Agonist induction and conformational selection during activation of a G-protein-coupled receptor (Q35057345)

6 August 2017

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title

Agonist induction and conformational selection during activation of a G-protein-coupled receptor (English)

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G protein-coupled receptor

6 August 2017

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author name string

László Hunyady

series ordinal

1

1 reference

PubMed ID

12559772

6 August 2017

Georges Vauquelin

series ordinal

2

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PubMed ID

12559772

6 August 2017

Patrick Vanderheyden

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3

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6 August 2017

1 February 2003

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Trends in Pharmacological Sciences

6 August 2017

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6 August 2017

24

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6 August 2017

2

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6 August 2017

81-86

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Uncovering molecular mechanisms involved in activation of G protein-coupled receptors

6 August 2017

1 reference

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Activation of the alpha1b-adrenergic receptor is initiated by disruption of an interhelical salt bridge constraint

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Mutagenesis and modelling of the alpha(1b)-adrenergic receptor highlight the role of the helix 3/helix 6 interface in receptor activation.

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Rhodopsin: insights from recent structural studies.

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Lessons from constitutively active mutants of G protein-coupled receptors

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The active state of the AT1 angiotensin receptor is generated by angiotensin II induction

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Mutation of Asn111 in the third transmembrane domain of the AT1A angiotensin II receptor induces its constitutive activation.

1 reference

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The conformational change responsible for AT1 receptor activation is dependent upon two juxtaposed asparagine residues on transmembrane helices III and VII.

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Identification of a conserved switch residue responsible for selective constitutive activation of the beta2-adrenergic receptor

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Alanine exchanges of polar amino acids in the transmembrane domains of a platelet-activating factor receptor generate both constitutively active and inactive mutants

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Constitutive activation of the human bradykinin B2 receptor induced by mutations in transmembrane helices III and VI.

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A point mutation that confers constitutive activity to CXCR4 reveals that T140 is an inverse agonist and that AMD3100 and ALX40-4C are weak partial agonists

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Constitutively active mutants of rhodopsin

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Interaction of biphenylimidazole and imidazoleacrylic acid nonpeptide antagonists with valine 108 in TM III of the AT1 angiotensin receptor

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Mechanism of constitutive activation of the AT1 receptor: influence of the size of the agonist switch binding residue Asn(111).

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Angiotensin IV is a potent agonist for constitutive active human AT1 receptors. Distinct roles of the N-and C-terminal residues of angiotensin II during AT1 receptor activation

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The docking of Arg2 of angiotensin II with Asp281 of AT1 receptor is essential for full agonism

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G protein-coupled receptors. II. Mechanism of agonist activation.

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The ligand paradox between affinity and efficacy: can you be there and not make a difference?

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Agonist-induced phosphorylation of the angiotensin II (AT(1A)) receptor requires generation of a conformation that is distinct from the inositol phosphate-signaling state

1 reference

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Rhodopsin: structural basis of molecular physiology

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Thyroid-stimulating hormone and thyroid-stimulating hormone receptor structure-function relationships

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Mutational analysis of the interaction of the N- and C-terminal ends of angiotensin II with the rat AT(1A) receptor

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Role of aromaticity of agonist switches of angiotensin II in the activation of the AT1 receptor

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Tetrazole and carboxylate groups of angiotensin receptor antagonists bind to the same subsite by different mechanisms

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Interaction of Phe8 of angiotensin II with Lys199 and His256 of AT1 receptor in agonist activation

1 reference

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The ligand binding site of the angiotensin AT1 receptor.

1 reference

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Amino acids of the third transmembrane domain of the AT1A angiotensin II receptor are involved in the differential recognition of peptide and nonpeptide ligands

1 reference

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7 January 2021

10.1016/S0165-6147(02)00050-0

Identifiers

DOI

1 reference

6 August 2017

1 reference

PubMed ID

12559772