Related ArticlesApplication of Site-Specific Spin Labeling for NMR Detecting Inhibitor-Induced Conformational Change of HIV-1 Reverse Transcriptase.
ChemMedChem. 2016 Jan 25;
Authors: Seetaha S, Yagi-Utsumi M, Yamaguchi T, Ishii K, Hannongbua S, Choowongkomon K, Kato K
Abstract
Paramagnetism-assisted nuclear magnetic resonance (NMR) techniques can provide long-range structural information complemented with local information derived from chemical-shift perturbation and nuclear Overhauser effect data. Here, we address the application of paramagnetic relaxation enhancement (PRE) to detect inhibitor-induced conformational change of a drug target protein using human immunodeficiency virus type 1 reverse transcriptase (HIV-1 RT) as a model protein. Using a site-specific spin-labeled HIV-1 RT mutant with selective (13) C labeling, conformation-dependent PREs were successfully observed reflecting the stabilization of an open conformation of this enzyme caused by inhibitor binding. This study demonstrates that the paramagnetism-assisted NMR approach offers an alternative strategy in protein-based drug screening to identify allosteric inhibitors of a target protein.
PMID: 26804978 [PubMed - as supplied by publisher]
[NMR paper] NMR assignments of the N-terminal domain of Ogataea polymorpha telomerase reverse transcriptase.
NMR assignments of the N-terminal domain of Ogataea polymorpha telomerase reverse transcriptase.
Related Articles NMR assignments of the N-terminal domain of Ogataea polymorpha telomerase reverse transcriptase.
Biomol NMR Assign. 2015 Dec 31;
Authors: Polshakov VI, Petrova OA, Parfenova YY, Efimov SV, Klochkov VV, Zvereva MI, Dontsova OA
Abstract
Telomerase is a ribonucleoprotein enzyme that adds telomeric DNA fragments to the ends of chromosomes. This enzyme is the focus of substantial attention, both because its structure and...
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[NMR paper] Ligand-induced conformational change of Plasmodium falciparum AMA1 detected using (19)F NMR.
Ligand-induced conformational change of Plasmodium falciparum AMA1 detected using (19)F NMR.
Related Articles Ligand-induced conformational change of Plasmodium falciparum AMA1 detected using (19)F NMR.
J Med Chem. 2014 Jul 28;
Authors: Ge X, MacRaild CA, Devine S, Debono CO, Wang G, Scammells PJ, Scanlon MJ, Anders RF, Foley M, Norton RS
Abstract
We established an efficient means of probing ligand-induced conformational change in the malaria drug target AMA1 using 19F NMR. AMA1 was labeled with 5-fluorotryptophan (5F-Trp) and...
NMR analysis reveals 17?-estradiol induced conformational change in ER? ligand binding domain expressed in E. coli.
NMR analysis reveals 17?-estradiol induced conformational change in ER? ligand binding domain expressed in E. coli.
NMR analysis reveals 17?-estradiol induced conformational change in ER? ligand binding domain expressed in E. coli.
Mol Biol Rep. 2010 Dec 12;
Authors: Paramanik V, Thakur MK
Nuclear magnetic resonance (NMR) spectroscopy is a useful biophysical technique to study the ligand-protein interaction. In this report, we have used bacterially produced ER? and its domains for studying the functional analysis of ligand-protein interaction....
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[NMR paper] NMR structure of free RGS4 reveals an induced conformational change upon binding Galp
NMR structure of free RGS4 reveals an induced conformational change upon binding Galpha.
Related Articles NMR structure of free RGS4 reveals an induced conformational change upon binding Galpha.
Biochemistry. 2000 Jun 20;39(24):7063-73
Authors: Moy FJ, Chanda PK, Cockett MI, Edris W, Jones PG, Mason K, Semus S, Powers R
Heterotrimeric guanine nucleotide-binding proteins (G-proteins) are transducers in many cellular transmembrane signaling systems where regulators of G-protein signaling (RGS) act as attenuators of the G-protein signal cascade...
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11-18-2010 09:15 PM
[NMR paper] Irreversible conformational change of bacterio-opsin induced by binding of retinal du
Irreversible conformational change of bacterio-opsin induced by binding of retinal during its reconstitution to bacteriorhodopsin, as studied by (13)C NMR.
Related Articles Irreversible conformational change of bacterio-opsin induced by binding of retinal during its reconstitution to bacteriorhodopsin, as studied by (13)C NMR.
J Biochem. 2000 May;127(5):861-9
Authors: Yamaguchi S, Tuzi S, Tanio M, Naito A, Lanyi JK, Needleman R, Saitô H
We compared (13)C NMR spectra of Ala- and Val-labeled bacterio-opsin (bO), produced either by bleaching bR...
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NMR evidence of GM1-induced conformational change of substance P using isotropic bice
NMR evidence of GM1-induced conformational change of substance P using isotropic bicelles.
Related Articles NMR evidence of GM1-induced conformational change of substance P using isotropic bicelles.
Biochim Biophys Acta. 2010 Oct 8;
Authors: Gayen A, Goswami SK, Mukhopadhyay C
Substance P (SP) is one of the target neurotransmitters associated with diseases related to chronic inflammation, pain and depression. The selective receptor for SP, NK(1)R is located in the heterogeneous microdomains or caveolaes in membrane. Gangliosides, specifically...
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[NMR paper] Application of amino acid type-specific 1H- and 14N-labeling in a 2H-, 15N-labeled ba
Application of amino acid type-specific 1H- and 14N-labeling in a 2H-, 15N-labeled background to a 47 kDa homodimer: potential for NMR structure determination of large proteins.
Related Articles Application of amino acid type-specific 1H- and 14N-labeling in a 2H-, 15N-labeled background to a 47 kDa homodimer: potential for NMR structure determination of large proteins.
J Biomol NMR. 1999 May;14(1):79-83
Authors: Kelly MJ, Krieger C, Ball LJ, Yu Y, Richter G, Schmieder P, Bacher A, Oschkinat H
NMR investigations of larger macromolecules (> 20...
Application of Site-Specific Spin Labeling for NMR Detecting Inhibitor-Induced Conformational Change of HIV-1 Reverse Transcriptase.
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