| Structural highlights
1h5u is a 1 chain structure with sequence from Oryctolagus cuniculus. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
| | Ligands: | , ,
| | Related: | 1a8i, 1abb, 1axr, 1b4d, 1bx3, 1c50, 1c8k, 1c8l, 1e1y, 1fs4, 1ftq, 1ftw, 1fty, 1fu4, 1fu7, 1fu8, 1gfz, 1gg8, 1ggn, 1gpa, 1gpb, 1gpy, 1hlf, 1noi, 1noj, 1nok, 1pyg, 2amv, 2gpa, 2gpb, 2gpn, 2pri, 2prj, 2skc, 2skd, 2ske, 3amv, 3gpb, 4gpb, 5gpb, 6gpb, 7gpb, 8gpb, 9gpb |
| Activity: | Phosphorylase, with EC number 2.4.1.1 |
| Resources: | FirstGlance, OCA, RCSB, PDBsum |
Evolutionary Conservation
Check, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf.
Publication Abstract from PubMed
CP320626, a potential antidiabetic drug, inhibits glycogen phosphorylase in synergism with glucose. To elucidate the structural basis of synergistic inhibition, we determined the structure of muscle glycogen phosphorylase b (MGPb) complexed with both glucose and CP320626 at 1.76 A resolution, and refined to a crystallographic R value of 0.211 (R(free)=0.235). CP320626 binds at a novel allosteric site, which is some 33 A from the catalytic site, where glucose binds. The high resolution structure allows unambiguous definition of the conformation of the 1-acetyl-4-hydroxy-piperidine ring supported by theoretical energy calculations. Both CP320626 and glucose promote the less active T-state, thereby explaining their synergistic inhibition. Structural comparison of MGPb--glucose--CP320626 complex with liver glycogen phosphorylase a (LGPa) complexed with a related compound (CP403700) show that the ligand binding site is conserved in LGPa.
The 1.76 A resolution crystal structure of glycogen phosphorylase B complexed with glucose, and CP320626, a potential antidiabetic drug.,Oikonomakos NG, Zographos SE, Skamnaki VT, Archontis G Bioorg Med Chem. 2002 May;10(5):1313-9. PMID:11886794[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ Oikonomakos NG, Zographos SE, Skamnaki VT, Archontis G. The 1.76 A resolution crystal structure of glycogen phosphorylase B complexed with glucose, and CP320626, a potential antidiabetic drug. Bioorg Med Chem. 2002 May;10(5):1313-9. PMID:11886794
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