Kendomycin

Kendomycin是从各种链霉菌中分离得到的聚酮类大环内酯类抗生素，具有已证明的细胞毒性和抗骨质疏松性质。结构上对合成化学家很感兴趣，Kendomycin的大环含有稀有的醌甲基化物发色团。Kendomycin的抗生素活性对包括耐甲氧西林和万古霉素的金黄色葡萄球菌在内的多种细菌均显示功效。研究表明，Kendomycin对多种肿瘤细胞系的细胞毒性与胰凝乳蛋白酶样蛋白酶体活性的抑制有关。虽然该发现表明与细胞毒性没有直接关系，但也描述了通过抑制蛋白与Bak的相互作用，使霉素能够使抗凋亡蛋白Bcl-xl失活。早期

Kendomycin is a polyketide macrolide antibiotic isolated from various|Streptomyces|strains, with demonstrated cytotoxic and antiosteoporotic properties. Structurally intriguing to synthetic chemists, the macrocycle of Kendomycin contains a rare quinone methide chromophore. The antibiotic activity of Kendomycin shows efficacy against a range of bacteria including Methicillin- and Vancomycin-resistant|Staphylococcus aureus|. Studies correlate the demonstrated cytotoxicity of Kendomycin against multiple tumor cell lines to an inhibition of chymotrypsin-like proteasome activity. Kendomycin is also described to disable the antiapoptotic protein Bcl-xl by blocking protein-protein interaction with Bak, though this finding showed no direct correlation to cytotoxicity. Early reports described Kendomycin as an endothelin receptor antagonist, and the antiosteoporotic effects were correlated to CT-R (calcitonin receptor) agonism. Kendomycin is an inhibitor of ETAR and ETBR.