PDBsum entry 3g0c

Hydrolase/hydrolase inhibitor

PDB id: 3g0c

Contents

Protein chain

723 a.a. *

Ligands

NAG-NAG ×5

RUF ×4

NAG ×12

Waters ×774

* Residue conservation analysis

PDB id:

3g0c

Name:

Hydrolase/hydrolase inhibitor

Title:

Crystal structure of dipeptidyl peptidase iv in complex with a pyrimidinedione inhibitor 1

Structure:

Dipeptidyl peptidase 4. Chain: a, b, c, d. Fragment: unp residues 39-766. Synonym: dipeptidyl peptidase iv, dpp iv, t-cell activation antigen cd26, tp103, adenosine deaminase complexing protein 2, adabp, dipeptidyl peptidase 4 membrane form, dipeptidyl peptidase iv membrane form, dipeptidyl peptidase 4 soluble form, dipeptidyl peptidase iv soluble form. Engineered: yes

Source:

Homo sapiens. Human. Organism_taxid: 9606. Gene: adcp2, cd26, dpp4. Expressed in: spodoptera frugiperda. Expression_system_taxid: 7108. Expression_system_cell_line: sf9.

Resolution:

2.69Å R-factor: 0.198 R-free: 0.248

Authors:

Z.Zhang,M.B.Wallace,J.Feng,J.A.Stafford,S.W.Kaldor,L.Shi,R.J.Skene, K.Aertgeerts,B.Lee,A.Jennings,R.Xu,D.Kassel,D.R.Webb,S.L.Gwaltney

Key ref:

Z.Zhang et al. (2011). Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV. J Med Chem, 54, 510-524. PubMed id: 21186796

Date:

27-Jan-09 Release date: 16-Feb-10

Protein chains

P27487  (DPP4_HUMAN) -  Dipeptidyl peptidase 4 from Homo sapiens

Seq: 766 a.a.

Struc: 723 a.a.

Enzyme reactions

• Enzyme class: E.C.3.4.14.5 - dipeptidyl-peptidase Iv.
• Reaction: Release of an N-terminal dipeptide, Xaa-Xbb-|-Xcc, from a polypeptide, preferentially when Xbb is Pro, provided Xcc is neither Pro nor hydroxyproline.

J Med Chem 54:510-524 (2011)

PubMed id: 21186796

Design and synthesis of pyrimidinone and pyrimidinedione inhibitors of dipeptidyl peptidase IV.

Z.Zhang, M.B.Wallace, J.Feng, J.A.Stafford, R.J.Skene, L.Shi, B.Lee, K.Aertgeerts, A.Jennings, R.Xu, D.B.Kassel, S.W.Kaldor, M.Navre, D.R.Webb, S.L.Gwaltney.

ABSTRACT

No abstract given.