Radicicol

Radicicol is an inhibitor of heat shock protein 90 (Hsp90; IC₅₀ = <1 mM).^1,2 It inhibits p23 from associating with Hsp90, suppresses signaling through HIF-1α, and decreases levels of progesterone receptor, Raf-1, p185^erb82, and mutant p53.^3,4 Radicicol also binds to and inhibits DNA topoisomerase type II proteins and GRP94 through an ATPase domain common to Hsp90.^3,5

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1. Kato, M., Li, J., Chuang, J.L., et al. Distinct structural mechanisms for inhibition of pyruvate dehydrogenase kinase isoforms by AZD7545, dichloroacetate, and radicicol. Structure 15(8), 992-1004 (2007).

2. Sharma, S.V., Agatsuma, T., and Nakano, H. Targeting of the protein chaperone, HSP90, by the transformation suppressing agent, radicicol. Oncogene 16, 2639-2645 (1998).

3. Schulte, T.W., Akinaga, S., Soga, S., et al. Antibiotic radicicol binds to the N-terminal domain of Hsp90 and shares important biological activities with geldanamycin. Cell Stress Chaperones 3(2), 100-108 (1998).

4. Hur, E., Kim, H.H., Choi, S.M., et al. Reduction of hypoxia-induced transcription through the repression of hypoxia-inducible factor-1 α/aryl hydrocarbon receptor nuclear translocator DNA binding by the 90-kDa heat-shock protein inhibitor radicicol. Mol. Pharmacol. 62(5), 975-982 (2002).

5. Gadelle, D., Bocs, C., Graille, M., et al. Inhibition of archaeal growth and DNA topoisomerase VI activities by the Hsp90 inhibitor radicicol. Nucleic Acids Res. 33(7), 2310-2317 (2005).