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Cover Picture: Characterization of C ‐Alkyl Amidines as Bioavailable Covalent Reversible Inhibitors of Human DDAH‐1 (ChemMedChem 1/2011)
Author(s) -
Lluis Matthew,
Wang Yun,
Monzingo Arthur F.,
Fast Walter,
Robertus Jon D.
Publication year - 2011
Publication title -
chemmedchem
Language(s) - English
Resource type - Reports
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201090059
Subject(s) - covalent bond , chemistry , amidine , protein data bank (rcsb pdb) , alkyl , stereochemistry , organic chemistry
The cover picture shows N 5 ‐(1‐iminopentyl)‐L‐ornithine bound to dimethylarginine dimethylaminohydrolase‐1 (DDAH‐1). This inhibitory amidine is a bioavailable dual‐targeted inhibitor of both DDAH‐1 and nitric oxide (NO) synthase, designed to more effectively block biological NO production. An unusual covalent, reversible mode of inhibition is illustrated by the covalent bond formed with wild‐type DDAH‐1 (in blue; PDB code: 3P8E) but not with the C274S variant (in white; PDB code: 3P8P). For more details, see the Full Paper by Walter Fast, Jon D. Robertus et al. on p. 81 ff.