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

ADCYAP1R1 (P41586) - Overview - Molecular Target Synopsis

Protein


ADCYAP1R1, Pituitary adenylate cyclase-activating polypeptide type I receptor
UniProt P41586

Also Known as PACR_HUMAN, ADCYAP1R1

This is a receptor for PACAP-27 and PACAP-38. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase. May regulate the release of adrenocorticotropin, luteinizing hormone, growth hormone, prolactin, epinephrine, and catecholamine. May play a role in spermatogenesis and sperm motility. Causes smooth muscle relaxation and secretion in the gastrointestinal tract. Interacts (via N-terminal extracellular domain) with ADCYAP1.

3N94 deposition date (2010-05-28)
CRYSTAL STRUCTURE OF HUMAN PITUITARY ADENYLATE CYCLASE 1 RECEPTOR- SHORT N-TERMINAL EXTRACELLULAR DOMAIN
RCSB/PDB
Inspect Structure
See all 3D Structures for ADCYAP1R1

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: ADCYAP1R1 is active in the following subcellular-locations: cell membrane.
GO terms: ADCYAP1R1 is active in the following subcellular-locations: bicellular tight junction, caveola, cell surface, endosome, integral component of plasma membrane, intracellular membrane-bounded organelle, neuron projection, plasma membrane, receptor complex, rough endoplasmic reticulum.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project ADCYAP1R1 has gain in 6 cell-lines, loss in 1 cell-lines and no signal in 998 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: MCF7, LOXIMVI, UACC_62

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: NCI-N417, KELLY, SK-N-DZ

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)

RNA Interference


ADCYAP1R1 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: . (see details)

3D Structures


For ADCYAP1R1 there are:
2 structures (2 chains) solved
1 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


ADCYAP1R1 has been screened with 88 compounds (180 bioactivities), 45 compounds have bioactivities that show binding affinity of <= 500nM (74 bioactivities). (see details)