PDBsum entry 8w3b

Transferase/transferase inhibitor

PDB id: 8w3b

Contents

Protein chains

279 a.a.

294 a.a.

Ligands

TZ0 ×4

SO4 ×3

Waters ×149

PDB id:

8w3b

Name:

Transferase/transferase inhibitor

Title:

Tas-120 covalent structure with fgfr2 molecular brake mutant

Structure:

Fibroblast growth factor receptor 2. Chain: a, b, c, d. Synonym: fgfr-2,k-sam,kgfr,keratinocyte growth factor receptor. Engineered: yes. Mutation: yes

Source:

Homo sapiens. Human. Organism_taxid: 9606. Gene: fgfr2, bek, kgfr, ksam. Expressed in: escherichia coli. Expression_system_taxid: 562

Resolution:

2.23Å R-factor: 0.292 R-free: 0.312

Authors:

I.D.Hoffman,K.J.Nelson,D.C.Bensen,J.B.Bailey

Key ref:

L.Goyal et al. A model for decoding resistance in precision oncology acquired resistance to fgfr inhibitors in cholangiocarcinoma.. Ann oncol, . PubMed id: 39706336

Date:

22-Feb-24 Release date: 01-Jan-25

Protein chains

P21802  (FGFR2_HUMAN) -  Fibroblast growth factor receptor 2 from Homo sapiens

Seq: 821 a.a.

Struc: 279 a.a.*

Protein chain

P21802  (FGFR2_HUMAN) -  Fibroblast growth factor receptor 2 from Homo sapiens

Seq: 821 a.a.

Struc: 294 a.a.*

* PDB and UniProt seqs differ at 4 residue positions (black crosses)

Enzyme reactions

• Enzyme class: Chains A, B, C, D: E.C.2.7.10.1 - receptor 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