Target intelligence / Profile preview

Angiotensin II receptor type 1 (AT1R) (AT1R)

Target
AT1R
Molecular classification
G protein-coupled receptor, Receptor
01

Overview

The Angiotensin II receptor type 1 (AT1R) is a G protein-coupled receptor that serves as the primary mediator for the physiological and pathological effects of Angiotensin II, the central effector of the renin-angiotensin-aldosterone system (RAAS) (Source: UniProt P30556). Upon activation, AT1R triggers a complex cascade of downstream signaling pathways, including the Gq/11-phospholipase C pathway, which leads to intracellular calcium mobilization and activation of protein kinase C (Source: StatPearls, Angiotensin II Receptor Blockers). These events result in potent vasoconstriction, stimulation of aldosterone release from the adrenal cortex, and promotion of renal sodium reabsorption (Source: NIH, Gene ID 185). Chronic overactivation of AT1R signaling is a major driver of hypertension, cardiac hypertrophy, and renal fibrosis (Source: PubMed, PMID: 25454601). Consequently, AT1R is a major therapeutic target, with Angiotensin II Receptor Blockers (ARBs) widely used to treat cardiovascular and renal diseases by preventing the binding of Angiotensin II to the receptor (Source: PubChem). Clinical management involves monitoring for side effects such as hyperkalemia and hypotension, and the target is strictly avoided during pregnancy due to known teratogenic effects (Source: FDA).

Other names
AGTR1AT1 receptorAngiotensin II type-1 receptorType-1 angiotensin II receptor
02

Mechanism of action

Competitive antagonism of the Angiotensin II receptor type 1 (AT1R), preventing the activation of downstream signaling pathways that mediate vasoconstriction and aldosterone secretion.

03

Biological functions

Signal transductionVasoconstrictionAldosterone secretionCell proliferationInflammationSodium retention
04

Disease associations

Cardiovascular diseaseHypertensionHeart failureDiabetic nephropathyChronic kidney disease
05

Safety considerations

HypotensionHyperkalemiaRenal impairmentTeratogenicity (fetal toxicity)
06

Interacting drugs

Losartan

6 more in the full profile.

07

Biomarkers

Blood pressurePlasma renin activitySerum potassiumUrinary albumin-to-creatinine ratio

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