Songjiang Research Institute, Songjiang Hospital, affiliated to Shanghai Jiao Tong University School of Medicine, Shanghai 201600, China.
Department of Plastic and Reconstructive Surgery, Shanghai Ninth People's Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai 200011, China.
Trends Pharmacol Sci. 2024 Aug;45(8):678-690. doi: 10.1016/j.tips.2024.06.007. Epub 2024 Jul 25.
Achieving the efficacy and specificity of G-protein-coupled receptor (GPCR) targeting-drugs in the skin remains challenging. Understanding the molecular mechanism underlying GPCR dysfunction is crucial for developing targeted therapies. Recent advances in genetic, signal transduction, and structural studies have significantly improved our understanding of cutaneous GPCR functions in both normal and pathological states. In this review, we summarize recent discoveries of pathogenic GPCRs in dermal injuries, chronic inflammatory dermatoses, cutaneous malignancies, as well as the development of potent potential drugs. We also discuss targeting of cutaneous GPCR complexes via the transient receptor potential (TRP) channel and structure elucidation, which provide new opportunities for therapeutic targeting of GPCRs involved in skin disorders. These insights are expected to lead to more effective and specific treatments for various skin conditions.
实现皮肤中 G 蛋白偶联受体 (GPCR) 靶向药物的疗效和特异性仍然具有挑战性。了解 GPCR 功能障碍的分子机制对于开发靶向治疗至关重要。遗传、信号转导和结构研究的最新进展极大地提高了我们对正常和病理状态下皮肤 GPCR 功能的理解。在这篇综述中，我们总结了最近在皮肤损伤、慢性炎症性皮肤病、皮肤恶性肿瘤中发现的致病性 GPCR ，以及强效潜在药物的开发。我们还讨论了通过瞬时受体电位 (TRP) 通道和结构阐明靶向皮肤 GPCR 复合物，这为治疗涉及皮肤疾病的 GPCR 提供了新的机会。这些见解有望为各种皮肤状况提供更有效和更具特异性的治疗方法。
