Tchem PIEZO1 Piezo-type mechanosensitive ion channel component 1

Protein Summary

Description

Pore-forming subunit of a mechanosensitive non-specific cation channel (PubMed:23479567, PubMed:23695678). Generates currents characterized by a linear current-voltage relationship that are sensitive to ruthenium red and gadolinium. Plays a key role in epithelial cell adhesion by maintaining integrin activation through R-Ras recruitment to the ER, most probably in its activated state, and subsequent stimulation of calpain signaling (PubMed:20016066). In the kidney, may contribute to the detection of intraluminal pressure changes and to urine flow sensing. Acts as shear-stress sensor that promotes endothelial cell organization and alignment in the direction of blood flow through calpain activation (PubMed:25119035). Plays a key role in blood vessel formation and vascular structure in both development and adult physiology (By similarity). The protein encoded by this gene is a mechanically-activated ion channel that links mechanical forces to biological signals. The encoded protein contains 36 transmembrane domains and functions as a homotetramer. Defects in this gene have been associated with dehydrated hereditary stomatocytosis. [provided by RefSeq, Jul 2015]

Uniprot Accession IDs

• Q92508
• A6NHT9
• A7E2B7
• Q0KKZ9

Gene Name

• PIEZO1

Ensembl ID

• ENST00000301015
• ENSP00000301015
• ENSG00000103335

Symbol

• FAM38A
• KIAA0233
• DHS
• Mib
• LMPH3
• FAM38A
• LMPHM6

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
ligand (protein) perturbation	0.83
transcription factor perturbation	0.74
cell line	0.73
transcription factor binding site profile	0.6
small molecule perturbation	0.57

Protein Classes

DTO Classes

Protein / Ion Channel / Mechanical Nociceptor, Piezo (Piezo) Family / Piezo-type Mechanosensitive Ion Channel Component 1

IDG Development Level Summary

Tdark

These are targets about which virtually nothing is known. They do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 534.96   (req: < 5)

Gene RIFs: 196   (req: <= 3)

Antibodies: 142   (req: <= 50)

Tbio

These targets do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 534.96   (req: >= 5)

Gene RIFs: 196   (req: > 3)

Antibodies: 142   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 8

Tchem

Target has at least one ChEMBL compound with an activity cutoff of < 30 nM - AND - satisfies the preceding conditions

Active Ligands: 3

Tclin

Target has at least one approved drug - AND - satisfies the preceding conditions

Active Drug: 0