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首页> 外文期刊>Acta crystallographica. Section D, Structural biology. >Antibody fragments structurally enable a drug-discovery campaign on the cancer target Mcl-1
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Antibody fragments structurally enable a drug-discovery campaign on the cancer target Mcl-1

机译:抗体片断结构支持癌症药物运动的目标mcl1

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摘要

Apoptosis is a crucial process by which multicellular organisms control tissuegrowth, removal and inflammation. Disruption of the normal apoptotic functionis often observed in cancer, where cell death is avoided by the overexpression ofanti-apoptotic proteins of the Bcl-2 (B-cell lymphoma 2) family, including Mcl-1(myeloid cell leukaemia 1). This makes Mcl-1 a potential target for drug therapy,through which normal apoptosis may be restored by inhibiting the protectivefunction of Mcl-1. Here, the discovery and biophysical properties of an anti-Mcl-1 antibody fragment are described and the utility of both the scFv and Fabare demonstrated in generating an Mcl-1 crystal system amenable to iterativestructure-guided drug design.
机译:细胞凋亡是一个至关重要的过程多细胞生物控制tissuegrowth,删除和炎症。正常凋亡functionis经常观察到癌症,避免细胞死亡的超表达ofanti-apoptotic蛋白质的bcl - 2 (b细胞淋巴瘤2)的家庭,包括mcl1(髓细胞白血病1)。这使得mcl1一个潜在的药物治疗的目标,通过它正常细胞凋亡可能是通过抑制恢复mcl1的protectivefunction。发现和生物物理属性的anti-Mcl-1抗体片段和描述scFv和Fabare的效用在生成一个mcl1晶体系统适合iterativestructure-guided药物设计。

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