3, 1-benzoxazin-2-ones, was developed and L-743, 726 (DMP-266), a member of this class, was chosen for clinical evaluation because of its in vitro properties.
Journal ArticleDOI
A naphthyridine carboxamide provides evidence for discordant resistance between mechanistically identical inhibitors of HIV-1 integrase.
Daria J. Hazuda,Neville J. Anthony,Robert P. Gomez,Samson M. Jolly,John S. Wai,Linghang Zhuang,Thorsten E. Fisher,Mark Embrey,James P. Guare,Melissa S. Egbertson,Joseph P. Vacca,Joel R. Huff,Peter J. Felock,Marc V. Witmer,Kara A. Stillmock,Robert M. Danovich,Jay A. Grobler,Michael D. Miller,Amy S. Espeseth,Lixia Jin,I.-W. Chen,Jiunn H. Lin,Kelem Kassahun,Joan D. Ellis,Bradley K. Wong,Wei Xu,Paul G. Pearson,William A. Schleif,Riccardo Cortese,Emilio A. Emini,Vincenzo Summa,M. Katharine Holloway,Steven D. Young +32 more
TL;DR: These studies provide a structural basis and rationale for developing integrase inhibitors with the potential for unique and nonoverlapping resistance profiles and propose a model of the two inhibitors that is consistent with this observation and suggests specific interactions with discrete binding sites for each ligand.
Journal ArticleDOI
Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H- pyrazol-5-yl)benzamides that potentiate receptor function in vivo.
Craig W. Lindsley,David D. Wisnoski,William H. Leister,Julie A. O'Brien,Wei Lemaire,David L. Williams,Maryann Burno,Cyrille Sur,Gene G. Kinney,Doug J. Pettibone,Philip R. Tiller,Sheri Smith,Mark E. Duggan,George D. Hartman,P. Jeffrey Conn,Joel R. Huff +15 more
TL;DR: Compound 8q demonstrated in vivo proof of concept in an animal behavior model where known antipsychotics are active, supporting the development of new antipsychotic based on the NMDA hypofunction model for schizophrenia.