Výsledky vyhledávání - "Hodge Carl Nicholas"

Corticotropin-Releasing Hormone Receptor Antagonists: Framework Design and Synthesis Guided by Ligand Conformational Studies

Autor: Paul Krenitsky, Strucely P, Robert Scott Cheeseman, Hodge Carl Nicholas, Thomas E. Christos, Zelda R. Wasserman, Paul J. Gilligan, Ciganek E, Nemeth Ga, Fernandez Ch, Everett Latham Scholfield, Argyrios G. Arvanitis, Aldrich Pe, Robert J. Chorvat

Publikováno v: Journal of Medicinal Chemistry. 42:819-832

As described in the preceding paper (Arvanitis et al. J. Med. Chem. 1999, 42), anilinopyrimidines I were identified as potent antagonists of corticotropin-releasing hormone-1 receptor (CRH1-R, also referred to as corticotropin-releasing factor, CRF1-

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::42bf303a90348d0e84a147404df8be90
https://doi.org/10.1021/jm980223o

Zobrazit plný text záznamu

Molecular Recognition of Cyclic Urea HIV-1 Protease Inhibitors

Autor: M.C. Schadt, Charles J. Eyermann, Patricia C. Weber, E. E. Huston, Hodge Carl Nicholas, F.A. Lewandowski, D. D. Mccabe, J. L. Duke, R. J. Deloskey, C.-H. Chang, Prabhakar K. Jadhav, Patrick Y.S. Lam, Paul J. Ala

Publikováno v: Journal of Biological Chemistry. 273:12325-12331

As long as the threat of human immunodeficiency virus (HIV) protease drug resistance still exists, there will be a need for more potent antiretroviral agents. We have therefore determined the crystal structures of HIV-1 protease in complex with six c

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::689417b6939bbd16e9df99fb6043cc24
https://doi.org/10.1074/jbc.273.20.12325

Zobrazit plný text záznamu

Nonpeptide Cyclic Cyanoguanidines as HIV-1 Protease Inhibitors: Synthesis, Structure−Activity Relationships, and X-ray Crystal Structure Studies

Autor: Charles J. Eyermann, Lee T. Bacheler, Francis J. Woerner, W. F. Daneker, C.-H. Chang, Susan Erickson-Viitanen, Patrick Y.S. Lam, J. L. Meek, M. M. Rayner, M.C. Schadt, H.-W. Man, David A. Jackson, Hodge Carl Nicholas, Joseph C. Calabrese, Prabhakar K. Jadhav

Publikováno v: Journal of Medicinal Chemistry. 41:1446-1455

Comparison of the high-resolution X-ray structures of the native HIV-1 protease and its complexes with the inhibitors suggested that the enzyme flaps are flexible. The movement at the tip of the flaps could be as large as 7 A. On the basis of this ob

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2ad2f305239006f212328978f4139bf3
https://doi.org/10.1021/jm970524i

Zobrazit plný text záznamu

Studies on Orally Available Inhibitors of HIV Protease. Peptidyl Aldehydes and Trifluoromethyl Ketones

Autor: Hodge Carl Nicholas, Susan Erickson-Viitanen, Y. N. Wong, M. M. Rayner, M. J. Otto, Fernandez Ch, Aldrich Pe

Publikováno v: Antiviral Chemistry and Chemotherapy. 5:257-262

Low-molecular-weight peptidyl aldehyde inhibitors of HIV protease that reach in vivo plasma concentrations after oral administration substantiailly in excess of the antiviral IC90 are described. We also report efforts to improve the potency and stabi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::0e964180057e59d3025ee9ede9123cd0
https://doi.org/10.1177/095632029400500407

Zobrazit plný text záznamu

In vitro isolation and identification of human immunodeficiency virus (HIV) variants with reduced sensitivity to C-2 symmetrical inhibitors of HIV type 1 protease

Autor: Dean L. Winslow, Sena Garber, Caroline Reid, Y. S. E. Cheng, Hodge Carl Nicholas, C. E. Patterson, P. E. Aldrich, Prabhakar K. Jadhav, M. J. Otto

Publikováno v: Proceedings of the National Academy of Sciences. 90:7543-7547

Protease inhibitors are another class of compounds for treatment of human immunodeficiency virus (HIV)-caused disease. The emergence of resistance to the current anti-HIV drugs makes the determination of potential resistance to protease inhibitors im

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::398306193761e402dd34165e7106eb8c
https://doi.org/10.1073/pnas.90.16.7543

Zobrazit plný text záznamu

Thermodynamic linkage between the binding of protons and inhibitors to HIV-1 protease

Autor: Michael K. Gilson, Joanna Trylska, Martha S. Head, Ronald M. Klabe, Jan M. Antosiewicz, Hodge Carl Nicholas, Maciej Geller

Publikováno v: Protein science : a publication of the Protein Society. 8(1)

The aspartyl dyad of free HIV-1 protease has apparent pK(a)s of approximately 3 and approximately 6, but recent NMR studies indicate that the aspartyl dyad is fixed in the doubly protonated form over a wide pH range when cyclic urea inhibitors are bo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6c56ad8a850f1a814d61be97db5da185
https://pubmed.ncbi.nlm.nih.gov/10210196

Zobrazit plný text záznamu

Molecular basis of HIV-1 protease drug resistance: structural analysis of mutant proteases complexed with cyclic urea inhibitors

Autor: D. D. Mccabe, E. E. Huston, R. J. Deloskey, Ronald M. Klabe, Patrick Y.S. Lam, Hodge Carl Nicholas, C.-H. Chang, C. J. Rizzo, B. D. Korant, Paul J. Ala, J. L. Duke

Publikováno v: Biochemistry. 36(7)

In cell cultures, the key residues associated with HIV-1 resistance to cyclic urea-based HIV-1 protease (PR) inhibitors are Val82 and Ile84 of HIV-1 PR. To gain an understanding of how these two residues modulate inhibitor binding, we have measured t

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f5d7d9e24ba0290f1b74106b55ed3344
https://pubmed.ncbi.nlm.nih.gov/9048541

Zobrazit plný text záznamu

Cyclic HIV protease inhibitors: synthesis, conformational analysis, P2/P2' structure-activity relationship, and molecular recognition of cyclic ureas

Publikováno v: Journal of medicinal chemistry. 39(18)

High-resolution X-ray structures of the complexes of HIV-1 protease (HIV-1PR) with peptidomimetic inhibitors reveal the presence of a structural water molecule which is hydrogen bonded to both the mobile flaps of the enzyme and the two carbonyls flan

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ca252d7787d2a50a77209a603a4cff0c
https://pubmed.ncbi.nlm.nih.gov/8784449

Zobrazit plný text záznamu

Improved cyclic urea inhibitors of the HIV-1 protease: synthesis, potency, resistance profile, human pharmacokinetics and X-ray crystal structure of DMP 450

Publikováno v: Chemistry & Biology. (4):301-314

Background: Effective HIV protease inhibitors must combine potency towards wild-type and mutant variants of HIV with oral bioavailability such that drug levels in relevant tissues continuously exceed that required for inhibition of virus replication.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7b6f9933f8fa950862e149d305a73bd1

Zobrazit plný text záznamu

Vyhledávací nástroje:

Upřesnit hledání