Highlights from new publications on C21 and the AT2 receptor
Effect of Compound 21, a Selective Angiotensin II Type 2 Receptor Agonist, in a Murine Xenograft Model of Dupuytren Disease. Chrisholm et al., Plast Reconstr Surg. 2017 Nov;140(5):686e-696e. https://www.ncbi.nlm.nih.gov/pubmed/29068929
This study is the first that investigated the anti-fibrotic effect of C21 in a model of Dupuytren Disease. The authors showed that C21 reduced the expression of pro-fibrotic genes such as TGFb, CTGF, SMAD 3, 4 and 7 in primary human fibroblasts, which were stimulated with TGFb. Moreover, they demonstrated that C21 inhibited fibrotic activity in human Dupuytren Disease cord segments transplanted into nude mice. Based on these data, Dupuytren Disease may be considered as another clinical indication of interest for C21.
Direct Activation of the Angiotensin II Type-2 Receptors Enhances Muscle Microvascular Perfusion, Oxygenation and Insulin Delivery in Male Rats. Yan et al., Endocrinology. 2017 Nov 24. doi: 10.1210/en.2017-00585 https://www.ncbi.nlm.nih.gov/pubmed/29186390
This publication adds an important piece of information to the understanding of the beneficial effect of AT2 receptor stimulation on insulin sensitivity and glucose metabolism. While other studies had shown effects on adipokine expression, PPARg activity and adipocyte differentiation, this study demonstrates for the first time that direct activation of AT2 receptors with C21 significantly increases microvascular perfusion, oxygenation, insulin delivery and metabolic action in muscular tissue. Therefore, the findings of this study further strengthen evidence for a beneficial effect of AT2 receptor stimulation on glucose/insulin metabolism.
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