Ontology highlight
ABSTRACT:
SUBMITTER: Qian Z
PROVIDER: S-EPMC4174996 | biostudies-literature | 2014 Sep
REPOSITORIES: biostudies-literature
Qian Ziqing Z Dougherty Patrick G PG Liu Tao T Oottikkal Shameema S Hogan Patrick G PG Hadad Christopher M CM Pei Dehua D
Journal of medicinal chemistry 20140904 18
Calcineurin inhibitors such as cyclosporine A and FK506 are effective immunosuppressants but produce severe side effects. Rational modification of a previously reported peptide inhibitor, GPHPVIVITGPHEE (KD ∼ 500 nM), by replacing the two valine residues with tert-leucine and the C-terminal proline with a cis-proline analogue, gave an improved inhibitor ZIZIT-cisPro, which binds to calcineurin with a KD value of 2.6 nM and is more resistant to proteolysis. ...[more]