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 Chemjournal_title
Bioorganic & medicinal chemistryauthors
Li J,Xi W,Li X,Sun H,Li Ydoi
10.1016/j.bmc.2019.01.042subject
Has Abstractpub_date
2019-04-01 00:00:00pages
1145-1158issue
7eissn
0968-0896issn
1464-3391pii
S0968-0896(18)31976-Xjournal_volume
27pub_type
杂志文章,评审abstract::The present work describes the preparation of three novel series of compounds based on the structure of goniothalamin, a natural styryl lactone which has been found to display cytotoxic and antiproliferative activities against a variety of cancer cell lines. A focused library of 29 novel goniothalamin analogues was pr...
journal_title:Bioorganic & medicinal chemistry
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更新日期:2017-10-15 00:00:00
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