PDBsum entry 3rvg

Transferase/transferase inhibitor

PDB id: 3rvg

Contents

Protein chain

287 a.a.

Ligands

17P

Waters ×7

PDB id:

3rvg

Name:

Transferase/transferase inhibitor

Title:

Crystals structure of jak2 with a 1-amino-5h-pyrido[4,3-b]indol-4- carboxamide inhibitor

Structure:

Tyrosine-protein kinase jak2. Chain: a. Fragment: unp residues 835-1132. 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:

2.50Å R-factor: 0.225 R-free: 0.300

Authors:

J.Lim,B.Taoka,R.D.Otte,K.Spencer,C.J.Dinsmore,M.D.Altman,G.Chan, C.Rosenstein,S.Sharma,H.P.Su,A.A.Szewczak,L.Xu,H.Yin,J.Zugay-Murphy, C.G.Marshall,J.R.Young

Key ref:

J.Lim et al. (2011). Discovery of 1-amino-5H-pyrido[4,3-b]indol-4-carboxamide inhibitors of Janus kinase 2 (JAK2) for the treatment of myeloproliferative disorders. J Med Chem, 54, 7334-7349. PubMed id: 21942426

Date:

06-May-11 Release date: 21-Mar-12

Protein chain

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

Seq: 1132 a.a.

Struc: 287 a.a.

Enzyme reactions

• Enzyme class: E.C.2.7.10.2 - non-specific protein-tyrosine kinase.
• Reaction: 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 54:7334-7349 (2011)

PubMed id: 21942426

Discovery of 1-amino-5H-pyrido[4,3-b]indol-4-carboxamide inhibitors of Janus kinase 2 (JAK2) for the treatment of myeloproliferative disorders.

J.Lim, B.Taoka, R.D.Otte, K.Spencer, C.J.Dinsmore, M.D.Altman, G.Chan, C.Rosenstein, S.Sharma, H.P.Su, A.A.Szewczak, L.Xu, H.Yin, J.Zugay-Murphy, C.G.Marshall, J.R.Young.

ABSTRACT

No abstract given.