PDBsum entry 4r7i

Transferase/transferase inhibitor

PDB id

4r7i

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Contents

			Protein chain

					290 a.a.

			Ligands

					STI

			Waters ×55

PDB id:

4r7i

Links

Name:

Transferase/transferase inhibitor

Title:

Crystal structure of fms kinase domain with a small molecular inhibitor, gleevec

Structure:

Macrophage colony-stimulating factor 1 receptor. Chain: a. Fragment: fms kinase domain with kid (unp residues 538-919). Synonym: csf-1 receptor, csf-1-r, csf-1r, m-csf-r, proto-oncogenE C- fms. Engineered: yes. Mutation: yes

Source:

Homo sapiens. Human. Organism_taxid: 9606. Gene: csf1r, fms. Expressed in: spodoptera frugiperda. Expression_system_taxid: 7108.

Resolution:

2.75Å

R-factor:

0.202

R-free:

0.236

Authors:

Y.Zhang,C.Zhang

Key ref:

W.D.Tap et al. (2015). Structure-Guided Blockade of CSF1R Kinase in Tenosynovial Giant-Cell Tumor. N Engl J Med, 373, 428-437. PubMed id: 26222558 DOI: 10.1056/NEJMoa1411366

Date:

27-Aug-14

Release date:

12-Aug-15

PROCHECK

	Headers

	References

Protein chain

P07333 (CSF1R_HUMAN) - Macrophage colony-stimulating factor 1 receptor from Homo sapiens

Seq: Struc:

Seq: Struc:					972 a.a. 290 a.a.*

Key:

PfamA domain

Secondary structure

CATH domain

* PDB and UniProt seqs differ at 3 residue positions (black crosses)



		Enzyme reactions

Enzyme class:

E.C.2.7.10.1 - receptor protein-tyrosine kinase.

[IntEnz] [ExPASy] [KEGG] [BRENDA]

Reaction:

L-tyrosyl-[protein] + ATP = O-phospho-L-tyrosyl-[protein] + ADP + H⁺

L-tyrosyl-[protein]	+	ATP	=	O-phospho-L-tyrosyl-[protein]	+	ADP	+	H(+)

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

Added reference

DOI no: 10.1056/NEJMoa1411366	N Engl J Med 373:428-437 (2015)
PubMed id: 26222558

Structure-Guided Blockade of CSF1R Kinase in Tenosynovial Giant-Cell Tumor.

W.D.Tap, Z.A.Wainberg, S.P.Anthony, P.N.Ibrahim, C.Zhang, J.H.Healey, B.Chmielowski, A.P.Staddon, A.L.Cohn, G.I.Shapiro, V.L.Keedy, A.S.Singh, I.Puzanov, E.L.Kwak, A.J.Wagner, D.D.Von Hoff, G.J.Weiss, R.K.Ramanathan, J.Zhang, G.Habets, Y.Zhang, E.A.Burton, G.Visor, L.Sanftner, P.Severson, H.Nguyen, M.J.Kim, A.Marimuthu, G.Tsang, R.Shellooe, C.Gee, B.L.West, P.Hirth, K.Nolop, M.van de Rijn, H.H.Hsu, C.Peterfy, P.S.Lin, S.Tong-Starksen, G.Bollag.

ABSTRACT

No abstract given.