Self-made allostery: endogenous COMP antagonizes pathologic AT1AR signaling

Article Medicine, Research & Experimental

TREM-1 orchestrates angiotensin II-induced monocyte trafficking and promotes experimental abdominal aortic aneurysm

Marie Vandestienne et al.

Summary: The study demonstrated that TREM-1 plays a crucial role in the pathophysiology of AAA and could be a potential therapeutic target for the disease in humans.

JOURNAL OF CLINICAL INVESTIGATION (2021)

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Article Cell Biology

Cartilage oligomeric matrix protein is an endogenous beta-arrestin-2-selective allosteric modulator of AT1 receptor counteracting vascular injury

Yi Fu et al.

Summary: This study reveals that the extracellular matrix protein COMP acts as an endogenous allosteric biased modulator of the AT1 receptor, inhibiting specific signaling pathways through the regulation of intracellular conformational states. COMP deficiency leads to exclusive AAA formation in response to AngII infusion, indicating a potential therapeutic target for cardiovascular diseases.

CELL RESEARCH (2021)

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Article Cell Biology

Biased signaling as allosteric probe dependence

Terry Kenakin

Summary: Signaling bias is a phenomenon in seven transmembrane receptors where different agonists can activate specific signaling pathways more than others, potentially leading to therapeutic benefits. However, determining a quantitative value for receptor bias that can be translated to useful in vivo studies remains a challenge, and further research is needed to overcome current limitations.

CELLULAR SIGNALLING (2021)

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Review Cell Biology