PYR-41 explained

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

Notes and References

  1. 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. . Inhibitors of Ubiquitin-Activating Enzyme (E1), a New Class of Potential Cancer Therapeutics . Cancer Research . 1 October 2007 . 67 . 19 . 9472–9481 . 10.1158/0008-5472.CAN-07-0568 . 17909057. free .
  2. Biochem Pharmacol. Protein cross-linking as a novel mechanism of action of a ubiquitin-activating enzyme inhibitor with anti-tumor activity. . Kapuria V, Peterson LF, Showalter HD, etal . Aug 15, 2011. 82. 4. 341–349. 10.1016/j.bcp.2011.05.012. 21621524.
  3. Immunology. 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.. Jun 2014. 142. 2. 307–319. 10.1111/imm.12255 . Chen C, etal . 24456201. 4008238.

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