Identification of potent pyrazole based APELIN receptor (APJ) agonists
نویسندگان
چکیده
منابع مشابه
Apelin-APJ signaling in retinal angiogenesis.
The G protein–coupled receptor (GPCR) APJ (X-msr, angiotensin receptor like 1b) was cloned in several laboratories by homology screening, with the goal of identifying new members of this class of cell surface receptor.1 This gene attracted attention because of its sequence similarity to the important angiotensin II type 1 receptor and its highly restricted pattern of expression in endothelial c...
متن کاملEndogenous regulation of cardiovascular function by apelin-APJ.
Studies have shown significant cardiovascular effects of exogenous apelin administration, including the potent activation of cardiac contraction. However, the role of the endogenous apelin-APJ pathway is less clear. To study the loss of endogenous apelin-APJ signaling, we generated mice lacking either the ligand (apelin) or the receptor (APJ). Apelin-deficient mice were viable, fertile, and sho...
متن کاملThe Apelin-APJ System in the Evolution of Heart Failure
Heart failure is a chronic, progressive disease in which the overexpression of biologically active molecules and neurohomonal activation are the key factors of the evolution and natural history. The apelin-APJ system is a newly discovered molecular pathway and the RAAS counterbalance is its principal effect. The apelin is a potent inotrope, vasodilator and diuretic with crucial cardioprotective...
متن کاملApelin/APJ system: A key therapeutic target for liver disease
Apelin, a new bioactive peptide, was identified as an endogenous ligand for APJ (Angiotensin II receptor-like 1). Apelin and its receptor have an abundant distribution in central nervous system and peripheral tissues, including liver. Apelin/APJ has diverse physiological and pathological effects, including regulation of cardiovascular function, angiogenesis, fluid homeostasis and so on. Apelin/...
متن کاملThe apelin-APJ system induces tumor arteriogenesis in hepatocellular carcinoma.
AIM The apelin-APJ system regulates angiogenesis, and is overexpressed in several types of cancer. The aim of this study was to clarify the role of the apelin-APJ system in the angiogenesis of hepatocellular carcinoma (HCC). MATERIALS AND METHODS Expressions of angiogenic factors and vascular markers were investigated in specimens from 90 HCC patients. A subcutaneous HCC tumor mouse model was...
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ژورنال
عنوان ژورنال: Bioorganic & Medicinal Chemistry
سال: 2020
ISSN: 0968-0896
DOI: 10.1016/j.bmc.2019.115237