L-735,524: an orally bioavailable human immunodeficiency virus type 1 protease inhibitor.

JP Vacca, BD Dorsey, WA Schleif… - Proceedings of the …, 1994 - National Acad Sciences
To date, numerous inhibitors of the human immunodeficiency virus type 1 protease have
been reported, but few have been studied extensively in humans, primarily as a consequence …

L-735,524: the design of a potent and orally bioavailable HIV protease inhibitor

…, RB Levin, SL McDaniel, JP Vacca… - Journal of medicinal …, 1994 - ACS Publications
A series of HIV protease inhibitors possessing a hydroxylaminepentanamide transition state
isostere have been developed. Incorporationof a basic amine into the backbone of the L-…

A naphthyridine carboxamide provides evidence for discordant resistance between mechanistically identical inhibitors of HIV-1 integrase

…, MS Egbertson, JP Vacca… - Proceedings of the …, 2004 - National Acad Sciences
The increasing incidence of resistance to current HIV-1 therapy underscores the need to
develop antiretroviral agents with new mechanisms of action. Integrase, one of three viral …

Design and synthesis of 8-hydroxy-[1, 6] naphthyridines as novel inhibitors of HIV-1 integrase in vitro and in infected cells

…, LS Payne, JP Guare, JP Vacca… - Journal of medicinal …, 2003 - ACS Publications
Naphthyridine 7 inhibits the strand transfer of the integration process catalyzed by integrase
with an IC 50 of 10 nM and inhibits 95% of the spread of HIV-1 infection in cell culture at …

Structure-based design of potent and selective cell-permeable inhibitors of human β-secretase (BACE-1)

…, S Munshi, AJ Simon, L Kuo, JP Vacca - Journal of medicinal …, 2004 - ACS Publications
We describe the development of cell-permeable β-secretase inhibitors that demonstratively
inhibit the production of the secreted amino terminal fragment of an artificial amyloid …

Integrase inhibitors and cellular immunity suppress retroviral replication in rhesus macaques

…, JP Guare, NJ Anthony, RP Gomez, JS Wai, JP Vacca… - Science, 2004 - science.org
We describe the efficacy of L-870812, an inhibitor of HIV-1 and SIV integrase, in rhesus
macaques infected with the simian-human immunodeficiency virus (SHIV) 89.6P. When initiated …

MK-5172, a selective inhibitor of hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants

…, A Soriano, MW Stahlhut, JP Vacca… - Antimicrobial agents …, 2012 - Am Soc Microbiol
HCV NS3/4a protease inhibitors are proven therapeutic agents against chronic hepatitis C
virus infection, with boceprevir and telaprevir having recently received regulatory approval as …

Discovery of MK‐8742: an HCV NS5A inhibitor with broad genotype activity

…, JA McCauley, AA Nomeir, RM Soll, JP Vacca… - …, 2013 - Wiley Online Library
The NS5A protein plays a critical role in the replication of HCV and has been the focus of
numerous research efforts over the past few years. NS5A inhibitors have shown impressive in …

4-Aryl-2, 4-dioxobutanoic acid inhibitors of HIV-1 integrase and viral replication in cells

…, JP Guare, L Zhuang, VE Grey, JP Vacca… - Journal of medicinal …, 2000 - ACS Publications
Introduction. Human immunodeficiency virus type 1 (HIV-1) is the etiological agent of acquired
immunedeficiency syndrome (AIDS). The unique nature of the replicative cycle of HIV-1 …

Discovery of MK-5172, a macrocyclic hepatitis C virus NS3/4a protease inhibitor

…, M Rowley, PJ Coleman, JP Vacca… - ACS medicinal …, 2012 - ACS Publications
A new class of HCV NS3/4a protease inhibitors containing a P2 to P4 macrocyclic constraint
was designed using a molecular modeling-derived strategy. Building on the profile of …