Search Results - "Himmel, Daniel M"
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Non-Nucleoside Reverse Transcriptase Inhibitors Join Forces with Integrase Inhibitors to Combat HIV
Published in Pharmaceuticals (Basel, Switzerland) (11-06-2020)“…In the treatment of acquired immune deficiency syndrome (AIDS), the diarylpyrimidine (DAPY) analogs etravirine (ETR) and rilpivirine (RPV) have been widely…”
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2
Structure and Function of HIV-1 Reverse Transcriptase: Molecular Mechanisms of Polymerization and Inhibition
Published in Journal of molecular biology (23-01-2009)“…The rapid replication of HIV-1 and the errors made during viral replication cause the virus to evolve rapidly in patients, making the problems of vaccine…”
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3
Identification of Alternative Binding Sites for Inhibitors of HIV-1 Ribonuclease H Through Comparative Analysis of Virtual Enrichment Studies
Published in Journal of chemical information and modeling (22-08-2011)“…The ribonuclease H (RNase H) domain on the p66 monomer of HIV-1 reverse transcriptase enzyme has become a target for inhibition. The active site is one…”
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4
The On–Off Switch in Regulated Myosins: Different Triggers but Related Mechanisms
Published in Journal of molecular biology (04-12-2009)“…In regulated myosin, motor and enzymatic activities are toggled between the on-state and off-state by a switch located on its lever arm domain, here called the…”
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Myosin Subfragment 1 Structures Reveal a Partially Bound Nucleotide and a Complex Salt Bridge That Helps Couple Nucleotide and Actin Binding
Published in Proceedings of the National Academy of Sciences - PNAS (15-06-2004)“…Structural studies of myosin have induced some of the conformational changes that occur in this protein during the contractile cycle, and we have now observed…”
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Exploring structural variability in X-ray crystallographic models using protein local optimization by torsion-angle sampling
Published in Acta crystallographica. Section D, Biological crystallography. (01-04-2008)“…Modeling structural variability is critical for understanding protein function and for modeling reliable targets for in silico docking experiments. Because of…”
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Structure of HIV-1 Reverse Transcriptase with the Inhibitor β-Thujaplicinol Bound at the RNase H Active Site
Published in Structure (London) (09-12-2009)“…Novel inhibitors are needed to counteract the rapid emergence of drug-resistant HIV variants. HIV-1 reverse transcriptase (RT) has both DNA polymerase and…”
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8
Structure of a Dihydroxycoumarin Active-Site Inhibitor in Complex with the RNase H Domain of HIV-1 Reverse Transcriptase and Structure–Activity Analysis of Inhibitor Analogs
Published in Journal of molecular biology (15-07-2014)“…Human immunodeficiency virus (HIV) encodes four essential enzymes: protease, integrase, reverse transcriptase (RT)-associated DNA polymerase, and RT-associated…”
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Synthesis, Activity, and Structural Analysis of Novel α-Hydroxytropolone Inhibitors of Human Immunodeficiency Virus Reverse Transcriptase-Associated Ribonuclease H
Published in Journal of medicinal chemistry (14-07-2011)“…The α-hydroxytroplone, manicol (5,7-dihydroxy-2-isopropenyl-9-methyl-1,2,3,4-tetrahydro-benzocyclohepten-6-one), potently and specifically inhibits…”
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10
Rigor-like Structures from Muscle Myosins Reveal Key Mechanical Elements in the Transduction Pathways of This Allosteric Motor
Published in Structure (London) (01-05-2007)“…Unlike processive cellular motors such as myosin V, whose structure has recently been determined in a “rigor-like” conformation, myosin II from contracting…”
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HIV-1 Reverse Transcriptase Structure with RNase H Inhibitor Dihydroxy Benzoyl Naphthyl Hydrazone Bound at a Novel Site
Published in ACS chemical biology (20-12-2006)“…The rapid emergence of drug-resistant variants of human immunodeficiency virus, type 1 (HIV-1), has limited the efficacy of anti-acquired immune deficiency…”
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12
Crystal Structures for HIV-1 Reverse Transcriptase in Complexes with Three Pyridinone Derivatives: A New Class of Non-Nucleoside Inhibitors Effective against a Broad Range of Drug-Resistant Strains
Published in Journal of medicinal chemistry (01-12-2005)“…In the treatment of AIDS, the efficacy of all drugs, including non-nucleoside inhibitors (NNRTIs) of HIV-1 reverse transcriptase (RT), has been limited by the…”
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Crystal Structure of Scallop Myosin S1 in the Pre-Power Stroke State to 2.6 Å Resolution: Flexibility and Function in the Head
Published in Structure (London) (01-12-2003)“…We have extended the X-ray structure determination of the complete scallop myosin head in the pre-power stroke state to 2.6 Å resolution, allowing an atomic…”
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14
Crystal engineering of HIV-1 reverse transcriptase for structure-based drug design
Published in Nucleic acids research (01-09-2008)“…HIV-1 reverse transcriptase (RT) is a primary target for anti-AIDS drugs. Structures of HIV-1 RT, usually determined at ~2.5-3.0 Å resolution, are important…”
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4-Benzyl and 4-Benzoyl-3-dimethylaminopyridin-2(1H)-ones: In Vitro Evaluation of New C-3-Amino-Substituted and C-5,6-Alkyl-Substituted Analogues against Clinically Important HIV Mutant Strains
Published in Journal of medicinal chemistry (24-03-2005)“…In a program to optimize the anti-HIV activity of the 4-benzyl and 4-benzoyl-3-dimethylaminopyridinones 9 and 10, lead compounds in a new class of highly…”
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16
Introducing Our Authors
Published in ACS chemical biology (15-12-2006)Get full text
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Crystal Structure of Scallop Myosin S1 in the Pre-Power Stroke State to 2.6 Å Resolution
Published in Structure (London) (01-12-2003)Get full text
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Structure of HIV-1 Reverse Transcriptase with the Inhibitor b-Thujaplicinol Bound at the RNase H Active Site
Published in Structure (London) (09-12-2009)“…Novel inhibitors are needed to counteract the rapid emergence of drug-resistant HIV variants. HIV-1 reverse transcriptase (RT) has both DNA polymerase and…”
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