KISS1R Q969F8

KiSS-1受体 (KiSS-1R) (G蛋白偶联受体54) (G蛋白偶联受体OT7T175) (hOT7T175) (促性腺激素释放激素-1) (Kisspeptins受体) (Metastin受体)

功能描述

Kisspeptins (kisspeptin-10, kisspeptin-13, kisspeptin-14 和 metastin/kisspeptin-54) 的受体 (PubMed:11457843, PubMed:11527393, PubMed:15020672, PubMed:15596153)。下丘脑 KISS1/KISS1R 信号系统通过调节 GnRH 神经元分泌促性腺激素释放激素 (GnRH)，在下丘脑-垂体-性腺生殖轴的调节中发挥核心作用 (PubMed:12944565, PubMed:14573733, PubMed:15598687, PubMed:17164310, PubMed:18272894)。在这些神经元中，kisspeptin 与其受体结合激活 G(q) 依赖性信号，导致磷脂酶 C (PLC) 激活，以及磷脂酰肌醇 4,5-二磷酸 (PIP2) 的水解 (PubMed:14573733, PubMed:15598687, PubMed:39151001)。随后细胞内钙水平的升高导致内向整流钾通道的抑制和 TRPC 样阳离子通道的激活，导致 GnRH 神经元去极化和兴奋 (By similarity)。除了该途径外，kisspeptin 还通过 beta-arrestin 触发非 G(q) 依赖性信号，导致 MAPK 级联激活和 ERK1/ERK2 磷酸化 (PubMed:25147978)。此外，kisspeptin-10 激活 KISS1R 通过 G(q) 依赖性信号通路将磷酸酶 DUSP18 和 SRC 募集到 KISS1R C 端，导致 DUSP18 介导的 SRC 去磷酸化 (PubMed:38346942)。在骨组织中，这导致破骨细胞分化和活性下调，从而抑制骨吸收 (By similarity)。KISS1R 还参与其他过程的调节，包括细胞增殖和细胞迁移 (PubMed:11457843, PubMed:11527393, PubMed:15020672, PubMed:15596153, PubMed:38512807)。 {ECO:0000250|UniProtKB:Q91V45, ECO:0000269|PubMed:11457843, ECO:0000269|PubMed:11527393, ECO:0000269|PubMed:12944565, ECO:0000269|PubMed:14573733, ECO:0000269|PubMed:15020672, ECO:0000269|PubMed:15596153, ECO:0000269|PubMed:15598687, ECO:0000269|PubMed:17164310, ECO:0000269|PubMed:18272894, ECO:0000269|PubMed:25147978, ECO:0000269|PubMed:38346942, ECO:0000269|PubMed:38512807, ECO:0000269|PubMed:39151001}.

组织特异性

Expressed in the pancreas, placenta and spinal cord, with lower-level of expression in peripheral blood leukocytes, kidney, lung, fetal liver, stomach, small intestine, testes, spleen, thymus, adrenal glands and lymph nodes. In the adult brain, expressed in the superior frontal gyrus, putamen, caudate nucleus, cingulate gyrus, nucleus accumbens, hippocampus, pons and amygdala, as well as the hypothalamus and pituitary. Expression levels are higher in early (7-9 weeks) than term placentas. Expression levels were increased in both early placentas and molar pregnancies and were reduced in choriocarcinoma cells. Expressed at higher levels in first trimester trophoblasts than at term of gestation. Also found in the extravillous trophoblast suggesting endocrine/paracrine activation mechanism.

亚细胞定位

Cell membrane