Identification and Development of Cyclic Peptide Inhibitors of Hypoxia Inducible Factors 1 and 2 That Disrupt Hypoxia-Response Signaling in Cancer Cells

• Published in: Journal of the American Chemical Society Vol. 146; no. 13; pp. 8877 - 8886
• Main Authors: Ball, Andrew T., Mohammed, Soran, Doigneaux, Cyrielle, Gardner, Reece M., Easton, James W., Turner, Steven, Essex, Jonathan W., Pairaudeau, Garry, Tavassoli, Ali
• Format: Journal Article
• Language: English
• Published: WASHINGTON American Chemical Society 03.04.2024; Amer Chemical Soc
• Subjects: Cell Hypoxia; Chemistry; Chemistry, Multidisciplinary; Humans; Hypoxia; Hypoxia-Inducible Factor 1 - metabolism; Hypoxia-Inducible Factor 1, alpha Subunit - metabolism; Neoplasms - drug therapy; Oxygen - metabolism; Peptides, Cyclic - metabolism; Peptides, Cyclic - pharmacology; Physical Sciences; Science & Technology; Signal Transduction; ACTIVATION; SOLID TUMORS; TRANSCRIPTION; BIOLOGY; GENE-EXPRESSION; HIF2-ALPHA; FACTOR-I; HIF-1-ALPHA; TISSUES; BINDING

Hypoxia inducible factor (HIF) is a heterodimeric transcription factor composed of an oxygen-regulated α subunit and a constitutively expressed β subunit that serves as the master regulator of the cellular response to low oxygen concentrations. The HIF transcription factor senses and responds to hyp...