PDBsum entry 3tjc

Transferase/transferase inhibitor

PDB id

3tjc

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Contents

			Protein chain

					286 a.a.

			Ligands

					0TP ×2

			Waters ×253

PDB id:

3tjc

Links

Name:

Transferase/transferase inhibitor

Title:

Co-crystal structure of jak2 with thienopyridine 8

Structure:

Tyrosine-protein kinase jak2. Chain: a, b. Fragment: unp residues 837-1132. Synonym: janus kinase 2, jak-2. Engineered: yes

Source:

Homo sapiens. Human. Organism_taxid: 9606. Gene: jak2. Expressed in: spodoptera frugiperda. Expression_system_taxid: 7108

Resolution:

2.40Å

R-factor:

0.265

R-free:

0.275

Authors:

X.Huang

Key ref:

L.B.Schenkel et al. (2011). Discovery of potent and highly selective thienopyridine Janus kinase 2 inhibitors. J Med Chem, 54, 8440-8450. PubMed id: 22087750

Date:

24-Aug-11

Release date:

30-Nov-11

PROCHECK

	Headers

	References

Protein chains

O60674 (JAK2_HUMAN) - Tyrosine-protein kinase JAK2 from Homo sapiens

Seq: Struc:

Seq: Struc:

Seq: Struc:					1132 a.a. 286 a.a.

Key:

PfamA domain

Secondary structure

CATH domain



		Enzyme reactions

Enzyme class:

E.C.2.7.10.2 - non-specific 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

	J Med Chem 54:8440-8450 (2011)
PubMed id: 22087750

Discovery of potent and highly selective thienopyridine Janus kinase 2 inhibitors.
L.B.Schenkel, X.Huang, A.Cheng, H.L.Deak, E.Doherty, R.Emkey, Y.Gu, H.Gunaydin, J.L.Kim, J.Lee, R.Loberg, P.Olivieri, J.Pistillo, J.Tang, Q.Wan, H.L.Wang, S.W.Wang, M.C.Wells, B.Wu, V.Yu, L.Liu, S.Geuns-Meyer.

ABSTRACT

No abstract given.