| Structural highlights
2yb9 is a 1 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA.
| | Ligands: | ,
| | Related: | 1qvd, 1y8j, 1r1j, 1dl9, 1r1h, 1dmt, 1r1i |
| Activity: | Glucokinase, with EC number 2.7.1.2 |
| Resources: | FirstGlance, OCA, RCSB, PDBsum |
Publication Abstract from PubMed
Heteroarylalanine derivatives 4 were designed as potential inhibitors of neutral endopeptidase (NEP EC 3.4.24.11). Selectivity over other zinc metalloproteinases was explored through occupation of the S2' subsite within NEP. Structural optimisation led to the identification of 5-phenyl oxazole 4f, a potent and selective NEP inhibitor. A crystal structure of the inhibitor bound complex is reported.
Synthesis and evaluation of heteroarylalanine diacids as potent and selective neutral endopeptidase inhibitors.,Glossop MS, Bazin RJ, Dack KN, Fox DN, Macdonald GA, Mills M, Owen DR, Phillips C, Reeves KA, Ringer TJ, Strang RS, Watson CA Bioorg Med Chem Lett. 2011 Jun 1;21(11):3404-6. Epub 2011 Apr 5. PMID:21515054[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
References
- ↑ Glossop MS, Bazin RJ, Dack KN, Fox DN, Macdonald GA, Mills M, Owen DR, Phillips C, Reeves KA, Ringer TJ, Strang RS, Watson CA. Synthesis and evaluation of heteroarylalanine diacids as potent and selective neutral endopeptidase inhibitors. Bioorg Med Chem Lett. 2011 Jun 1;21(11):3404-6. Epub 2011 Apr 5. PMID:21515054 doi:10.1016/j.bmcl.2011.03.109
|
