Target intelligence / Profile preview

Solute carrier organic anion transporter family member 3A1 (OATP3A1)

Target
OATP3A1
Molecular classification
Transporter, Solute carrier family
01

Overview

Solute carrier organic anion transporter family member 3A1 (OATP3A1) is a transmembrane transporter protein of the solute carrier (SLC) superfamily, encoded by the SLCO3A1 gene in humans. It is characterized by broad substrate specificity, transporting various organic anions, including prostaglandins (PGE1, PGE2), bile acids (taurocholate, glycocholate, glycochenodeoxycholate), thyroid hormones (L-thyroxine), and peptide hormones (such as vasopressin). The protein localizes to plasma membranes, including the basal and apical membranes, and may function in a tissue-specific manner. OATP3A1 is notably upregulated in cholestatic liver disease, serving as a bile acid efflux transporter under cholestatic stress, and has been implicated in maintaining bile acid homeostasis. Dysregulation or knockout of this transporter in animal models results in impaired hepatic bile acid clearance and increased susceptibility to liver injury. The gene has also been associated with other disorders, including intestinal perforation and primary hypertrophic osteoarthropathy. At present, there are no therapeutically approved drugs specifically targeting OATP3A1, but drug interactions are possible via altered transport of substrate drugs or endogenous substances[1][2][3][4].

Other names
OATP3A1OATP-DOATP-RP3OATPDOATPRP3Organic anion transporter polypeptide-related protein 3Organic anion-transporting polypeptide DPGE1 transporterSLC21A11Sodium-independent organic anion transporter DSolute carrier family 21 member 11Androgen regulated protein 1
02

Mechanism of action

Inhibition or modulation of substrate (organic anion, prostaglandin, bile acid, thyroid hormone) transport across cell membranes\nPossible impact on bile acid homeostasis and prostaglandin-mediated signaling

03

Biological functions

Organic anion transmembrane transportProstaglandin transmembrane transportBile acid efflux transportRegulation of NF-kappaB activityPositive regulation of MAPK cascadeTransport across blood-brain barrier
04

Disease associations

CholestasisIntestinal perforationPrimary hypertrophic osteoarthropathyLiver injury (related to bile acid transport dysfunction)
05

Safety considerations

Disruption may lead to impaired bile acid efflux and liver injury during cholestasis or other hepatic dysfunctionsPossible drug-drug interactions via organic anion transport competition
06

Interacting drugs

Prostaglandin E1

6 more in the full profile.

07

Biomarkers

Increased hepatic OATP3A1 expression (biomarker for cholestasis adaptation)SLCO3A1 gene/protein detection in liver tissue

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