Structure of PDB 4pxm Chain A

Receptor sequence

>4pxmA (length=230) Species: 9606 (Homo sapiens) [Search protein sequence]

ALSLTADQMVSALLDAEPPILYSEYDPTRPFSEASMMGLLTNLADRELVH
MINWAKRVPGFVDLTLHDQVHLLECAWLEILMIGLVWRSMEHPGKLLFAP
NLLLDRNQGKCVEGMVEIFDMLLATSSRFRMMNLQGEEFVCLKSIILLNS
GVYDHIHRVLDKITDTLIHLMAKAGLTLQQQHQRLAQLLLILSHIRHMSN
KGMEHLYSMKCKNVVPLYGLLLEMLDAHRL

3D structure

PDB

4pxm Estrogen receptor alpha somatic mutations Y537S and D538G confer breast cancer endocrine resistance by stabilizing the activating function-2 binding conformation.

Chain

Resolution

1.9 Å

3D
structure

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Enzymatic activity

Enzyme Commision number

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	peptide	A	I358 K362 L372 V376 G538 E542	I52 K56 L66 V70 G219 E223
BS02	EST	A	E353 L387 F404 G521 H524 L525	E47 L81 F98 G202 H205 L206	PDBbind-CN: -logKd/Ki=8.89,Kd=1.3nM BindingDB: IC50=1.3nM,Kd=0.2nM,EC50=0.75nM,Ki=0.21nM

External links

PDB	RCSB:4pxm, PDBe:4pxm, PDBj:4pxm
PDBsum	4pxm
PubMed	26836308
UniProt	P03372\|ESR1_HUMAN Estrogen receptor (Gene Name=ESR1)

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