Isothermal chemical denaturation to determine binding affinity of small molecules to G-protein coupled receptors

Analytical Biochemistry

Volumn 473, Issue , 2015, Pages 41-45

  Ross, Patrick ^a   Weihofen, Wilhelm ^b   Siu, Fai ^b   Xie, Amy ^b   Katakia, Hetal ^b   Wright, S Kirk ^b   Hunt, Ian ^b   Brown, Richard K ^a   Freire, Ernesto ^a,c  

^a AVIA Biosystems   (United States)

^b NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH   (United States)

^c JOHNS HOPKINS UNIVERSITY   (United States)

Author keywords

Binding affinity determination; Binding thermodynamics; Chemical denaturation; GPCR

Indexed keywords

BINDING ENERGY; DENATURATION; DRUG DELIVERY; ISOTHERMS; LIGANDS; MOLECULES; SURFACE PLASMON RESONANCE;

BINDING AFFINITIES; BINDING THERMODYNAMICS; BIOPHYSICAL METHODS; BIOPHYSICAL TECHNIQUES; CHEMICAL DENATURATION; G PROTEIN COUPLED RECEPTORS; GPCR; INTEGRAL MEMBRANE PROTEINS;

PROTEINS;

2 [4 (2 CARBOXYETHYL)PHENETHYLAMINO]ADENOSINE 5' (N ETHYLCARBOXAMIDE); 4 [2 [7 AMINO 2 (2 FURYL) 1,2,4 TRIAZOLO[2,3 A][1,3,5]TRIAZIN 5 YLAMINO]ETHYL]PHENOL; 5 AMINO 2 (2 FURYL) 7 (2 PHENYLETHYL)PYRAZOLO[4,3 E][1,2,4]TRIAZOLO[1,5 C]PYRIMIDINE; ADENOSINE A2A RECEPTOR AGONIST; ADENOSINE A2A RECEPTOR ANTAGONIST; ADENOSINE RECEPTOR STIMULATING AGENT; ANR 94; BENALFOCIN; CAFFEINE; G PROTEIN COUPLED RECEPTOR; GUANFACINE; HEMADO; ISTRADEFYLLINE; LUF 5834; MRS 1334; PSB 0777; PSB 1115; SCH 442416; TC G 1004; THEOPHYLLINE; UNCLASSIFIED DRUG; WZ 811; ZK 756326; ADENOSINE A2 RECEPTOR AGONIST; ADENOSINE A2 RECEPTOR ANTAGONIST; ADENOSINE A2A RECEPTOR; GUANIDINE; LIGAND; PROTEIN BINDING;

ARTICLE; BINDING AFFINITY; DISSOCIATION CONSTANT; DRUG RECEPTOR BINDING; IN VITRO STUDY; ISOTHERMAL CHEMICAL DENATURATION; LIGAND BINDING; PRIORITY JOURNAL; PROTEIN DENATURATION; PROTEIN STABILITY; RADIOASSAY; RECEPTOR BINDING; SURFACE PLASMON RESONANCE; BIOPHYSICS; CHEMISTRY; DRUG EFFECTS; METABOLISM; PROCEDURES; TEMPERATURE;

ADENOSINE A2 RECEPTOR AGONISTS; ADENOSINE A2 RECEPTOR ANTAGONISTS; BIOPHYSICS; GUANIDINE; LIGANDS; PROTEIN BINDING; PROTEIN DENATURATION; RECEPTOR, ADENOSINE A2A; TEMPERATURE;

EID: 84961291514     PISSN: 00032697     EISSN: 10960309     Source Type: Journal    
DOI: 10.1016/j.ab.2014.11.019     Document Type: Article

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