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Advances in inhibition of protein-protein interactions targeting hypoxia-inducible factor-1 for cancer therapy.

Abstract：

:Hypoxia is a common characteristic of many types of solid tumors and is associated with tumor propagation, malignant progression, and resistance to anti-cancer therapy. HIF-1 pathway is one of the survival pathways activated in tumor in response to hypoxia. In hypoxic condition, hypoxia-inducible factor-1α (HIF-1α) is stabilized and translocated into nucleus where it forms heterodimer with HIF-1β and regulates the expression of a plethora of genes involved in different processes, such as cell proliferation, differentiation, apoptosis, vascularization/angiogenesis, tumor invasion and metastasis. Recruitment of co-activator p300 or CBP to HIF-1α is critical to the transactivation activity of HIF-1 dimer, therefore, small molecules which can block the dimerization of HIF-1α and HIF-1β or inhibit the interaction between HIF-1α and p300 can function as inhibitors of HIF-1 and have the potential to be developed as novel therapies for the treatment of human cancers. In this review, recent progress of small molecular inhibitors of protein-protein interactions targeting HIF-1 is summarized, the mechanism of functions of these compounds and their potential usage as anti-cancer agents have also been discussed.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Li J,Xi W,Li X,Sun H,Li Y

doi

10.1016/j.bmc.2019.01.042

subject

Has Abstract

pub_date

2019-04-01 00:00:00

pages

1145-1158

issue

7

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(18)31976-X

journal_volume

27

pub_type

杂志文章,评审

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