Lipidated peptides: a therapeutic tool kit

Access through your institution Buy or subscribe The large number of GPCRs and their role in disease have made them attractive drug targets. As most GPCR agonists and antagonists act on the

extracellular surface of the receptor, the intracellular surface has not been exploited for therapeutic targets. However, pepducins act as receptor-modulating agents by targeting the

intracellular surface of the GPCR. PAR1 and PAR4 are activated by the protease thrombin, which results in the activation of platelets. The ability to control this signalling cascade would be

useful in preventing thrombotic complications associated with heart attacks and stroke. The present study set out to develop and test PAR1- and PAR4-based pepducin antagonists for their

ability to block platelet activation and thrombosis _in vivo_. This is a preview of subscription content, access via your institution ACCESS OPTIONS Access through your institution Subscribe

to this journal Receive 12 print issues and online access $209.00 per year only $17.42 per issue Learn more Buy this article * Purchase on SpringerLink * Instant access to full article PDF

Buy now Prices may be subject to local taxes which are calculated during checkout ADDITIONAL ACCESS OPTIONS: * Log in * Learn about institutional subscriptions * Read our FAQs * Contact

customer support REFERENCES ORIGINAL RESEARCH PAPER * Covic, L. et al. Pepducin-based intervention of thrombin receptor signalling and systemic platelet activation. _Nature Med._ 2002 Oct

(doi: 10.1038/nm760) FURTHER READING * Covic, L., Gresser, A. L., Talavera, J., Swift, S. & Kuliopulos, A. Activation and inhibition of G protein-coupled receptors by cell-penetrating,

membrane-tethered peptides. _Proc. Natl Acad. Sci. USA_ 99, 643–648 (2002). Article  CAS  PubMed  Google Scholar  * Covic, L., Singh, C., Smith, H. & Kuliopulos, A. Role of the PAR4

thrombin receptor in stabilizing platelet-platelet aggregates as revealed by a patient with Hermansky–Pudlak syndrome. _Thromb. Haemost._ 87, 722–727 (2002). Article  CAS  PubMed  Google

Scholar  Download references Authors * Melanie Brazil View author publications You can also search for this author inPubMed Google Scholar RELATED LINKS RELATED LINKS WEB SITE

Kuliopulos' laboratory RIGHTS AND PERMISSIONS Reprints and permissions ABOUT THIS ARTICLE CITE THIS ARTICLE Brazil, M. Lipidated peptides: a therapeutic tool kit. _Nat Rev Drug Discov_

1, 749 (2002). https://doi.org/10.1038/nrd929 Download citation * Issue Date: 01 October 2002 * DOI: https://doi.org/10.1038/nrd929 SHARE THIS ARTICLE Anyone you share the following link

with will be able to read this content: Get shareable link Sorry, a shareable link is not currently available for this article. Copy to clipboard Provided by the Springer Nature SharedIt

content-sharing initiative