HIF-1 Signaling Pathway Compound Library

Cell signaling is part of any communication process that governs basic activities of cells and coordinates all cell actions. The ability of cells to perceive and correctly respond to their microenvironment is the basis of development, tissue repair, and immunity, as well as normal tissue homeostasis. Errors in signaling interactions and cellular information processing are responsible for diseases such as cancer, autoimmunity, and diabetes. By understanding cell signaling, diseases may be treated more effectively.

As a key regulator of the hypoxia response, hypoxia inducible factor-1 (HIF-1) has been attracting more attention from scientists. HIF-1 is an evolutionarily conserved transcription factor that functions as a main regulator of gene expression in response to hypoxia. HIF-1 is functionally heterodimeric, composed of HIF-1β and one of three α subunits (HIF-1α, HIF-2α, or HIF-3α). All subunits are part of the basic helix-loop-helix superfamily of transcription factors, but its activity is primarily controlled by cellular levels of the HIF-1α subunit. As a transcriptional factor, the heterodimer HIF-1 recognizes and binds to the consensus sequence 5’-(A/G) CGTG-3’ named hypoxia-responsive elements (HREs) to activate the transcriptional activity of target genes. To date, more than 100 direct target genes of HIF-1 have been uncovered, which have been shown to be functionally involved in tumor metastasis, angiogenesis, energy metabolism, cell differentiation and apoptosis.

Intensive studies have clearly established the hypoxia/HIF signaling pathway as a master regulator of the vascular system. Accordingly, it represents an important therapeutic target for vascular diseases and cancer. Pharmacologically increased HIF function may aid in the treatment of a wide range of diseases, as HIF has been shown to be essential for phenomena as diverse as immune function, cartilage formation, and wound healing. Conversely, inhibition of HIF function could also have many applications: increased levels of HIF are seen in many cancers as well as in some cardiovascular diseases, including stroke, heart attack, and pulmonary hypertension.

To meet the need of research in oxygen-sensing pathways, TargetMol collects 1352 HIF-1 related small chemicals，involving PI3K-AKT, MAPK, Ubiquitination signaling pathways and targets such as HIF, HIF Prolyl-Hydroxylase, E1/E2/E3 Enzyme, PI3K, MAPK, Proteasome, etc.