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

SIMPLE SUMMARY: As hypoxia-inducible factor 1 (HIF-1) is recognized as a target for cancer therapy, extensive efforts have been devoted to developing its inhibitors. We provide an overview of the latest information about basic, translational, and clinical research for the development of HIF-1 inhibitors. 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.