PDBsum entry 6b1e

Hydrolase/hydrolase inhibitor

PDB id: 6b1e

Contents

Protein chains

728 a.a.

Ligands

NAG-NAG ×7

LF7 ×2

NAG ×5

Metals

_NA

Waters ×1877

PDB id:

6b1e

Name:

Hydrolase/hydrolase inhibitor

Title:

The structure of dpp4 in complex with vildagliptin

Structure:

Dipeptidyl peptidase 4. Chain: a, b. Synonym: adabp,adenosine deaminase complexing protein 2,adcp-2, dipeptidyl peptidase iv,dpp iv,t-cell activation antigen cd26,tp103. Engineered: yes. Mutation: yes

Source:

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

Resolution:

1.77Å R-factor: 0.162 R-free: 0.186

Authors:

G.Scapin

Key ref:

J.P.Berger et al. (2018). A comparative study of the binding properties, dipeptidyl peptidase-4 (DPP-4) inhibitory activity and glucose-lowering efficacy of the DPP-4 inhibitors alogliptin, linagliptin, saxagliptin, sitagliptin and vildagliptin in mice. Endocrinol Diabetes Metab, 1, e00002. PubMed id: 30815539 DOI: 10.1002/edm2.2

Date:

18-Sep-17 Release date: 27-Sep-17

Protein chains

P27487  (DPP4_HUMAN) -  Dipeptidyl peptidase 4 from Homo sapiens

Seq: 766 a.a.

Struc: 728 a.a.*

* PDB and UniProt seqs differ at 1 residue position (black cross)

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.

DOI no: 10.1002/edm2.2

Endocrinol Diabetes Metab 1:e00002 (2018)

PubMed id: 30815539

A comparative study of the binding properties, dipeptidyl peptidase-4 (DPP-4) inhibitory activity and glucose-lowering efficacy of the DPP-4 inhibitors alogliptin, linagliptin, saxagliptin, sitagliptin and vildagliptin in mice.

J.P.Berger, R.SinhaRoy, A.Pocai, T.M.Kelly, G.Scapin, Y.D.Gao, K.A.D.Pryor, J.K.Wu, G.J.Eiermann, S.S.Xu, X.Zhang, D.A.Tatosian, A.E.Weber, N.A.Thornberry, R.D.Carr.

ABSTRACT

No abstract given.