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

RAP1A (P62834) - Overview - Molecular Target Synopsis

Protein


RAP1A, Ras-related protein Rap-1A
UniProt P62834

Also Known as RAP1A_HUMAN, RAP1A, KREV1

Induces morphological reversion of a cell line transformed by a Ras oncogene. Counteracts the mitogenic function of Ras, at least partly because it can interact with Ras GAPs and RAF in a competitive manner. Together with ITGB1BP1, regulates KRIT1 localization to microtubules and membranes. Plays a role in nerve growth factor (NGF)-induced neurite outgrowth. Plays a role in the regulation of embryonic blood vessel formation. Involved in the establishment of basal endothelial barrier function. May be involved in the regulation of the vascular endothelial growth factor receptor KDR expression at endothelial cell-cell junctions. Found in a complex, at least composed of ITGB1BP1, KRIT1 and RAP1A. Interacts (active GTP-bound form preferentially) with KRIT1 (via C-terminus FERM domain); the interaction does not induce the opening conformation of KRIT1. In its GTP-bound form interacts with PLCE1 and RADIL. Interacts with SGSM1, SGSM2 and SGSM3. Interacts (via GTP-bound active form) with RAPGEF2 (via Ras-associating domain).

4KVG
CRYSTAL STRUCTURE OF RIAM RA-PH DOMAINS IN COMPLEX WITH GTP BOUND RAP1
RCSB/PDB
Inspect Structure
See all 3D Structures for RAP1A

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
129ENSG00000116473ENST00000433097ENSP00000396741

Sub-cellular localization


UniProt: RAP1A is active in the following subcellular-locations: cell junction, cell membrane, cytoplasm, early endosome, perinuclear region.
GO terms: RAP1A is active in the following subcellular-locations: cell junction, cytoplasm, cytosol, early endosome, extracellular exosome, glutamatergic synapse, guanyl-nucleotide exchange factor complex, late endosome, neuron projection, perinuclear region of cytoplasm, phagocytic vesicle, plasma membrane, specific granule membrane.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project RAP1A has gain in 1 cell-lines, loss in 3 cell-lines and no signal in 1001 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: SK_MEL_2, MDA_MB_231, HS578T

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: Pfeiffer, KARPAS-1106P, OVCAR-8

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: NHLF, AG445, NHEK

(see details)

3D Structures


For RAP1A there are:
4 structures (5 chains) solved
4 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


RAP1A has been screened with 4 compounds (5 bioactivities), 2 compounds have bioactivities that show binding affinity of <= 500nM (2 bioactivities). (see details)