Ubiquitin-Proteasome System (UPS) Research Reagents

Ubiquitin-Proteasome System (UPS) is an important system which regulates a number of signal transduction pathways and through which proteins are marked for proteasomal degradation by being linked to the polypeptide co-factor ubiquitin.
In the recent years, targeted protein degradation (TPD) using UPS to achieve knockdown of target proteins within cells (PROTAC, proteolysis targeting chimeras) became a useful drug discovery tool. ^1,2)

E3 ubiquitin ligase inhibitors

Proteasome inhibitors

Deubiquitinating enzyme inhibitors

Related products^3,4)

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References

• 1) Protacs: Chimeric molecules that target proteins to the Skp1–Cullin–F box complex for ubiquitination and degradation
  • K. M. Sakamoto, K. B. Kim, A. Kumagai, F. Mercurio, C. M. Crews, R. J. Deshies, Proc. Natl. Acad. Sci. USA 2001, 98, 8554.
• 2) Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs
  • S. An, L. Fu, EBioMedicine 2018, 36, 553.
• 3) Protein knockdown using methyl bestatin-ligand hybrid molecules: design and synthesis of inducers of ubiquitination-mediated degradation of cellular retinoic acid-binding proteins
  • Y. Itoh, M. Ishikawa, M. Naito, Y. Hashimoto, J. Am. Chem. Soc., 2010, 132, 5820.
• 4) Reversible inhibitor of p97, DBeQ, impairs both ubiquitin-dependent and autophagic protein clearance pathways
  • T. F. Chou, S. J. Brown, D. Minond, B. E. Nordin, K. Li, A. C. Jones, P. Chase, P. R. Porubsky, B. M. Stoltz, F. J. Schoenen, M. P. Patricelli, P .Hodder, H. Rosen, R. J. Deshaies, Proc. Natl. Acad. Sci. USA 2011, 108, 4834.

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