Hypoxia-inducible factor-1 (HIF-1), a heterodimeric (containing α and β subunits) transcription
factor, is involved in hypoxia response pathway that regulates the expression of many tumorrelated
genes. The stabilized HIF-1 heterodimer couples to the general co-activators p300/CBP (CREB
binding protein), forming an active transcription factor to initiate hypoxic responses. Inhibiting the
transcription factor-coactivator HIF-1α-p300/CBP interaction represents an attractive approach for
blocking hypoxia pathway in tumors. Recently, diverse HIF-1α-p300/CBP inhibitors have been designed
and their anti-tumor activities have been evaluated. The developments of inhibitors of HIF-1α-
p300/CBP are discussed in this review. An outline of structures and biological activities of these inhibitors
can be traced, along with the approaches for inhibitors discovery. The challenges in identifying
novel and selective potent inhibitors of HIF-1α-p300/CBP are also put forward.
Keywords: Anticancer, cancer therapy, HIF-1α/p300 inhibitors, hypoxia response pathway, hypoxia-inducible factor-1,
p300/CREB binding protein.
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