PDBsum entry 2x9e

Transferase

PDB id: 2x9e

Contents

Protein chain

254 a.a.

Ligands

SVE

Waters ×2

PDB id:

2x9e

Name:

Transferase

Title:

Human mps1 in complex with nms-p715

Structure:

Dual specificity protein kinase ttk. Chain: a. Fragment: kinase domain 514-828. Synonym: mps1, phosphotyrosine picked threonine-protein kinase, pyt. Engineered: yes

Source:

Homo sapiens. Human. Organism_taxid: 9606. Expressed in: trichoplusia ni. Expression_system_taxid: 7111. Expression_system_cell_line: high five.

Resolution:

3.10Å R-factor: 0.215 R-free: 0.306

Authors:

R.Colombo,M.Caldarelli,M.Mennecozzi,M.L.Giorgini,F.Sola,P.Cappella, C.Perrera,S.R.Depaolini,L.Rusconi,U.Cucchi,N.Avanzi,J.A.Bertrand, R.T.Bossi,E.Pesenti,A.Galvani,A.Isacchi,F.Colotta,D.Donati,J.Moll

Key ref:

R.Colombo et al. (2010). Targeting the mitotic checkpoint for cancer therapy with NMS-P715, an inhibitor of MPS1 kinase. Cancer Res, 70, 10255-10264. PubMed id: 21159646 DOI: 10.1158/0008-5472.CAN-10-2101

Date:

17-Mar-10 Release date: 29-Dec-10

Protein chain

P33981  (TTK_HUMAN) -  Dual specificity protein kinase TTK from Homo sapiens

Seq: 857 a.a.

Struc: 254 a.a.

Enzyme reactions

• Enzyme class: E.C.2.7.12.1 - dual-specificity kinase.
• Reaction:
  1. L-seryl-[protein] + ATP = O-phospho-L-seryl-[protein] + ADP + H⁺
  2. L-threonyl-[protein] + ATP = O-phospho-L-threonyl-[protein] + ADP + H⁺
  3. L-tyrosyl-[protein] + ATP = O-phospho-L-tyrosyl-[protein] + ADP + H⁺

Molecule diagrams generated from .mol files obtained from the KEGG ftp site

reference

DOI no: 10.1158/0008-5472.CAN-10-2101

Cancer Res 70:10255-10264 (2010)

PubMed id: 21159646

Targeting the mitotic checkpoint for cancer therapy with NMS-P715, an inhibitor of MPS1 kinase.

R.Colombo, M.Caldarelli, M.Mennecozzi, M.L.Giorgini, F.Sola, P.Cappella, C.Perrera, S.R.Depaolini, L.Rusconi, U.Cucchi, N.Avanzi, J.A.Bertrand, R.T.Bossi, E.Pesenti, A.Galvani, A.Isacchi, F.Colotta, D.Donati, J.Moll.

ABSTRACT

No abstract given.