Structure of PDB 4zz2 Chain A

Receptor sequence

>4zz2A (length=200) Species: 9606 (Homo sapiens)

ARVAVLISGTGSNLQALIDSTREPNSSAQIDIVISNKAAVAGLDKAERAG
IPTRVINHKLYKNRVEFDSAIDLVLEEFSIDIVCLAGFMRILSGPFVQKW
NGKMLNIHPSLLPSFKGSNAHEQALETGVTVTGCTVHFVAEDVDAGQIIL
QEAVPVKRGDTVATLSERVKLAEHKIFPAALQLVASGTVQLGENGKICWV

3D structure

• PDB: 4zz2 6-Substituted Pyrrolo[2,3-d]pyrimidine Thienoyl Regioisomers as Targeted Antifolates for Folate Receptor alpha and the Proton-Coupled Folate Transporter in Human Tumors.
• Chain: A
• Resolution: 1.451 Å

Enzymatic activity

• Catalytic site (original residue number in PDB): N913 H915 T942 D951
• Catalytic site (residue number reindexed from 1): N106 H108 T135 D144
• Enzyme Commision number: 2.1.2.2: phosphoribosylglycinamide formyltransferase 1.
  6.3.3.1: phosphoribosylformylglycinamidine cyclo-ligase.
  6.3.4.13: phosphoribosylamine--glycine ligase.

Interaction with ligand

Site #	Ligand	Ligand chain	Binding residues on receptor (original residue number in PDB)	Binding residues on receptor (residue number reindexed from 1)	Binding affinity
BS01	GAR	A	T817 G818 S819 N820 M896 P916 K977 E980	T10 G11 S12 N13 M89 P109 K170 E173
BS02	3YG	A	R871 F895 M896 R897 I898 L899 G924 S925 V946 A947 V950	R64 F88 M89 R90 I91 L92 G117 S118 V139 A140 V143	MOAD: Ki=9.1nM PDBbind-CN: -logKd/Ki=8.04,Ki=9.1nM BindingDB: Ki=9.1nM,IC50=2.6nM

Gene Ontology

Molecular Function

• GO:0004644 phosphoribosylglycinamide formyltransferase activity

Biological Process

• GO:0006189 'de novo' IMP biosynthetic process
• GO:0009058 biosynthetic process

External links

• PDB: RCSB:4zz2, PDBe:4zz2, PDBj:4zz2
• PDBsum: 4zz2
• PubMed: 26317331
• UniProt: P22102|PUR2_HUMAN Trifunctional purine biosynthetic protein adenosine-3 (Gene Name=GART)