G protein-coupled receptor allosterism and complexing

Pharmacological Reviews

Volumn 54, Issue 2, 2002, Pages 323-374

  Christopoulos, Arthur ^a   Kenakin, Terry ^b  

^a UNIVERSITY OF MELBOURNE   (Australia)

^b GLAXOSMITHKLINE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ACETYLCHOLINE; ALPHA 2A ADRENERGIC RECEPTOR; AMILORIDE DERIVATIVE; ARECOLINE; ATROPINE; BETA 1 ADRENERGIC RECEPTOR; BETHANECHOL; BUPRENORPHINE; CARBACHOL; CELL PROTEIN; CELL SURFACE RECEPTOR; CYCLOHEXYLADENOSINE; DICHLORISOPRENALINE; DOPAMINE 1 RECEPTOR; DOPAMINE 2 RECEPTOR; FURTRETHONIUM; G PROTEIN COUPLED RECEPTOR; GUANINE NUCLEOTIDE BINDING PROTEIN; KAPPA OPIATE RECEPTOR; METHADONE; METHYLFURTRETHONIUM; METHYLSCOPOLAMINE; MU OPIATE RECEPTOR; MUSCARINIC M1 RECEPTOR; MUSCARINIC M2 RECEPTOR; OLIGOMER; RECEPTOR SUBTYPE; SIGMA OPIATE RECEPTOR; UNINDEXED DRUG; ZINC;

ALLOSTERISM; BINDING SITE; COMPLEX FORMATION; CONFORMATIONAL TRANSITION; DRUG BINDING SITE; DRUG CONCENTRATION; DRUG RECEPTOR BINDING; LIGAND BINDING; PRIORITY JOURNAL; RECEPTOR DOWN REGULATION; RECEPTOR OCCUPANCY; REVIEW; SIGNAL TRANSDUCTION;

ALLOSTERIC REGULATION; ALLOSTERIC SITE; BINDING, COMPETITIVE; DRUG DESIGN; GTP-BINDING PROTEINS; HUMANS; MODELS, BIOLOGICAL; RADIOLIGAND ASSAY; RECEPTORS, CELL SURFACE;

EID: 0036258990     PISSN: 00316997     EISSN: None     Source Type: Journal    
DOI: 10.1124/pr.54.2.323     Document Type: Review

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290. Structural implication for receptor oligomerization from functional reconstitution studies of mutant V2 vasopressin receptors
291. Is there a "lock" for all agonist "keys" in 7TM receptors
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294. Potent inhibition of HIV-1 infectivity in macrophages and lymphocytes by a novel CCR5 antagonist
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305. GAP-43 augments G protein-coupled receptor transduction in Xenopus laevis oocytes
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308. Receptor-independent activators of heterotrimeric G-protein signaling pathways
309. A study of the action of picrotoxin on the inhibitory neuromuscular junction of the crayfish
310. Aspirin and sodium salicylate inhibit endothelin ETA receptors by an allosteric type of mechanism
311. Identification of the endophilins (SH3p4/p8/p13) as novel binding partners for the β1-adrenergic receptor
312. Unique allosteric regulation of 5-hydroxytryptamine receptor-mediated signal transduction by oleamide
313. On the analysis of pharmacological experiments in terms of an allosteric receptor model
314. 2 receptors
315. 2 receptors
316. 2 receptors
317. Is the R and R* dichotomy real? Observations of allosteric phenomena on G protein-coupled receptors point to problems in the interpretation of agonist-receptor-G protein interactions
318. Allosteric modulation of muscarinic acetylcholine receptors
319. Cloning and characterization of MUPP1, a novel PDZ domain protein
320. B receptors by 2,6-di-tert-butyl-4-(3-hydroxy-2,2-dimethyl-propyl)-phenol (CGP7930), and its aldehyde analog CGP13501
321. The model of metaffinoid interaction, in Histamine and Antihistamines
322. Mu and delta receptors: Their role in anlalgesia and in the differential effects of opioid peptides on analgesia
323. The structure of α- and β-adrenergic receptors
324. HIV-1 infection through the CCR5 receptor is blocked by receptor dimerization
325. s activation
326. iα 1
327. The use of stimulus-biased assay systems to detect agonist-specific receptor active states: Implications for the trafficking of receptor stimulus by agonists
328. RGS family members: GTPase-activating proteins for heterotrimeric G-protein α-subunits
329. 1-adrenergic receptor function by benzodiazepines: A potential site of allosteric modulation
330. Ligand binding and internal equilibria in proteins
331. Energetics of ligand binding to proteins
332. The cubic ternary complex receptor-occupancy model I. Model description
333. The cubic ternary complex receptor-occupancy model II. Understanding apparent affinity
334. The cubic ternary complex receptor-occupancy model III. Resurrecting efficacy
335. Mutational analysis of muscarinic acetylcholine receptors: Structural basis of ligand/receptor/G protein interactions
336. B receptor
337. 2S dopamine receptor: Evidence for multiple, agonist-specific active conformations
338. 2B-adrenergic receptor subtype
339. 2-dopamine receptor of the anterior pituitary gland
340. Cooperativity manifest in the binding properties of purified cardiac muscarinic receptors
341. The turning wheel: A study in steady states
342. The problem of heme interactions in hemoglobin and the basis for the Bohr effect
343. 1D receptors form homodimers when expressed alone and heterodimers when co-expressed
344. Heteromeric association creates a P2Y-like adenosine receptor
345. μ opioid receptor phosphorylation, desensitization and ligand efficacy
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347. Identification and molecular characterization of m3 muscarinic receptor dimers
348. Anti-HIV agent trichosanthin enhances the capabilities of chemokines to stimulate chemotaxis and G protein activation, and this is mediated through interaction of trichosanthin and chemokine receptors
349. Regulator of G protein signaling proteins: Novel multifunctional drug targets
350. Truncated V2 vasopressin receptors as negative regulators of wild-type V2 receptor function
351. Somatostatin receptor interacting protein defines a novel family of multidomain proteins present in human and rodent brain