Design, synthesis, structural analysis and biochemical studies of stapled AIF(370-394) analogues as ligand of CypA

• Published in: Biochimica et biophysica acta. General subjects Vol. 1864; no. 12; p. 129717
• Main Authors: Monti, Alessandra, Sturlese, Mattia, Caporale, Andrea, Roger, Jessica De Almeida, Mascanzoni, Fabiola, Ruvo, Menotti, Doti, Nunzianna
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 01.12.2020
• Subjects: AIF(370–394) stapled peptide; AIF/CypA complex; apoptosis; Apoptosis Inducing Factor - chemistry; Apoptosis Inducing Factor - metabolism; calorimetry; chromatin; Circular dichroism (CD); circular dichroism spectroscopy; Click chemistry; cyclophilin A; Cyclophilin A - metabolism; disulfides; DNA; Drug Design; Enspire label free; Humans; Isothermal Titration Calorimetry (ITC); Ligands; Molecular Docking Simulation; neurodegenerative diseases; neurons; Neuroprotective Agents - chemical synthesis; Neuroprotective Agents - chemistry; Neuroprotective Agents - pharmacology; neuroprotective effect; NMR and molecular modeling analysis; nuclear magnetic resonance spectroscopy; peptides; Peptides - chemical synthesis; Peptides - chemistry; Peptides - pharmacology; therapeutics; thermodynamics; titration; Enspire label free; Circular dichroism (CD); AIF/CypA complex; Click chemistry; Isothermal Titration Calorimetry (ITC); NMR and molecular modeling analysis; AIF(370–394) stapled peptide

The neuronal apoptotic process requires the nuclear translocation of Apoptosis Inducing Factor (AIF) in complex with Cyclophilin A (CypA) with consequent chromatin condensation and DNA degradation events. Targeting CypA by delivering an AIF-blocking peptide (AIF(370–394)) provides a significant neur...