Misplaced Pages

PYR-41

Article snapshot taken from Wikipedia with creative commons attribution-sharealike license. Give it a read and then ask your questions in the chat. We can research this topic together.
This article may be too technical for most readers to understand. Please help improve it to make it understandable to non-experts, without removing the technical details. (September 2014) (Learn how and when to remove this message)
PYR-41
Names
Preferred IUPAC name Ethyl 4-{(4Z)-4--3,5-dioxopyrazolidin-1-yl}benzoate
Identifiers
CAS Number
3D model (JSmol)
ChemSpider
ECHA InfoCard 100.213.089 Edit this at Wikidata
PubChem CID
UNII
CompTox Dashboard (EPA)
InChI
  • InChI=1S/C17H13N3O7/c1-2-26-17(23)10-3-5-11(6-4-10)19-16(22)13(15(21)18-19)9-12-7-8-14(27-12)20(24)25/h3-9H,2H2,1H3,(H,18,21)/b13-9-Key: ARGIPZKQJGFSGQ-LCYFTJDESA-N
SMILES
  • CCOC(=O)C1=CC=C(C=C1)N2C(=O)/C(=C\C3=CC=C(O3)(=O))/C(=O)N2
Properties
Chemical formula C17H13N3O7
Molar mass 371.3 g/mol
Density 1.5±0.1 g/cm3
Except where otherwise noted, data are given for materials in their standard state (at 25 °C , 100 kPa). Infobox references
Chemical compound

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

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.

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. (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.


Stub icon

This antineoplastic or immunomodulatory drug article is a stub. You can help Misplaced Pages by expanding it.

Categories: