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

YES1 (P07947) - Overview - Molecular Target Synopsis

Protein


YES1, Tyrosine-protein kinase Yes
Enzyme Classification 2.7.10.2
UniProt P07947

Also Known as YES_HUMAN, YES1, YES

Non-receptor protein tyrosine kinase that is involved in the regulation of cell growth and survival, apoptosis, cell-cell adhesion, cytoskeleton remodeling, and differentiation. Stimulation by receptor tyrosine kinases (RTKs) including EGRF, PDGFR, CSF1R and FGFR leads to recruitment of YES1 to the phosphorylated receptor, and activation and phosphorylation of downstream substrates. Upon EGFR activation, promotes the phosphorylation of PARD3 to favor epithelial tight junction assembly. Participates in the phosphorylation of specific junctional components such as CTNND1 by stimulating the FYN and FER tyrosine kinases at cell-cell contacts. Upon T-cell stimulation by CXCL12, phosphorylates collapsin response mediator protein 2/DPYSL2 and induces T-cell migration. Participates in CD95L/FASLG signaling pathway and mediates AKT-mediated cell migration. Plays a role in cell cycle progression by phosphorylating the cyclin-dependent kinase 4/CDK4 thus regulating the G1 phase. Also involved in G2/M progression and cytokinesis. Interacts with YAP1 and CSF1R (By similarity). Interacts with CTNND1; this interaction allows YES1-mediated activation of FYN and FER and subsequent phosphorylation of CTNND1 (By similarity). Interacts with FASLG.

2HDA
YES SH3 DOMAIN
RCSB/PDB
Inspect Structure
See all 3D Structures for YES1

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
548ENSG00000176105ENST00000577961ENSP00000464380
543ENSG00000176105ENST00000314574, ENST00000584307ENSP00000324740, ENSP00000462468P07947-1

Drugs


YES1 is targeted by Approved Drugs Dasatinib, Vandetanib. (see details)
Dasatinib
Vandetanib

Sub-cellular localization


UniProt: YES1 is active in the following subcellular-locations: cell membrane, centrosome, cytoplasm, cytoskeleton, cytosol, microtubule organizing center.
GO terms: YES1 is active in the following subcellular-locations: actin filament, cytosol, extracellular exosome, extrinsic component of cytoplasmic side of plasma membrane, focal adhesion, glutamatergic synapse, Golgi apparatus, microtubule organizing center, plasma membrane, postsynaptic specialization.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project YES1 has gain in 9 cell-lines, loss in 8 cell-lines and no signal in 988 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: OVCAR_3, HT29, TK_10

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: KYSE-70, Hs 746T, TYK-nu.CP-r

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, HSMM, HMEC

(see details)

RNA Interference


YES1 was reported in the following RNAI studies:

Cell - Large Scale Profiling of Kinase Dependencies in Cancer Cell Lines, the highest RNAi cell lines are: RMGI, SMOV2. (see details)

3D Structures


For YES1 there are:
1 structures (1 chains) solved
0 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


YES1 has been screened with 955 compounds (1628 bioactivities), 90 compounds have bioactivities that show binding affinity of <= 500nM (131 bioactivities). (see details)