Structure-function of alpha1-adrenergic receptors.

Structure-function of alpha1-adrenergic receptors. Research Abstract Details 

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Structure-function of alpha1-adrenergic receptors. Abstract Text:

Dianne M Perez,

The Easson-Stedman hypothesis provided the rationale for the first studies of drug design for the alpha(1)-adrenergic receptor. Through chemical modifications of the catecholamine core structure, the need was established for a protonated amine, a beta-hydroxyl on a chiral center, and an aromatic ring with substitutions capable of hydrogen bonding. After the receptors were cloned and three alpha(1)-adrenergic receptor subtypes were discovered, drug design became focused on the analysis of receptor structure and new interactions were uncovered. It became clear that alpha(1)- and beta-adrenergic receptors did not share stringent homology in the ligand-binding pocket but this difference has allowed for more selective drug design. Novel discoveries on allosterism and agonist trafficking may be used in the future design of therapeutics with fewer side effects. This review will explore past and current knowledge of the structure-function of the alpha(1)-adrenergic receptor subtypes.

Structure-function of alpha1-adrenergic receptors. Publishing Authors By Initials

DM Perez,

For similar biochemical phenomena, metabolism, and nutrition: biochemical phenomena: structure-activity relationship research abstracts see: biochemical phenomena, metabolism, and nutrition: biochemical phenomena: structure-activity relationship research

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Structure-function of alpha1-adrenergic receptors. Journal Published:

PUBLICATION TYPE: Review

Journal: Biochemical pharmacology

VOLUME: 73

Page Numbers: 1051-62

Journal Abbreviation: Biochem. Pharmacol.

ISSN: 0006-2952

DAY: 16

MONTH: 09

YEAR: 2006

Structure-function of alpha1-adrenergic receptors. Information

Number of References: 78

LANGUAGE: eng

NlmUniqueID: 101032

Structure-function of alpha1-adrenergic receptors. Keywords Mesh Terms:

KEYWORDS: Structure-Activity Relationship

MESH TERMS: physiology

Chemical & Substance for Abstract: Structure-function of alpha1-adrenergic receptors. Information

Substance Name: Receptors, Adrenergic, beta

Registry Number: 0

Grant and Affiliation Information for Structure-function of alpha1-adrenergic receptors.

AFFILIATION: Department of Molecular Cardiology, NB5, The Cleveland Clinic Foundation, Lerner Research Institute, 9500 Euclid Avenue, Cleveland, OH 44195, USA. Perezd@ccf.org

Country: England

AGENCY: United States NHLBI

GRANT: R01HL61438

ACRONYM: HL

MEDLINETA: Biochem Pharmacol

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