Self-made allostery:endogenous COMP antagonizes pathologic AT1AR signaling
The identification and development of biased modulators of proximal G protein-coupled receptor (GPCR) signaling to prevent pathological disease progression has been at the forefront of recent drug discovery efforts.Recently,Fu et al.identified cartilage oligomeric matrix protein (COMP) as an endogenous negative allosteric modulator of β-arrestin (βarr)-dependent angiotensin Ⅱ (Ang Ⅱ) Type 1A receptor (AT1AR)signaling,which attenuates the development of abdominal aortic aneurysm (AAA),a chronic inflammatory vascular disease lacking pharmacological treatment options.
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2021-08-04(万方平台首次上网日期,不代表论文的发表时间)
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730-731