PYR-41 is a cell permeable irreversible inhibitor of ubiquitin-activating enzyme E1.[1] It was also reported to increase sumoylation in cells.[1][2]

PYR-41 also blocks the downstream ubiquitination and ubiquitination-dependent protein degradation or other ubiquitination-mediated cellular activities. In addition, PYR-41 inhibits degradation of p53, a tumour suppressor.[3]

References

  1. ^ a b Yang, Yili; Kitagaki, Jirouta; Dai, Ren-Ming; Tsai, Yien Che; Lorick, Kevin L.; Ludwig, Robert L.; Pierre, Shervon A.; Jensen, Jane P.; Davydov, Ilia V.; Oberoi, Pankaj; Li, Chou-Chi H.; Kenten, John H.; Beutler, John A.; Vousden, Karen H.; Weissman, Allan M. (1 October 2007). "Inhibitors of Ubiquitin-Activating Enzyme (E1), a New Class of Potential Cancer Therapeutics". Cancer Research. 67 (19): 9472–9481. doi:10.1158/0008-5472.CAN-07-0568. PMID 17909057.
  2. ^ Kapuria V, Peterson LF, Showalter HD, et al. (Aug 15, 2011). "Protein cross-linking as a novel mechanism of action of a ubiquitin-activating enzyme inhibitor with anti-tumor activity". Biochem Pharmacol. 82 (4): 341–349. doi:10.1016/j.bcp.2011.05.012. PMID 21621524.
  3. ^ Chen C, et al. (Jun 2014). "Ubiquitin-activating enzyme E1 inhibitor PYR-41 attenuates angiotensin II-induced activation of dendritic cells via the IκBa/NF-κB and MKP1/ERK/STAT1 pathways". Immunology. 142 (2): 307–319. doi:10.1111/imm.12255. PMC 4008238. PMID 24456201.


Allikas: http://en.wikipedia.org/wiki/PYR-41
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