Zouboulis Christos C
Dermatoendocrinol. 2009 Mar;1(2):77-80. doi: 10.4161/derm.1.2.7804.
Receptors are proteins, embedded in a cell or cytoplasmic membrane, to which a mobile signaling molecule may attach. Receptor ligands may be peptides (such as neurotransmitters), hormones, pharmaceutical drugs and/or a toxins, whereas "binding" ordinarily initiates a cellular response. Human sebocytes are biologically and metabolically very active cells and consequently express numerous receptors. Three of four groups of peptide/neurotransmitter receptors, the so-called serpentine receptor group are present (corticotropin-releasing hormone receptors 1 and 2, melanocortin-1 and 5 receptors, mu-opiate receptors, VPAC receptors, cannabinoid receptors 1 and 2, vascular endothelial growth factor receptor and histamine 1 receptor). The single-transmembrane domain receptors are represented by the insulin-like growth factor-I receptor and the third group, which does not possess intrinsic tyrosine kinase activity, by the growth factor receptor. Nuclear receptors expressed in sebocytes are grouped into two major subtypes. From the steroid receptor family, the androgen receptor and the progesterone receptor are expressed. The thyroid receptor family includes the estrogen receptors (alpha and beta isotypes), the retinoic acid receptors (isotypes alpha and gamma) and retinoid X receptors (isotypes alpha, beta, gamma), the vitamin D receptor, the peroxisome proliferator-activated receptors (isotypes alpha, delta and gamma) and the liver X receptors (alpha and beta isotypes). The vanilloid receptor belongs to the transient ion channels and is expressed in differentiating human sebocytes. Further sebocyte receptors, which may influence their function are fibroblast growth factor receptor 2, epidermal growth factor receptor, c-MET, CD14, Toll-like receptor 2, Toll-like receptor 4 and Toll-like receptor 6. Receptor-ligand interactions control sebocyte proliferation, differentiation and lipid synthesis. However, not every ligand that binds to a sebocyte receptor also activates it, such ligands are receptor antagonists and inverse agonists.
受体是嵌入细胞或细胞质膜中的蛋白质,移动的信号分子可与之结合。受体配体可以是肽(如神经递质)、激素、药物和/或毒素,而“结合”通常会引发细胞反应。人皮脂腺细胞在生物学和代谢方面非常活跃,因此表达多种受体。存在四类肽/神经递质受体中的三类,即所谓的蛇形受体组(促肾上腺皮质激素释放激素受体1和2、黑皮质素-1和5受体、μ-阿片受体、血管活性肠肽受体、大麻素受体1和2、血管内皮生长因子受体和组胺1受体)。单跨膜结构域受体由胰岛素样生长因子-I受体代表,第三组不具有内在酪氨酸激酶活性的受体由生长因子受体代表。在皮脂腺细胞中表达的核受体分为两个主要亚型。在类固醇受体家族中,雄激素受体和孕激素受体表达。甲状腺受体家族包括雌激素受体(α和β亚型)、视黄酸受体(α和γ亚型)和视黄醇X受体(α、β、γ亚型)、维生素D受体、过氧化物酶体增殖物激活受体(α、δ和γ亚型)和肝脏X受体(α和β亚型)。香草酸受体属于瞬时离子通道,在分化的人皮脂腺细胞中表达。可能影响其功能的其他皮脂腺细胞受体有成纤维细胞生长因子受体2、表皮生长因子受体、c-MET、CD14、Toll样受体2、Toll样受体4和Toll样受体6。受体-配体相互作用控制皮脂腺细胞的增殖、分化和脂质合成。然而,并非每个与皮脂腺细胞受体结合的配体都会激活它,这类配体是受体拮抗剂和反向激动剂。