English (United Kingdom)

https://curated-unify.zendy.io/wp-json/zendy-region/v1/featured_content/oa?rat=en

https://curated-unify.zendy.io/wp-json/zendy-region/v1/highlighted_journal/

Global: Zendy Plus annual

Presents the access of premium content as premium feature

Premium Content

Presents the keyphrase highlighting as premium feature

Keyphrase Highlighting

Presents the summarisation as premium feature

Summarisation

Insights

Presents the pdf analysis as premium feature

PDF Analysis

Presents the zaia usage as premium feature

ZAIA

Global: Zendy Tools annual

Global: Zendy Free Plan

Global: Zendy Tools monthly

Global: Zendy Plus monthly

CXCR4 a G-protein coupled receptor is an important pharmaceutical target in a variety of diseases including HIV and many forms of cancer. CXCR4 is therefore an important pharmaceutical target but besides the cognate agonist SDF-1 only synthetic antagonists/inverse agonists are targeting CXCR4 with pertinent affinities. CXCR4 has important household functions; those antagonists lead to the emergence of significant adverse drug effects. We recently describe nanomolar CXCR4 agonists [1] where the SDF-1 N-terminus was grafting to the inverse agonist T140 [2] (Figure 1). In order to translate these peptidic compounds into peptidomimetic agonists, permitting eventual pharmaceutical applications, the present contribution describes the SAR of the grafted SDF-N-terminus in order to pinpoint the agonist-antagonist transition and to determine the peptidomimetic transition strategies.

Synthetic Agonists for the CXCR4 Receptor: SAR, Signaling Pathways and Peptidomimetic Transition