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An Overview of the Recent Development of Anticancer Agents Targeting the HIF-1 Transcription Factor.

ABSTRACT: Hypoxia, a characteristic feature of solid tumors, is associated with the malignant phenotype and therapy resistance of cancers. Hypoxia-inducible factor 1 (HIF-1), which is responsible for the metazoan adaptive response to hypoxia, has been recognized as a rational target for cancer therapy due to its critical functions in hypoxic regions. In order to efficiently inhibit its activity, extensive efforts have been made to elucidate the molecular mechanism underlying the activation of HIF-1. Here, we provide an overview of relevant research, particularly on a series of HIF-1 activators identified so far and the development of anticancer drugs targeting them.

SUBMITTER: Shirai Y

PROVIDER: S-EPMC8200185 | biostudies-literature | 2021 Jun

REPOSITORIES: biostudies-literature

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An Overview of the Recent Development of Anticancer Agents Targeting the HIF-1 Transcription Factor.

Shirai Yukari Y Chow Christalle C T CCT Kambe Gouki G Suwa Tatsuya T Kobayashi Minoru M Takahashi Itsuki I Harada Hiroshi H Nam Jin-Min JM

Cancers 20210604 11

Hypoxia, a characteristic feature of solid tumors, is associated with the malignant phenotype and therapy resistance of cancers. Hypoxia-inducible factor 1 (HIF-1), which is responsible for the metazoan adaptive response to hypoxia, has been recognized as a rational target for cancer therapy due to its critical functions in hypoxic regions. In order to efficiently inhibit its activity, extensive efforts have been made to elucidate the molecular mechanism underlying the activation of HIF-1. Here, ...[more]

PMID: 34200019

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