Selective Affimers Recognize the BCL-2 Family Proteins BCL-xL and MCL-1 through Non-Canonical Structural Motifs.,ChemBioChem

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Selective Affimers Recognize the BCL-2 Family Proteins BCL-xL and MCL-1 through Non-Canonical Structural Motifs.
ChemBioChem ( IF 3.2 ) Pub Date : 2020-09-22 , DOI: 10.1002/cbic.202000585
Jennifer A Miles _{1,

2,

3} , Fruzsina Hobor _{1,

2} , Chi H Trinh _{1,

2} , James Taylor _{1,

2} , Christian Tiede _{1,

2} , Philip R Rowell _{1,

2} , Brian R Jackson _{1,

2,

4} , Fatima A Nadat _{1,

2,

4} , Pallavi Ramsahye _{1,

2} , Hannah F Kyle _{1,

2} , Basile I M Wicky ₅ , Jane Clarke ₅ , Darren C Tomlinson _{1,

2} , Andrew J Wilson _{2,

3} , Thomas A Edwards _{1,

2}

Affiliation

Affimer reagents (non‐antibody binding proteins) are identified that bind selectively to the anti‐apoptotic proteins BCL‐x_L and MCL‐1. Crystallographic studies reveal an unprecedented mode of molecular recognition in which flexible loops from the Affimer dock into the BH3 binding cleft as opposed to a canonical α‐helix. Furthermore the Affimers induce changes in the target proteins towards desirable drug‐bound‐like conformations.

中文翻译：

选择性仿射器通过非规范结构基序识别 BCL-2 家族蛋白 BCL-xL 和 MCL-1。

亲和试剂（非抗体结合蛋白）被鉴定为选择性结合抗凋亡蛋白 BCL-x _L和 MCL-1。晶体学研究揭示了一种前所未有的分子识别模式，其中来自 Affimer 的柔性环停靠在 BH3 结合裂口中，而不是典型的 α 螺旋。此外，仿射体诱导靶蛋白向理想的药物结合样构象变化。

更新日期：2020-09-22

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