Targeting Extracellular Cyclophilin A via an Albumin-Binding Cyclosporine A Analogue.
ChemMedChem
; 16(24): 3649-3652, 2021 12 14.
Article
in En
| MEDLINE
| ID: mdl-34595834
ABSTRACT
An albumin-binding CsA analogue 4MCsA was achieved by attachment of a thiol-reactive maleimide group at the side-chain of P4 position of CsA derivative. 4MCsA was semi-synthesized from CsA, and the cell-impermeability of albumin-4MCsA was detected by mass spectrometry and a competitive flow cytometry. 4MCsA exhibits inhibition of chemotaxis activity and inflammation by targeting extracellular CypA without immunosuppressive effect and cellular toxicity. These combined results suggested that 4MCsA can be restricted extracellularly through covalently binding to Cys34 of albumin with its maleimide group, and regulate the functions of cyclophilin A extracellularly.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Cyclosporine
/
Cyclophilin A
/
Albumins
Limits:
Humans
Language:
En
Journal:
ChemMedChem
Journal subject:
FARMACOLOGIA
/
QUIMICA
Year:
2021
Document type:
Article
Affiliation country:
China