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Characterization of Inhibition Reveals Distinctive Properties for Human and Saccharomyces cerevisiae CRM1.

Abstract：

:The receptor CRM1 is responsible for the nuclear export of many tumor-suppressor proteins and viral ribonucleoproteins. This renders CRM1 an interesting target for therapeutic intervention in diverse cancer types and viral diseases. Structural studies of Saccharomyces cerevisiae CRM1 ( Sc CRM1) complexes with inhibitors defined the molecular basis for CRM1 inhibition. Nevertheless, no structural information is available for inhibitors bound to human CRM1 ( Hs CRM1). Here, we present the structure of the natural inhibitor Leptomycin B bound to the Hs CRM1-RanGTP complex. Despite high sequence conservation and structural similarity in the NES-binding cleft region, Sc CRM1 exhibits 16-fold lower binding affinity than Hs CRM1 toward PKI-NES and significant differences in affinities toward potential CRM1 inhibitors. In contrast to Hs CRM1, competition assays revealed that a human adapted mutant Sc CRM1-T539C does not bind all inhibitors tested. Taken together, our data indicate the importance of using Hs CRM1 for molecular analysis and development of novel antitumor and antiviral drugs.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Shaikhqasem A,Dickmanns A,Neumann P,Ficner R

doi

10.1021/acs.jmedchem.0c00143

subject

Has Abstract

pub_date

2020-07-23 00:00:00

pages

7545-7558

issue

14

eissn

0022-2623

issn

1520-4804

journal_volume

63

pub_type

杂志文章

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