P. Felock

发表

Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses.

G. McGaughey, Youwei Yan, M. Lai, 2008, Journal of medicinal chemistry.

The design and synthesis of diaryl ether second generation HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) with enhanced potency versus key clinical mutations.

G. McGaughey, Youwei Yan, M. Lai, 2008, Bioorganic & medicinal chemistry letters.

Design and synthesis of pyridone inhibitors of non-nucleoside reverse transcriptase.

G. McGaughey, Youwei Yan, M. Lai, 2011, Bioorganic & medicinal chemistry letters.

Design and synthesis of conformationally constrained inhibitors of non-nucleoside reverse transcriptase.

G. McGaughey, Youwei Yan, M. Lai, 2011, Journal of medicinal chemistry.

Crystal structure of human rhinovirus serotype 1A (HRV1A).

M S Chapman, M A McKinlay, M. S. Chapman, 1989, Journal of molecular biology.

Conformational change in the floor of the human rhinovirus canyon blocks adsorption to HeLa cell receptors

A. Treasurywala, M. Rossmann, M. Miller, 1989, Journal of virology.

A potent and orally active HIV-1 integrase inhibitor.

Wei Xu, D. Hazuda, Michael D. Miller, 2007, Bioorganic & medicinal chemistry letters.

Biaryl ethers as novel non-nucleoside reverse transcriptase inhibitors with improved potency against key mutant viruses.

Kenneth D Anderson, M. Lai, J. Vacca, 2009, Journal of medicinal chemistry.

Biaryl ethers as potent allosteric inhibitors of reverse transcriptase and its key mutant viruses: aryl substituted pyrazole as a surrogate for the pyrazolopyridine motif.

Kenneth D Anderson, M. Lai, J. Vacca, 2010, Bioorganic & medicinal chemistry letters.

Efficiency and Fidelity of Full-Site Integration Reactions Using Recombinant Simian Immunodeficiency Virus Integrase

D. Grandgenett, M. Witmer, P. Felock, 1999, Journal of Virology.

Four novel bis-(naphtho-gamma-pyrones) isolated from Fusarium species as inhibitors of HIV-1 integrase.

D. Hazuda, K. Silverman, G. Bills, 2003, Bioorganic & medicinal chemistry letters.

Four novel bis-(naphtho-γ-pyrones) isolated from Fusarium species as inhibitors of HIV-1 integrase

D. Hazuda, K. Silverman, G. Bills, 2003 .

Integracides: tetracyclic triterpenoid inhibitors of HIV-1 integrase produced by Fusarium sp.

D. Hazuda, J. Hirshfield, P. Felock, 2003, Bioorganic & medicinal chemistry.

Isolation and Characterization of Novel Human Immunodeficiency Virus Integrase Inhibitors from Fungal Metabolites

F. Bushman, D. Hazuda, C. Farnet, 1999, Antiviral chemistry & chemotherapy.

Equivalent inhibition of half-site and full-site retroviral strand transfer reactions by structurally diverse compounds

D. Hazuda, D. Grandgenett, J. Hastings, 1997, Journal of virology.

The role of manganese in promoting multimerization and assembly of human immunodeficiency virus type 1 integrase as a catalytically active complex on immobilized long terminal repeat substrates

D. Hazuda, C. Blau, J. Hastings, 1996, Journal of virology.

Design and synthesis of substituted 4-oxo-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrazine-2-carboxamides, novel HIV-1 integrase inhibitors.

H. M. Langford, D. Hazuda, W. Schleif, 2008, Bioorganic & medicinal chemistry letters.

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

Mark Embrey, Samson M Jolly, Wei Xu, 2004, Proceedings of the National Academy of Sciences of the United States of America.

HIV-1 integrase inhibitors that compete with the target DNA substrate define a unique strand transfer conformation for integrase.

Amy S. Espeseth, D. Hazuda, A. Espeseth, 2000, Proceedings of the National Academy of Sciences of the United States of America.

Structures of four methyltetrazole-containing antiviral compounds in human rhinovirus serotype 14.

V. Giranda, D. Pevear, P. Felock, 1995, Acta crystallographica. Section D, Biological crystallography.

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

Linghang Zhuang, D. Hazuda, W. Schleif, 2003, Journal of medicinal chemistry.

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

H. M. Langford, D. Hazuda, W. Schleif, 2000, Journal of medicinal chemistry.

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 cells.

D. Hazuda, Jiunn H. Lin, W. Schleif, 2005, Bioorganic & medicinal chemistry letters.

Differential divalent cation requirements uncouple the assembly and catalytic reactions of human immunodeficiency virus type 1 integrase

D. Hazuda, J. Hastings, A. Wolfe, 1997, Journal of virology.

Inhibitors of strand transfer that prevent integration and inhibit HIV-1 replication in cells.

J A Grobler, Amy S. Espeseth, D. Hazuda, 2000, Science.

Discovery of MK-8718, an HIV Protease Inhibitor Containing a Novel Morpholine Aspartate Binding Group.

W. Shipe, H. Su, J. Gesell, 2016, ACS medicinal chemistry letters.

Discovery and synthesis of HIV integrase inhibitors: development of potent and orally bioavailable N-methyl pyrimidones.

Michael Rowley, Cristina Gardelli, Marco Ferrara, 2007, Journal of medicinal chemistry.

Isolation, structure, absolute stereochemistry, and HIV-1 integrase inhibitory activity of integrasone, a novel fungal polyketide.

D. Hazuda, Z. Guan, G. Bills, 2004, Journal of natural products.

Diketo acid inhibitor mechanism and HIV-1 integrase: Implications for metal binding in the active site of phosphotransferase enzymes

Amy S. Espeseth, Amy S Espeseth, D. Hazuda, 2002, Proceedings of the National Academy of Sciences of the United States of America.

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 integrase.

D. Hazuda, Z. Guan, K. Silverman, 2002, Organic letters.

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 I.

O. Genilloud, K. Silverman, B. Heimbuch, 2001, Journal of natural products.

Isolation, Structure, and HIV‐1 Integrase Inhibitory Activity of Xanthoviridicatin E and F, Two Novel Fungal Metabolites Produced by Penicillium chrysogenum.

D. Hazuda, Z. Guan, F. Peláez, 2004 .

Complete Absolute Configuration of Integramide A, a Natural, 16‐mer Peptide Inhibitor of HIV‐1 Integrase, Elucidated by Total Synthesis

D. Hazuda, C. Toniolo, F. Formaggio, 2009, Chembiochem : a European journal of chemical biology.

Assessment of the susceptibility of mutant HIV-1 to antiviral agents.

D. Hazuda, C. Coburn, Kristen L G Jones, 2010, Journal of virological methods.

Integrastatins: structure and HIV-1 integrase inhibitory activities of two novel racemic tetracyclic aromatic heterocycles produced by two fungal species

D. Hazuda, F. Peláez, P. Felock, 2002 .

Structure and absolute stereochemistry of HIV-1 integrase inhibitor integric acid. A novel eremophilane sesquiterpenoid produced by a Xylaria sp.

D. Hazuda, K. Silverman, P. Felock, 1999 .

Monitoring the development of non-nucleoside reverse transcriptase inhibitor-associated resistant HIV-1 using an electrochemiluminescence-based reverse transcriptase polymerase assay.

D. Hazuda, M. Lai, Michael D Miller, 2008, Analytical biochemistry.

Synthesis of 5-(1-H or 1-alkyl-5-oxopyrrolidin-3-yl)-8-hydroxy-[1,6]-naphthyridine-7-carboxamide inhibitors of HIV-1 integrase.

D. Hazuda, W. Schleif, L. Gabryelski, 2008, Bioorganic & medicinal chemistry letters.

Isolation, structure, and HIV-1-integrase inhibitory activity of structurally diverse fungal metabolites

D. Hazuda, Z. Guan, G. Platas, 2003, Journal of Industrial Microbiology and Biotechnology.

X-ray structure of simian immunodeficiency virus integrase containing the core and C-terminal domain (residues 50-293)--an initial glance of the viral DNA binding platform.

D. Hazuda, Youwei Yan, L. Kuo, 2000, Journal of molecular biology.

Distinct Mutation Pathways of Non-Subtype B HIV-1 during In Vitro Resistance Selection with Nonnucleoside Reverse Transcriptase Inhibitors

D. Hazuda, G. McGaughey, Youwei Yan, 2010, Antimicrobial Agents and Chemotherapy.

Structure, stereochemistry, and biological activity of integramycin, a novel hexacyclic natural product produced by Actinoplanes sp. that inhibits HIV-1 integrase.

D. Hazuda, O. Genilloud, K. Silverman, 2002, Organic letters.

Antiviral Activity and In Vitro Mutation Development Pathways of MK-6186, a Novel Nonnucleoside Reverse Transcriptase Inhibitor

D. Hazuda, G. McGaughey, Youwei Yan, 2012, Antimicrobial Agents and Chemotherapy.

Selective and controlled hydrolysis of chloropeptin I. HIV-1 integrase activity of fragments

M. Patane, M. Sardana, P. Felock, 1998 .

Genetic Algorithm Based Method To Design a Primary Screen for Antirhinovirus Agents

Adi Treasurywala, E. P. Jaeger, Daniel C. Pevear, 1995 .

Isolation, structure, and HIV-1 integrase inhibitory activity of Cytosporic acid, a fungal metabolite produced by a Cytospora sp.

D. Hazuda, Z. Guan, P. Felock, 2003, Journal of natural products.

Isolation, structure and HIV-1 integrase inhibitory activity of exophillic acid, a novel fungal metabolite from Exophiala pisciphila.

D. Hazuda, P. Felock, Sheo B. Singh, 2003, The Journal of antibiotics.

Isolation, Structure and HIV‐1 Integrase Inhibitory Activity of Exophillic Acid, a Novel Fungal Metabolite from Exophiala pisciphila.

D. Hazuda, P. Felock, Sheo B. Singh, 2004 .

Discovery, Structure and HIV‐1 Integrase Inhibitory Activities of Integracins, Novel Dimeric Alkyl Aromatics from Cytonaema sp.

D. Hazuda, K. Silverman, F. Peláez, 2002 .

Discovery, structure and HIV-1 integrase inhibitory activities of integracins, novel dimeric alkyl aromatics from Cytonaema sp.

D. Hazuda, K. Silverman, F. Peláez, 2002 .

Chemical and enzymatic modifications of integric acid and HIV-1 integrase inhibitory activity.

D. Hazuda, P. Felock, S. B. Singh, 2000, Bioorganic & medicinal chemistry letters.

Isolation, Structure, and HIV‐1 Integrase Inhibitory Activity of Xanthoviridicatin E and F, Two Novel Fungal Metabolites Produced by Penicillium chrysogenum

D. Hazuda, Z. Guan, F. Peláez, 2003 .

Chemistry and structure-activity relationship of HIV-1 integrase inhibitor integracide B and related natural products.

D. Hazuda, W. Schleif, P. Felock, 2003, Journal of natural products.

Total synthesis, characterization, and conformational analysis of the naturally occurring hexadecapeptide integramide A and a diastereomer.

D. Hazuda, C. Toniolo, F. Formaggio, 2010, Chemistry.

Triple Hyp→Pro replacement in integramide A, a peptaib inhibitor of HIV‐1 integrase: Effect on conformation and bioactivity

D. Hazuda, C. Toniolo, F. Formaggio, 2011, Biopolymers.

A series of 5-aminosubstituted 4-fluorobenzyl-8-hydroxy-[1,6]naphthyridine-7-carboxamide HIV-1 integrase inhibitors.

D. Hazuda, W. Schleif, L. Gabryelski, 2006, Bioorganic & medicinal chemistry letters.

Substituted tetrahydroquinolines as potent allosteric inhibitors of reverse transcriptase and its key mutants.

Kenneth D Anderson, Youwei Yan, M. Lai, 2009, Bioorganic & Medicinal Chemistry Letters.

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 mutants.

D. Hazuda, W. Schleif, L. Gabryelski, 2008, Bioorganic & medicinal chemistry letters.

8-Hydroxy-3,4-dihydropyrrolo[1,2-a]pyrazine-1(2H)-one HIV-1 integrase inhibitors.

D. Hazuda, W. Schleif, L. Gabryelski, 2007, Bioorganic & medicinal chemistry letters.

Dihydroxypyridopyrazine-1,6-dione HIV-1 integrase inhibitors.

D. Hazuda, W. Schleif, L. Gabryelski, 2007, Bioorganic & medicinal chemistry letters.

Design and synthesis of bicyclic pyrimidinones as potent and orally bioavailable HIV-1 integrase inhibitors.

Fabrizio Fiore, Michael Rowley, Cristina Gardelli, 2008, Journal of medicinal chemistry.

Purification, solution properties and crystallization of SIV integrase containing a continuous core and C-terminal domain.

D. Hazuda, L. Kuo, Z. Chen, 1999, Acta crystallographica. Section D, Biological crystallography.