Identification of selective agonists and positive allosteric modulators for μ- And δ-opioid receptors from a single high-throughput screen

Journal of Biomolecular Screening

Volumn 19, Issue 9, 2014, Pages 1255-1265

  Burford, Neil T ^a   Wehrman, Tom ^b   Bassoni, Daniel ^b   O'Connell, Jonathan ^c   Banks, Martyn ^a   Zhang, Litao ^a   Alt, Andrew ^a  

^a BRISTOL MYERS SQUIBB   (United States)

^b DiscoveRx Corporation   (United States)

^c FORMA Therapeutics   (United States)

Author keywords

GPCR; high throughput screen; opioid receptor; positive allosteric modulator; arrestin

Indexed keywords

4 [ALPHA (4 ALLYL 2,5 DIMETHYL 1 PIPERAZINYL) 3 METHOXYBENZYL] N,N DIETHYLBENZAMIDE; BETA ARRESTIN; BETA ENDORPHIN; DELTA OPIATE RECEPTOR; DELTA OPIATE RECEPTOR AGONIST; DELTA OPIATE RECEPTOR POSITIVE ALLOSTERIC MODULATOR; DELTORPHIN; DELTORPHIN II; DEXTRO PHENYLALANYLCYSTEINYLTYROSYL DEXTRO TRYPTOPHYLARGINYLTHREONYLPENICILLAMINYLTHREONINAMIDE 2,7 DISULFIDE; ENDOMORPHIN 1; ENKEPHALIN[2 DEXTRO ALANINE 4 METHYLPHENYLALANINE 5 GLYCINE]; G PROTEIN COUPLED RECEPTOR; LEUCINE ENKEPHALIN; MORPHINE; MU OPIATE RECEPTOR; MU OPIATE RECEPTOR AGONIST; MU OPIATE RECEPTOR POSITIVE ALLOSTERIC MODULATOR; N,N DIALLYLTYROSYL 2 METHYLALANYL 2 METHYLALANYLPHENYLALANYLLEUCINE; NALTRINDOLE; OLIGOMER; UNCLASSIFIED DRUG; CYCLIC AMP; FORSKOLIN; NARCOTIC ANALGESIC AGENT; NARCOTIC ANTAGONIST; RETINA S ANTIGEN;

ALLOSTERISM; ANIMAL CELL; ARTICLE; CONTROLLED STUDY; DRUG BINDING SITE; DRUG IDENTIFICATION; DRUG RECEPTOR BINDING; DRUG SCREENING; DRUG SELECTIVITY; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN CELL; IC50; LIGAND BINDING; NONHUMAN; RECEPTOR AFFINITY; RECEPTOR BINDING ASSAY; U2OS CELL LINE; AGONISTS; ANIMAL; CHEMISTRY; CHO CELL LINE; CRICETULUS; DOSE RESPONSE; DRUG EFFECTS; HAMSTER; METABOLISM; PROTEIN MULTIMERIZATION;

ALLOSTERIC REGULATION; ANALGESICS, OPIOID; ANIMALS; ARRESTINS; CHO CELLS; COLFORSIN; CRICETINAE; CRICETULUS; CYCLIC AMP; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG EVALUATION, PRECLINICAL; HIGH-THROUGHPUT SCREENING ASSAYS; HUMANS; NARCOTIC ANTAGONISTS; PROTEIN MULTIMERIZATION; RECEPTORS, OPIOID, DELTA; RECEPTORS, OPIOID, MU;

EID: 84908866820     PISSN: 10870571     EISSN: 1552454X     Source Type: Journal    
DOI: 10.1177/1087057114542975     Document Type: Article

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