Pepducin
Pepducins are cell-penetrating
intracellular modulators of signal transference from receptors to G proteins. Pepducins were first developed at the Tufts Medical Center laboratories of Dr. Athan Kuliopulos and Dr. Lidija Covic.[1]
Pepducins employ lipidated fragments of intracellular
allosteric mechanism. Pepducins for over 15 different GPCRs have been successfully produced, several of which have shown activity in preclinical in vivo models.[3]
An anti-
PAR4 pepducin extended bleeding time in mice and protected against systemic platelet activation and thrombosis.[2]
A CXCR4 agonist pepducin mobilizes bone marrow hematopoietic cells.[4]
A PAR1 pepducin, PZ-128, has successfully completed phase I clinical trials.[5][6][7]
References
- PMID 11805322.
- ^ PMID 14607253.
- S2CID 24166439.
- ^ "Discovery of a CXCR4 agonist pepducin that mobilizes bone marrow hematopoietic cells". 2010. Archived from the original on 2011-07-24. Retrieved 2011-03-02.
- PMID 22705889.
- )
- PMID 22374997.