cilengitide

Cilengitide (EMD 121974) is a potent integrin inhibitor for the αvβ3/5 receptor (IC50: 4.1/79 nM, in cell-free assays) with approximately 10-fold selectivity against gpIIbIIIa.

Cilengitide is a potent integrin inhibitor for αvβ3 receptor and αvβ5 receptor with IC50 of 4.1 nM and 79 nM in cell-free assays, respectively; ~10-fold selectivity against gpIIbIIIa. Phase 2.

Cilengitide hydrochloride sis the salt form of Cilengitide, a cyclic Arg-Gly-Asp peptide with potential antineoplastic activity. Cilengitide binds to and inhibits the activities of the alpha(v)beta(3) and alpha(v)beta(5) integrins, thereby inhibiting endothelial cell-cell interactions, endothelial cell-matrix interactions, and angiogenesis.

Fmoc-Aeg(N3)-OH is a click chemistry reagent characterized by its azide group that participates in copper-catalyzed azide-alkyne cycloaddition reactions (CuAAc) with molecules containing alkyne groups. This building block, which also reacts in strain-promoted alkyne-azide cycloaddition (SPAAC) with DBCO or BCN group-containing molecules, facilitates the alteration of cytotoxicity through the creation of peptidomimetics such as Cilengitide, Piscidin 1, and MC3, MC4, MC5 receptor agonists. Its incorporation in molecules can lead to conformational restraint in peptidic structures due to amidic nitrogen alkylation, which results in structures such as N-methylated peptides, allows backbone derivatization, and enables the design of macrocycles through intramolecular cross-linking or stabilization of the main chain by intramolecular cyclization. Fmoc-Aeg(N3)-OH is a potential cornerstone for the construction of custom peptide nucleic acids (PNAs) and peptide synthesis.