Molecular Target Synopsis
Overview
Domains and Structures
Drugs and Clinical Candidates
Druggability
Chemistry
Ligand Efficiency Plot
Pathways
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
RNAi
Mutations
Germline Genetics

APLNR (P35414) - Overview - Molecular Target Synopsis

Protein


APLNR, Apelin receptor
UniProt P35414

Also Known as APJ_HUMAN, APLNR, AGTRL1, APJ

Receptor for apelin receptor early endogenous ligand (APELA) and apelin (APLN) hormones coupled to G proteins that inhibit adenylate cyclase activity (PubMed:11090199, PubMed:25639753, PubMed:28137936). Plays a key role in early development such as gastrulation, blood vessels formation and heart morphogenesis by acting as a receptor for APELA hormone (By similarity). May promote angioblast migration toward the embryonic midline, i.e. the position of the future vessel formation, during vasculogenesis (By similarity). Promotes sinus venosus (SV)-derived endothelial cells migration into the developing heart to promote coronary blood vessel development (By similarity). Plays also a role in various processes in adults such as regulation of blood vessel formation, blood pressure, heart contractility and heart failure (PubMed:25639753, PubMed:28137936)., (Microbial infection) Alternative coreceptor with CD4 for HIV-1 infection; may be involved in the development of AIDS dementia (PubMed:11090199).

5VBL
STRUCTURE OF APELIN RECEPTOR IN COMPLEX WITH AGONIST PEPTIDE
RCSB/PDB
Inspect Structure
See all 3D Structures for APLNR

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
450ENSG00000134817ENST00000606794ENSP00000475344
408ENSG00000134817ENST00000257254ENSP00000257254
380P35414-1

Sub-cellular localization


UniProt: APLNR is active in the following subcellular-locations: cell membrane.
GO terms: APLNR is active in the following subcellular-locations: integral component of plasma membrane, plasma membrane.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project APLNR has gain in 1 cell-lines, loss in 0 cell-lines and no signal in 1002 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: SK_OV_3, MCF7, NCI_H460

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: RPMI 2650, SK-N-FI, SET-2

In Array Express (RNA-seq of long poly adenylated RNA and long non poly adenylated RNA from ENCODE cell lines), the highest expressing cell lines are: SK-N-SH, NHLF, HSMM

(see details)

3D Structures


For APLNR there are:
5 structures (5 chains) solved
1 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


APLNR has been screened with 208 compounds (368 bioactivities), 69 compounds have bioactivities that show binding affinity of <= 500nM (181 bioactivities). (see details)