PDBsum entry 5tb6

Transferase

PDB id: 5tb6

Contents

Protein chain

119 a.a.

Ligands

77X

EDO

Waters ×157

PDB id:

5tb6

Name:

Transferase

Title:

Structure of bromodomain of crebbp with a pyrazolo[4,3-c]pyridin fragment

Structure:

Creb-binding protein. Chain: a. Engineered: yes

Source:

Homo sapiens. Human. Organism_taxid: 9606. Gene: crebbp, cbp. Expressed in: escherichia coli. Expression_system_taxid: 469008.

Resolution:

1.79Å R-factor: 0.175 R-free: 0.244

Authors:

P.Filippakopoulos,S.Picaud,S.Knapp,F.Von Delft,C.Bountra, C.H.Arrowsmith,A.Edwards,Structural Genomics Consortium (Sgc)

Key ref:

I.Navratilova et al. (2016). Discovery of New Bromodomain Scaffolds by Biosensor Fragment Screening. Acs Med Chem Lett, 7, 1213-1218. PubMed id: 27994766 DOI: 10.1021/acsmedchemlett.6b00154

Date:

11-Sep-16 Release date: 12-Oct-16

Protein chain

Q92793  (CBP_HUMAN) -  CREB-binding protein from Homo sapiens

Seq: 2442 a.a.

Struc: 119 a.a.*

* PDB and UniProt seqs differ at 2 residue positions (black crosses)

Enzyme reactions

• Enzyme class 1: E.C.2.3.1.- - ?????
• Enzyme class 2: E.C.2.3.1.48 - histone acetyltransferase.
• Reaction: L-lysyl-[protein] + acetyl-CoA = N₆-acetyl-L-lysyl-[protein] + CoA + H⁺

Note, where more than one E.C. class is given (as above), each may correspond to a different protein domain or, in the case of polyprotein precursors, to a different mature protein.

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

Added reference

DOI no: 10.1021/acsmedchemlett.6b00154

Acs Med Chem Lett 7:1213-1218 (2016)

PubMed id: 27994766

Discovery of New Bromodomain Scaffolds by Biosensor Fragment Screening.

I.Navratilova, T.Aristotelous, S.Picaud, A.Chaikuad, S.Knapp, P.Filappakopoulos, A.L.Hopkins.

ABSTRACT

No abstract given.