Identification of mechanistically distinct inhibitors of HIV-1 reverse transcriptase through fragment screening.

scientific article published on 18 May 2015

Identification of mechanistically distinct inhibitors of HIV-1 reverse transcriptase through fragment screening. is …
instance of (P31):
scholarly articleQ13442814

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P819ADS bibcode2015PNAS..112.6979L
P356DOI10.1073/PNAS.1423900112
P932PMC publication ID4460473
P698PubMed publication ID26038551

P50authorDavid K. ChalmersQ43296593
Gilda TachedjianQ57006431
Stephen J HeadeyQ73161340
Nicolas Sluis-CremerQ113121065
P2093author name stringAdam Johnson
Jamie S Simpson
Catherine F Latham
Kelly D Huber
Jennifer La
David Tyssen
Ricky N Tinetti
P2860cites workMurine leukemia virus reverse transcriptase: structural comparison with HIV-1 reverse transcriptaseQ24647519
Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activityQ24652600
Crystal engineering of HIV-1 reverse transcriptase for structure-based drug designQ27651402
Crystal structure of HIV-1 reverse transcriptase bound to a non-nucleoside inhibitor with a novel mechanism of actionQ27659605
Detecting Allosteric Sites of HIV-1 Reverse Transcriptase by X-ray Crystallographic Fragment ScreeningQ27675974
Integrated biophysical approach to fragment screening and validation for fragment-based lead discoveryQ27679154
Parallel screening of low molecular weight fragment libraries: do differences in methodology affect hit identification?Q27683344
N348I in the connection domain of HIV-1 reverse transcriptase confers zidovudine and nevirapine resistanceQ28471689
Novel high-throughput screen identifies an HIV-1 reverse transcriptase inhibitor with a unique mechanism of actionQ28829256
Ligand efficiency: a useful metric for lead selectionQ29617403
The determination of enzyme inhibitor constantsQ29618526
A fluorescence-based high-throughput screening assay for inhibitors of human immunodeficiency virus-1 reverse transcriptase-associated ribonuclease H activityQ33196450
Identification of a novel scaffold for allosteric inhibition of wild type and drug resistant HIV-1 reverse transcriptase by fragment library screening.Q33786075
Antiretroviral therapy in the clinicQ33877347
Identification of alternative binding sites for inhibitors of HIV-1 ribonuclease H through comparative analysis of virtual enrichment studiesQ33945786
A ‘Rule of Three’ for fragment-based lead discovery?Q33973131
Mechanism of allosteric inhibition of HIV-1 reverse transcriptase revealed by single-molecule and ensemble fluorescenceQ34313002
Fragment screening by weak affinity chromatography: comparison with established techniques for screening against HSP90.Q34353935
Identification and characterization of a novel HIV-1 nucleotide-competing reverse transcriptase inhibitor seriesQ34643481
Indolopyridones inhibit human immunodeficiency virus reverse transcriptase with a novel mechanism of actionQ35185934
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Oral antiretroviral drugs as public health tools for HIV prevention: global implications for adherence, drug resistance, and the success of HIV treatment programsQ37003938
NMR methods in fragment screening: theory and a comparison with other biophysical techniquesQ37588998
Aptamer displacement identifies alternative small-molecule target sites that escape viral resistanceQ38299698
Novel mechanism of inhibition of HIV-1 reverse transcriptase by a new non-nucleoside analog, KM-1.Q38339368
2014 Update of the drug resistance mutations in HIV-1Q39498339
Inhibition of the ribonuclease H and DNA polymerase activities of HIV-1 reverse transcriptase by N-(4-tert-butylbenzoyl)-2-hydroxy-1-naphthaldehyde hydrazoneQ41120477
HIV-1 Reverse Transcriptase Still Remains a New Drug Target: Structure, Function, Classical Inhibitors, and New Inhibitors with Innovative Mechanisms of Actions.Q41879018
Selective and synergistic inhibition of human immunodeficiency virus type 1 reverse transcriptase by a non-nucleoside inhibitor, MKC-442Q42278294
Efavirenz accelerates HIV-1 reverse transcriptase ribonuclease H cleavage, leading to diminished zidovudine excisionQ46892314
Collective motions in HIV-1 reverse transcriptase: examination of flexibility and enzyme function.Q47624236
Thermodynamics of HIV-1 reverse transcriptase in action elucidates the mechanism of action of non-nucleoside inhibitors.Q50931641
Ligand efficiency indices as guideposts for drug discovery.Q55040766
PAINS: Relevance to Tool Compound Discovery and Fragment-Based ScreeningQ58854342
Discovery of Non-Nucleoside Inhibitors of HIV-1 Reverse Transcriptase Competing with the Nucleotide SubstrateQ60197493
P433issue22
P407language of work or nameEnglishQ1860
P304page(s)6979-6984
P577publication date2015-05-18
P1433published inProceedings of the National Academy of Sciences of the United States of AmericaQ1146531
P1476titleIdentification of mechanistically distinct inhibitors of HIV-1 reverse transcriptase through fragment screening
P478volume112

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cites work (P2860)
Q38587368Fragment-based approaches to anti-HIV drug discovery: state of the art and future opportunities
Q40506281Identification and characterization of antibacterial compound(s) of cockroaches (Periplaneta americana).
Q36262959Identification of allosteric binding sites for PI3Kα oncogenic mutant specific inhibitor design
Q47563456Penicillixanthone A, a marine-derived dual-coreceptor antagonist as anti-HIV-1 agent

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