PDBsum entry 5u2c

Transcription regulator/inhibitor

PDB id: 5u2c

Contents

Protein chains

120 a.a.

111 a.a.

Ligands

82Y ×2

PDB id:

5u2c

Name:

Transcription regulator/inhibitor

Title:

Brd4 second bromodomain (bd2) in complex with dual pi3 kinase (pi3k) inhibitor sf2558ha

Structure:

Bromodomain-containing protein 4. Chain: a, b. Synonym: protein hunk1. Engineered: yes

Source:

Homo sapiens. Human. Organism_taxid: 9606. Gene: brd4, hunk1. Expressed in: escherichia coli. Expression_system_taxid: 562

Resolution:

3.30Å R-factor: 0.279 R-free: 0.296

Authors:

F.H.Andrews,T.G.Kutateladze

Key ref:

F.H.Andrews et al. (2017). Dual-activity PI3K-BRD4 inhibitor for the orthogonal inhibition of MYC to block tumor growth and metastasis. Proc Natl Acad Sci U S A, 114, E1072. PubMed id: 28137841 DOI: 10.1073/pnas.1613091114

Date:

30-Nov-16 Release date: 08-Feb-17

Protein chain

O60885  (BRD4_HUMAN) -  Bromodomain-containing protein 4 from Homo sapiens

Seq: 1362 a.a.

Struc: 120 a.a.*

Protein chain

O60885  (BRD4_HUMAN) -  Bromodomain-containing protein 4 from Homo sapiens

Seq: 1362 a.a.

Struc: 111 a.a.

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

Enzyme reactions

• Enzyme class: Chains A, B: E.C.?

DOI no: 10.1073/pnas.1613091114

Proc Natl Acad Sci U S A 114:E1072 (2017)

PubMed id: 28137841

Dual-activity PI3K-BRD4 inhibitor for the orthogonal inhibition of MYC to block tumor growth and metastasis.

F.H.Andrews, A.R.Singh, S.Joshi, C.A.Smith, G.A.Morales, J.R.Garlich, D.L.Durden, T.G.Kutateladze.

ABSTRACT

No abstract given.