Drozdz R, Siegrist W, Baker B I, Chluba-de Tapia J, Eberle A N
Department of Research, University Hospital, Basel, Switzerland.
FEBS Lett. 1995 Feb 13;359(2-3):199-202. doi: 10.1016/0014-5793(95)00043-9.
An analogue of human melanin-concentrating hormone (MCH) suitable for radioiodination was designed in which Tyr13 was replaced by Phe and Val19 by Tyr. The resulting monoiodinated [125I] [Phe13,Tyr19]-MCH radioligand was biologically active and led to the discovery of high-affinity binding sites on mouse B16-F1, G4F and G4F-7 melanoma cells. Saturation binding analysis with G4F-7 cells revealed 1090 MCH receptors per cell and a KD of 1.18 x 10(-10) mol/l. Receptors for MCH were also found on rat PC12 phaeochromocytoma cells, human RE melanoma cells and COS-7 cells. Competition binding analyses with other peptides such as alpha-MSH, NPY and PACAP demonstrated that MCH receptor binding is specific. rANF(1-28) was found to be a weak competitor of MCH, indicating topological similarities between MCH and rANF(1-28) when interacting with MCH receptors.
设计了一种适合进行放射性碘化的人促黑素细胞激素（MCH）类似物，其中Tyr13被Phe取代，Val19被Tyr取代。所得的单碘化[125I][Phe13,Tyr19]-MCH放射性配体具有生物活性，并导致在小鼠B16-F1、G4F和G4F-7黑色素瘤细胞上发现了高亲和力结合位点。对G4F-7细胞进行的饱和结合分析显示，每个细胞有1090个MCH受体，解离常数KD为1.18×10^(-10) mol/l。在大鼠PC12嗜铬细胞瘤细胞、人RE黑色素瘤细胞和COS-7细胞上也发现了MCH受体。用其他肽如α-MSH、NPY和PACAP进行的竞争结合分析表明，MCH受体结合具有特异性。发现rANF(1-28)是MCH的弱竞争者，表明MCH与rANF(1-28)在与MCH受体相互作用时存在拓扑相似性。
