Gilles Nicolas
CEA, SIMoS, Département Médicaments et Technologies pour la Santé (DMTS), Université Paris-Saclay, 91191 Gif-sur-Yvette, France.
Biology (Basel). 2023 Apr 3;12(4):544. doi: 10.3390/biology12040544.
The type 2 vasopressin receptor (V2R) is expressed in the kidneys, and it is the keystone of water homeostasis. Under the control of the antidiuretic hormone vasopressin, the V2R ensures vital functions, and any disturbance has dramatic consequences. Despite decades of research to develop drugs capable of activating or blocking V2R function to meet real medical needs, only one agonist and one antagonist are virtually used today. These two drugs cover only a small portion of patients' needs, leaving millions of patients without treatment. Natural peptide toxins known to act selectively and at low doses on their receptor target could offer new therapeutic options.
2型血管加压素受体（V2R）在肾脏中表达，是水稳态的关键。在抗利尿激素血管加压素的控制下，V2R确保重要功能，任何干扰都会产生严重后果。尽管经过数十年研究以开发能够激活或阻断V2R功能以满足实际医疗需求的药物，但如今实际上仅使用一种激动剂和一种拮抗剂。这两种药物仅满足了患者需求的一小部分，使数百万患者得不到治疗。已知能以低剂量选择性作用于其受体靶点的天然肽毒素可能提供新的治疗选择。
