Research Topics
Species | D HazudaSummaryAffiliation: Merck Research Laboratories Country: USA Publications
| Collaborators
|
Detail Information
Publications
Replication fitness and NS5B drug sensitivity of diverse hepatitis C virus isolates characterized by using a transient replication assaySteven W Ludmerer
Department of Antiviral Research, Merck Research Laboratories, P.O. Box 4, Sumneytown Pike, West Point, PA 19486, USA
Antimicrob Agents Chemother 49:2059-69. 2005....- Biochemical and cell-based assays for characterization of BACE-1 inhibitorsBeth L Pietrak
Department of Biological Chemistry, Merck Research Laboratories, West Point, PA 19486, USA
Anal Biochem 342:144-51. 2005..To illustrate the use of these assays, the properties of a potent, cell-active BACE-1 inhibitor are described... - A potent and orally active HIV-1 integrase inhibitorMelissa S Egbertson
Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA
Bioorg Med Chem Lett 17:1392-8. 2007..A 1,6-naphthyridine inhibitor of HIV-1 integrase has been discovered with excellent inhibitory activity in cells, good pharmacokinetics, and an excellent ability to inhibit virus with mutant enzyme... - Synthesis of 5-(1-H or 1-alkyl-5-oxopyrrolidin-3-yl)-8-hydroxy-[1,6]-naphthyridine-7-carboxamide inhibitors of HIV-1 integraseJeffrey Y Melamed
Department of Medicinal Chemistry, Merck Research Laboratories, 770 Sumneytown Pike, PO Box 4, West Point, PA 19486, USA
Bioorg Med Chem Lett 18:5307-10. 2008..These analogs exhibit excellent activity against viral replication in a cell-based assay. The preparation of these compounds was enabled by a three-step, two-pot reaction sequence from a common butenolide intermediate... - Resistance to inhibitors of the human immunodeficiency virus type 1 integrationDaria J Hazuda
State University of New York, NY, USA
Braz J Infect Dis 14:513-8. 2010..This review will summarize the role of integrase in HIV-1 infection, the mechanism of integrase inhibitors and resistance with an emphasis on raltegravir (RAL), the first integrase inhibitor licensed to treat HIV-1 infection... - Isolation and characterization of novel human immunodeficiency virus integrase inhibitors from fungal metabolitesD Hazuda
Department of Antiviral Research, Merck Research Laboratories, West Point, PA 19486, USA
Antivir Chem Chemother 10:63-70. 1999..These results demonstrate the utility of using an appropriately configured assay to identify compounds that are effective post-assembly and the potential of isolating novel integrase inhibitors from complex natural product extracts... - Integrase inhibitors and cellular immunity suppress retroviral replication in rhesus macaquesDaria J Hazuda
Department of Biological Chemistry, Merck Research Laboratories, Post Office Box 4, West Point, PA 19486, USA
Science 305:528-32. 2004..These studies demonstrate integrase inhibitor activity in vivo and suggest that cellular immunity facilitates chemotherapeutic efficacy in retroviral infections... - Emerging pharmacology: inhibitors of human immunodeficiency virus integrationDaria Hazuda
Merck Research Labs, West Point, Pennsylvania 19486, USA
Annu Rev Pharmacol Toxicol 49:377-94. 2009..In addition, available pharmacokinetic and drug interaction data for raltegravir and elvitegravir, the two integrase inhibitors that are the most advanced in clinical development to date, are reviewed... - A naphthyridine carboxamide provides evidence for discordant resistance between mechanistically identical inhibitors of HIV-1 integraseDaria J Hazuda
Department of Biological Chemistry, Merck Research Laboratories, P O Box 4, West Point, PA 19486, USA
Proc Natl Acad Sci U S A 101:11233-8. 2004..These studies provide a structural basis and rationale for developing integrase inhibitors with the potential for unique and nonoverlapping resistance profiles... - Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 2: structure-activity relationships for substituted 2-Aryl-1-[N-(methyl)-N-(phenylsulfonyl)amino]-4-(piperidin-1-yl)butanesP E Finke
Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA
Bioorg Med Chem Lett 11:265-70. 2001..The phenyl was found to be important for CCR5 antagonism and substitution was limited to small moieties at the 3-position (13 and 16: X= H, 3-F, 3-Cl, 3-Me)... - Design, synthesis, and SAR of heterocycle-containing antagonists of the human CCR5 receptor for the treatment of HIV-1 infectionD Kim
Department of Medicinal Chemistry, Merck Research Laboratories, RY 121 240, PO Box 2000, Rahway, NJ 07065, USA
Bioorg Med Chem Lett 11:3103-6. 2001..The synthesis, SAR, and biological profiles of this class of antagonists are described... - Equivalent inhibition of half-site and full-site retroviral strand transfer reactions by structurally diverse compoundsD Hazuda
Department of Antiviral Research, Merck Research Laboratories, West Point, Pennsylvania 19486, USA
J Virol 71:807-11. 1997..These studies therefore support the utility of using in vitro assays employing either recombinant or virion-derived IN to identify inhibitors of integration... - 1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 2: lead optimization affording selective, orally bioavailable compounds with potent anti-HIV activityJ J Hale
Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA
Bioorg Med Chem Lett 11:2741-5. 2001..Investigations of the structure-activity relationships of 1,3,4-trisubstituted pyrrolidine human CCR5 receptor antagonists afforded orally bioavailable compounds with the ability to inhibit HIV replication in vitro... - Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 4: synthesis and structure-activity relationships for 1-[N-(methyl)-N-(phenylsulfonyl)amino]-2-(phenyl)-4-(4-(N-(alkyl)-N-(benzyloxycarbonyl)amino)piperidin-1-yl)butanesP E Finke
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA
Bioorg Med Chem Lett 11:2475-9. 2001..Herein, structure-activity relationship studies of non-spiro piperidines are described, which led to the discovery of 4-(N-(alkyl)-N-(benzyloxycarbonyl)amino)piperidine derivatives (3-5) as potent CCR5 antagonists... - Dissecting the effects of DNA polymerase and ribonuclease H inhibitor combinations on HIV-1 reverse-transcriptase activitiesCathryn A Shaw-Reid
Department of Antiviral Research, Merck Research Laboratories, West Point, Pennsylvania 19486-0004, USA
Biochemistry 44:1595-606. 2005.... - Antagonists of the human CCR5 receptor as anti-HIV-1 agents. part 1: discovery and initial structure-activity relationships for 1 -amino-2-phenyl-4-(piperidin-1-yl)butanesC P Dorn
Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA
Bioorg Med Chem Lett 11:259-64. 2001..Herein, we describe the discovery of this lead structure and our initial structure activity relationship studies directed toward the requirement for and optimization of the 1-amino fragment... - Isolation, structure, absolute stereochemistry, and HIV-1 integrase inhibitory activity of integrasone, a novel fungal polyketideKithsiri B Herath
Natural Products Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, New Jersey 07065, USA
J Nat Prod 67:872-4. 2004..This bicyclic dihydroxy epoxide lactone inhibited the strand transfer reaction of HIV-1 integrase with an IC(50) of 41 microM... - Diketo acid inhibitor mechanism and HIV-1 integrase: implications for metal binding in the active site of phosphotransferase enzymesJay A Grobler
Department of Biological Chemistry, Merck Research Laboratories, P.O. Box 4, West Point, PA 19486, USA
Proc Natl Acad Sci U S A 99:6661-6. 2002..These studies thus have implications for modeling active site inhibitors of IN, designing and evaluating analogs with improved efficacy, and identifying inhibitors of other metal-dependent phosphotransferases... - The complestatins as HIV-1 integrase inhibitors. Efficient isolation, structure elucidation, and inhibitory activities of isocomplestatin, chloropeptin I, new complestatins, A and B, and acid-hydrolysis products of chloropeptin IS B Singh
Merck Research Laboratories, P O Box 2000, Rahway, New Jersey 07065, USA
J Nat Prod 64:874-82. 2001..The structure-activity relationship as revealed by these compounds could possibly lead to the design of better inhibitors or understanding of the HIV-1 integrase target... - Rapid P1 SAR of brain penetrant tertiary carbinamine derived BACE inhibitorsHong Zhu
Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA
Bioorg Med Chem Lett 20:1779-82. 2010..This inhibitor was characterized in a cisterna magna ported rhesus monkey model, where significant lowering of CSF Abeta40 was observed... - Isolation, structure, and HIV-1 integrase inhibitory activity of Cytosporic acid, a fungal metabolite produced by a Cytospora spHiranthi Jayasuriya
Merck Research Laboratories, P.O. Box 2000, Rahway, New Jersey 07065, USA
J Nat Prod 66:551-3. 2003..collected from Puerto Rico. It inhibited strand transfer reaction of HIV-1 integrase with an IC(50) of 20 microM. The isolation, structure elucidation, relative stereochemistry, and activity of 1 are described... - Monitoring the development of non-nucleoside reverse transcriptase inhibitor-associated resistant HIV-1 using an electrochemiluminescence-based reverse transcriptase polymerase assayVandna Munshi
Department of Antiviral Research, Merck Research Laboratories, West Point, PA 19486, USA
Anal Biochem 374:121-32. 2008..The magnitude of resistance of the resulting mutant viruses was assessed directly by the assay, eliminating the need for cloning, expressing, and purifying the RT mutants... - Compounds that bind APP and inhibit Abeta processing in vitro suggest a novel approach to Alzheimer disease therapeuticsAmy S Espeseth
Biological Chemistry, Medicinal Chemistry, and Automated Biotechnology, Merck Research Laboratories, West Point, Pennsylvania 19486, USA
J Biol Chem 280:17792-7. 2005..These studies demonstrate that APP binding agents can affect its processing through multiple pathways, providing proof of concept for novel strategies aimed at selectively modulating Abeta production... - Isolation, structure and HIV-1 integrase inhibitory activity of exophillic acid, a novel fungal metabolite from Exophiala pisciphilaJohn G Ondeyka
Natural Products Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, New Jersey 07065, USA
J Antibiot (Tokyo) 56:1018-23. 2003..Exophillic acid (1) and aquastatin A (2), a related compound, inhibited the strand transfer reaction of HIV-1 integrase with IC50 values of 68 and 50 microM, respectively... - Combinatorial synthesis of CCR5 antagonistsC A Willoughby
Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA
Bioorg Med Chem Lett 11:3137-41. 2001..Compounds with novel combinations of subunits were discovered that have high binding affinity for the CCR5 receptor. A potent CCR5 antagonist from the library, compound 11 was found to have moderate anti-HIV-1 activity... - 10-Hydroxy-7,8-dihydropyrazino[1',2':1,5]pyrrolo[2,3-d]pyridazine-1,9(2H,6H)-diones: potent, orally bioavailable HIV-1 integrase strand-transfer inhibitors with activity against integrase mutantsCatherine M Wiscount
Department of Medicinal Chemistry, WP14 3, Merck Research Laboratories, West Point, PA 19486, USA
Bioorg Med Chem Lett 18:4581-3. 2008..v. t(1/2)=5.3 h, f=17%)... - Design and synthesis of substituted 4-oxo-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrazine-2-carboxamides, novel HIV-1 integrase inhibitorsH Marie Langford
Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA
Bioorg Med Chem Lett 18:721-5. 2008.... - 8-Hydroxy-3,4-dihydropyrrolo[1,2-a]pyrazine-1(2H)-one HIV-1 integrase inhibitorsThorsten E Fisher
Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA
Bioorg Med Chem Lett 17:6511-5. 2007..31microM. Further SAR exploration led to the preparation of pseudosymmetrical tricyclic pyrrolopyrazine inhibitors 23 and 24 with further improvement in antiviral activity... - Dihydroxypyridopyrazine-1,6-dione HIV-1 integrase inhibitorsJohn S Wai
Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA
Bioorg Med Chem Lett 17:5595-9. 2007..31 microM and exhibits no shift in potency in the presence of 50% normal human serum. It displays a good pharmacokinetic profile when dosed in rats and no covalent binding with microsomal proteins in both in vitro and in vivo models... - Gene expression profiling of rat liver reveals a mechanistic basis for ritonavir-induced hyperlipidemiaPek Yee Lum
Rosetta Inpharmatics LLC, 401 Terry Avenue North, Seattle, WA 98109, USA
Genomics 90:464-73. 2007.... - A human monoclonal antibody neutralizes diverse HIV-1 isolates by binding a critical gp41 epitopeMichael D Miller
Department of Antiviral Research, Merck Research Laboratories, West Point, PA 19486, USA
Proc Natl Acad Sci U S A 102:14759-64. 2005..Our data provide a structural framework for the design of new immunogens and therapeutic antibodies with crossneutralizing potential... - Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infectionVincenzo Summa
Istituto di Ricerche di Biologia Molecolare, P Angeletti SpA Merck Research Laboratories, Rome, Via Pontina Km 30, 600, 00040 Pomezia, Italy
J Med Chem 51:5843-55. 2008.... - Distinct mutation pathways of non-subtype B HIV-1 during in vitro resistance selection with nonnucleoside reverse transcriptase inhibitorsMing Tain Lai
Department of Antiviral Research, Merck Research Laboratories, 770 Sumneytown Pike, West Point, PA 19486, USA
Antimicrob Agents Chemother 54:4812-24. 2010..Thus, the interactions between NNRTIs and the residues in the NNRTIBPs of different subtypes may not be identical, leading to distinct mutation pathways during resistance selection in cell culture... - Structural basis for the inhibition of RNase H activity of HIV-1 reverse transcriptase by RNase H active site-directed inhibitorsHua Poo Su
Department of Global Structural Biology, Merck Research Laboratories, West Point, Pennsylvania 19486, USA
J Virol 84:7625-33. 2010..These structures provide a means for structurally guided design of novel RNase H inhibitors... - SAR of tertiary carbinamine derived BACE1 inhibitors: role of aspartate ligand amine pKa in enzyme inhibitionHemaka A Rajapakse
Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA
Bioorg Med Chem Lett 20:1885-9. 2010..The potency of compounds as inhibitors of Alphabeta production in a cell culture assay correlated much better with BACE1 enzyme potency measured at pH 7.5 than at pH 4.5... - Assessment of the susceptibility of mutant HIV-1 to antiviral agentsYing Jie Wang
Department of Antiviral Research, Merck Research Laboratories, West Point, PA 19486, USA
J Virol Methods 165:230-7. 2010.... - Integramides A and B, two novel non-ribosomal linear peptides containing nine C(alpha)-methyl amino acids produced by fungal fermentations that are inhibitors of HIV-1 integraseSheo B Singh
Merck Research Laboratories, Rahway, New Jersey 07065, and West Point, Pennsylvania 19486, USA
Org Lett 4:1431-4. 2002..Integramides A and B inhibited the coupled reaction of HIV-1 integrase with IC50 values of 17 and 10 microM, respectively... - Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitorMing Tain Lai
Department of Antiviral Research, Merck Research Laboratories, 770 Sumneytown Pike, West Point, PA 19486, USA
Antimicrob Agents Chemother 53:2424-31. 2009..Taken together, these in vitro data show that MK-4965 possesses the desired properties for further development as a new NNRTI for the treatment of HIV-1 infection... - Scintillation proximity assays for mechanistic and pharmacological analyses of HIV-1 integrationJay A Grobler
Department of Antiviral Research, Merck Research Laboratories, WP26A 3000, 770 Sumneytown Pike, P O Box 4, West Point, PA 19486, USA
Methods 47:249-53. 2009..Assembled complexes can be used in high-throughput DNA strand transfer assays if radio labeled target DNA is employed or in integrase binding assays using a suitable radioligand... - PD-1 blockade in rhesus macaques: impact on chronic infection and prophylactic vaccinationAdam C Finnefrock
Vaccine Basic Research, Merck Research Laboratories, West Point, PA 19486, USA
J Immunol 182:980-7. 2009..05) increase in the peak percentage of T cells specific for the CM9 Gag epitope. These new results on PD-1 blockade in nonhuman primates point to a broader role for PD-1 immunomodulation and to potential applications in humans... - Potent and selective HIV-1 ribonuclease H inhibitors based on a 1-hydroxy-1,8-naphthyridin-2(1H)-one scaffoldPeter D Williams
Department of Medicinal Chemistry, Merck and Co, Inc, West Point, PA 19486, USA
Bioorg Med Chem Lett 20:6754-7. 2010..19 ?M) with a modest window with respect to cytotoxicity (CC(50)=3.3 ?M)... - HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitroJay A Grobler
Department of Antiviral Research, Merck Research Laboratories, West Point, Pennsylvania 19486, USA
J Biol Chem 282:8005-10. 2007..The data presented here suggest that specific inhibition of plus-strand initiation may be an important mechanism by which NNRTIs block HIV-1 replication... - A 7-deaza-adenosine analog is a potent and selective inhibitor of hepatitis C virus replication with excellent pharmacokinetic propertiesDavid B Olsen
Department of Biological Chemistry, Merck Research Laboratories, West Point, Pennsylvania 19486, USA
Antimicrob Agents Chemother 48:3944-53. 2004..Taken together, these data demonstrate that 7-deaza-2'-C-methyl-adenosine is an attractive candidate for further investigation as a potential treatment for HCV infection... - Structure, stereochemistry, and biological activity of integramycin, a novel hexacyclic natural product produced by Actinoplanes sp. that inhibits HIV-1 integraseSheo B Singh
Merck Research Laboratories, Rahway, New Jersey 07065, USA
Org Lett 4:1123-6. 2002..The isolation, structure elucidation, stereochemistry, conformation, and biological activity has been described... - HIV resistance to the fusion inhibitor enfuvirtide: mechanisms and clinical implicationsMichael D Miller
Department of Biological Chemistry, Merck Research Laboratories, P O Box 4, WP16 101, West Point, PA 19486, USA
Drug Resist Updat 7:89-95. 2004..Many aspects of the complexities observed in ENF resistance are likely to be relevant for other classes of HIV entry inhibitors currently in development... - Isolation, structure, and HIV-1-integrase inhibitory activity of structurally diverse fungal metabolitesSheo B Singh
Natural Products Chemistry, Merck Research Laboratories, P O Box 2000, Rahway, New Jersey 07065, USA
J Ind Microbiol Biotechnol 30:721-31. 2003..5-120 micro M. The bioassay-directed isolation, structure elucidation, and HIV-1 inhibitory activity of these compounds are described... - Chemistry and structure-activity relationship of HIV-1 integrase inhibitor integracide B and related natural productsSheo B Singh
Merck Research Laboratories, P O Box 2000, Rahway, New Jersey 07065, USA
J Nat Prod 66:1338-44. 2003..These compounds showed HIV-1 integrase activity with IC(50) values in the range 4.8-15 muM and exhibited antiviral activity in a viral spread assay, but with only a small or no therapeutic window... - Beta-secretase cleavage at amino acid residue 34 in the amyloid beta peptide is dependent upon gamma-secretase activityXiao Ping Shi
Department of Biological Chemistry, Merck Research Laboratories, West Point, Pennsylvania 19486, USA
J Biol Chem 278:21286-94. 2003..Our data thus suggest that gamma-secretase cleavage of CT99 is a prerequisite for BACE-mediated processing at Abeta-34 site. Therefore, BACE and gamma-secretase activity can be mutually dependent... - Four novel bis-(naphtho-gamma-pyrones) isolated from Fusarium species as inhibitors of HIV-1 integraseSheo B Singh
Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA
Bioorg Med Chem Lett 13:713-7. 2003..The discovery, structure elucidation, chemical modification and the structure-activity relationship of these compounds are described... - Integracides: tetracyclic triterpenoid inhibitors of HIV-1 integrase produced by Fusarium spSheo B Singh
Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA
Bioorg Med Chem 11:1577-82. 2003..The discovery, structure elucidation including single crystal X-ray structure and HIV-1 inhibitory activity of these compounds are described... - Design and synthesis of 8-hydroxy-[1,6]naphthyridines as novel inhibitors of HIV-1 integrase in vitro and in infected cellsLinghang Zhuang
Departments of Medicinal Chemistry, Antiviral Research, and Pharmacology, Merck Research Laboratories, West Point, Pennsylvania 19486, USA
J Med Chem 46:453-6. 2003..5 microM and shows a good pharmacokinetic profile when dosed orally to rats. The antiviral activity of 7 and its effect on integration were confirmed using viruses with specific integrase mutations... - Inhibition of HIV-1 ribonuclease H by a novel diketo acid, 4-[5-(benzoylamino)thien-2-yl]-2,4-dioxobutanoic acidCathryn A Shaw-Reid
Department of Biological Chemistry, Merck Research Laboratories, West Point, Pennsylvania 19486 0004, USA
J Biol Chem 278:2777-80. 2003.... - Novel mutations introduced at the beta-site of amyloid beta protein precursor enhance the production of amyloid beta peptide by BACE1 in vitro and in cellsXiao Ping Shi
Department of Biological Chemistry, Merck Research Laboratories, West Point, PA 19486, USA
J Alzheimers Dis 7:139-48; discussion 173-80. 2005..Our data indicates that the "NFEV" mutant is not only an enhanced substrate for BACE1 in vitro, but also a specific substrate for BACE1 in cells... - Discovery of oxadiazoyl tertiary carbinamine inhibitors of beta-secretase (BACE-1)Hemaka A Rajapakse
Department of Medicinal Chemistry, Merck Research Laboratories, P O Box 4, West Point, Pennsylvania 19486, USA
J Med Chem 49:7270-3. 2006..Optimization of this series provided inhibitors with intrinsic and functional potency comparable to evolved transition state isostere derived inhibitors of BACE-1... - A series of 5-aminosubstituted 4-fluorobenzyl-8-hydroxy-[1,6]naphthyridine-7-carboxamide HIV-1 integrase inhibitorsJames P Guare
Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA
Bioorg Med Chem Lett 16:2900-4. 2006..This compound was demonstrated to be efficacious against replication of simian-human immunodeficiency virus (SHIV) 89.6P in infected rhesus macaques... - A series of 5-(5,6)-dihydrouracil substituted 8-hydroxy-[1,6]naphthyridine-7-carboxylic acid 4-fluorobenzylamide inhibitors of HIV-1 integrase and viral replication in cellsMark W Embrey
Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA
Bioorg Med Chem Lett 15:4550-4. 2005..Compound 11 is a 150-fold more potent antiviral agent than 1, with a CIC(95) of 40 nM in the presence of human serum. It displays good pharmacokinetics when dosed in rats and dogs... - Design, synthesis, and SAR of macrocyclic tertiary carbinamine BACE-1 inhibitorsStacey R Lindsley
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 4, West Point, PA 19486, USA
Bioorg Med Chem Lett 17:4057-61. 2007..These macrocyclic inhibitors, some of which incorporate novel P2 substituents, display a 2- to 100-fold increase in potency relative to the previously described acyclic analogs while affording greater stability... - Discovery of human CCR5 antagonists containing hydantoins for the treatment of HIV-1 infectionD Kim
Department of Medicinal Chemistry, Merck Research Laboratories, RY 121 240, PO Box 2000, Rahway, NJ 07065, USA
Bioorg Med Chem Lett 11:3099-102. 2001..A series of hydantoin derivatives has been discovered as highly potent nonpeptide antagonists for the human CCR5 receptor. The synthesis, SAR, and biological profiles of this class of antagonists are described... - Altering expression levels of human immunodeficiency virus type 1 gp120-gp41 affects efficiency but not kinetics of cell-cell fusionJanet E Lineberger
Department of Biological Chemistry, Merck Research Laboratories, West Point, Pennsylvania 19486, USA
J Virol 76:3522-33. 2002..Furthermore, the probability of reaching this threshold is governed, in part, by the surface density of gp120/gp41... - Genome-scale RNAi screen for host factors required for HIV replicationHonglin Zhou
Department of Virus and Cell Biology, Merck and Co, Inc, West Point, PA 19486, USA
Cell Host Microbe 4:495-504. 2008..This study highlights both the power and shortcomings of large scale loss-of-function screens in discovering host-pathogen interactions... - A genotype 2b NS5B polymerase with novel substitutions supports replication of a chimeric HCV 1b:2b replicon containing a genotype 1b NS3-5A backgroundDonald J Graham
Department of Antiviral Research, Merck Research Laboratories, P.O. Box 4, West Point, PA 19486, USA
Antiviral Res 69:24-30. 2006.... - Potential new therapies for the treatment of HIV-1 infectionJon H Condra
Merck Research Laboratories, West Point, Pennsylvania 19486, USA
Annu Rev Med 53:541-55. 2002..This brief review describes the current state of this search as well as potentially novel viral targets for chemotherapeutic intervention... - Purification of untagged HIV-1 reverse transcriptase by affinity chromatographyMeiqing Lu
Department of Antiviral Research, Merck Research Laboratories, West Point, PA 19486, USA
Protein Expr Purif 71:231-9. 2010..Untagged RT was released from the column by reductive cleavage of the intein by DTT. These two methods significantly shorten the time required to purify untagged WT and mutant RTs... - Characterization of resistance to non-obligate chain-terminating ribonucleoside analogs that inhibit hepatitis C virus replication in vitroGiovanni Migliaccio
Department of Biochemistry, Istituto di Ricerche di Biologia Molecolare P. Angeletti (IRBM, 00040 Pomezia, Italy
J Biol Chem 278:49164-70. 2003.... - Dissecting Tn5 transposition using HIV-1 integrase diketoacid inhibitorsAgata Czyz
Department of Biochemistry, University of Wisconsin, 433 Babcock Drive, Madison, Wisconsin 53706, USA
Biochemistry 46:10776-89. 2007..Thus, DKA inhibitors will provide an important set of tools to investigate the mechanism of action of transposases and integrases... - Antiretroviral therapy with the integrase inhibitor raltegravir alters decay kinetics of HIV, significantly reducing the second phaseJohn M Murray
National Centre in HIV Epidemiology and Clinical Research, Sydney, NSW 2052, Australia
AIDS 21:2315-21. 2007..To date, there have been no reports investigating the potential for differential effects on viral dynamics with integrase inhibitors relative to current antiretroviral drugs... - Raltegravir with optimized background therapy for resistant HIV-1 infectionRoy T Steigbigel
State University of New York at Stony Brook, Stony Brook, USA
N Engl J Med 359:339-54. 2008..Raltegravir (MK-0518) is an inhibitor of human immunodeficiency virus type 1 (HIV-1) integrase active against HIV-1 susceptible or resistant to older antiretroviral drugs... - Subgroup and resistance analyses of raltegravir for resistant HIV-1 infectionDavid A Cooper
National Centre in HIV Epidemiology and Clinical Research, University of New South Wales, Sydney
N Engl J Med 359:355-65. 2008.... - c-Myc and Sp1 contribute to proviral latency by recruiting histone deacetylase 1 to the human immunodeficiency virus type 1 promoterGuochun Jiang
Department of Medicine, University of North Carolina at Chapel Hill, 3302 Michael Hooker Research Ctr, Chapel Hill, NC 27599 7435, USA
J Virol 81:10914-23. 2007..These results expand the understanding of mechanisms that recruit HDAC and maintain the latency of HIV-1, suggesting novel therapeutic approaches against latent proviral HIV infection...