Bombesin and substance P analogues differentially regulate G-protein coupling to the bombesin receptor. Direct evidence for biased agonism.
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International Union of Pharmacology. LXVIII. Mammalian bombesin receptors: nomenclature, distribution, pharmacology, signaling, and functions in normal and disease statesIncreased gastrin-releasing peptide (GRP) receptor expression in tumour cells confers sensitivity to [Arg6,D-Trp7,9,NmePhe8]-substance P (6-11)-induced growth inhibitionSeven transmembrane receptors as shapeshifting proteins: the impact of allosteric modulation and functional selectivity on new drug discovery.Pharmacology of putative selective hBRS-3 receptor agonists for human bombesin receptors (BnR): affinities, potencies and selectivity in multiple native and BnR transfected cells.Bradykinin antagonist dimer, CU201, inhibits the growth of human lung cancer cell lines by a "biased agonist" mechanism.Exploring a role for heteromerization in GPCR signalling specificity.Sensitization of pulmonary chemosensitive neurons by bombesin-like peptides in ratsAntagonist, partial agonist and antiproliferative actions of B-9870 (CU201) as a function of the expression and density of the bradykinin B1 and B2 receptorsTherapeutic potential of β-arrestin- and G protein-biased agonists.Pharmacological onomastics: what's in a name?The origins of diversity and specificity in g protein-coupled receptor signalingProinflammatory tachykinins that signal through the neurokinin 1 receptor promote survival of dendritic cells and potent cellular immunity.Targeting V1A-vasopressin receptors with [Arg6, D-Trp7,9, NmePhe8]-substance P (6-11) identifies a strategy to develop novel anti-cancer therapies.Allosteric modulators of g protein-coupled receptors: future therapeutics for complex physiological disorders.A perspective on more effective GPCR-targeted drug discovery efforts.Achieving signalling selectivity of ligands for the corticotropin-releasing factor type 1 receptor by modifying the agonist's signalling domain.Expression of V1A and GRP receptors leads to cellular transformation and increased sensitivity to substance-P analogue-induced growth inhibition.The oxytocin receptor antagonist atosiban inhibits cell growth via a "biased agonist" mechanism.Interrogating 7TM receptors: does texture in the question yield greater texture in the answer?Collateral efficacy as a pharmacological problem applied to new drug discovery.
P2860
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P2860
Bombesin and substance P analogues differentially regulate G-protein coupling to the bombesin receptor. Direct evidence for biased agonism.
description
2001 nî lūn-bûn
@nan
2001年の論文
@ja
2001年論文
@yue
2001年論文
@zh-hant
2001年論文
@zh-hk
2001年論文
@zh-mo
2001年論文
@zh-tw
2001年论文
@wuu
2001年论文
@zh
2001年论文
@zh-cn
name
Bombesin and substance P analo ...... t evidence for biased agonism.
@en
type
label
Bombesin and substance P analo ...... t evidence for biased agonism.
@en
prefLabel
Bombesin and substance P analo ...... t evidence for biased agonism.
@en
P2093
P2860
P356
P1476
Bombesin and substance P analo ...... t evidence for biased agonism.
@en
P2093
P2860
P304
28083-28091
P356
10.1074/JBC.M009772200
P407
P577
2001-04-25T00:00:00Z