Detail Information of Exogenous Modulation

General Information of Drug Transporter (DT)
DT ID	DTD0029 Transporter Info
Gene Name	SLCO1A2
Transporter Name	Organic anion transporting polypeptide 1A2
Gene ID	6579
UniProt ID	P46721

Exogenous factors (drugs, dietary constituents, etc.) Modulation of This DT (EGM)
Chemical Compound
DT Modulation1	SLCO1A2 protein affects the uptake of Saquinavir			[52]
Regulation Mechanism				Transcription Factor Info
DT Modulation1	Verapamil inhibits the reaction SLCO1A2 protein results in increased uptake of Quercetin			[50]
Regulation Mechanism				Transcription Factor Info
DT Modulation1	NOG protein co-treated with Valproic Acid co-treated with dorsomorphin co-treated with 4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide results in increased expression of SLCO1A2 mRNA			[24]
Regulation Mechanism				Transcription Factor Info
DT Modulation2	Valproic Acid affects the expression of SLCO1A2 mRNA			[55]
Regulation Mechanism				Transcription Factor Info
DT Modulation3	Valproic Acid results in increased expression of SLCO1A2 mRNA			[35]
Regulation Mechanism				Transcription Factor Info
DT Modulation1	NOG protein co-treated with Phenylmercuric Acetate co-treated with dorsomorphin co-treated with 4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide results in decreased expression of SLCO1A2 mRNA			[24]
Regulation Mechanism				Transcription Factor Info
3-iodothyronamine	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	SLCO1A2 mRNA affects the uptake of 3-iodothyronamine			[39]
Regulation Mechanism				Transcription Factor Info
4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide	2 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	NOG protein co-treated with Phenylmercuric Acetate co-treated with dorsomorphin co-treated with 4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide results in decreased expression of SLCO1A2 mRNA			[24]
Regulation Mechanism				Transcription Factor Info
DT Modulation2	NOG protein co-treated with Valproic Acid co-treated with dorsomorphin co-treated with 4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide results in increased expression of SLCO1A2 mRNA			[24]
Regulation Mechanism				Transcription Factor Info
7-hydroxymethotrexate	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	7-hydroxymethotrexate inhibits the reaction SLCO1A2 mRNA results in increased import of estrone sulfate			[40]
Regulation Mechanism				Transcription Factor Info
artemisinin	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	artemisinin inhibits the reaction SLCO1A2 protein results in increased uptake of estrone sulfate			[42]
Regulation Mechanism				Transcription Factor Info
Asbestos, Serpentine	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Asbestos, Serpentine results in increased methylation of SLCO1A2 5' UTR			[43]
Regulation Mechanism				Transcription Factor Info
Benzo(a)pyrene	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Benzo(a)pyrene affects the methylation of SLCO1A2 5' UTR			[44]
Regulation Mechanism				Transcription Factor Info
Chloroquine	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Chloroquine inhibits the reaction SLCO1A2 protein results in increased uptake of estrone sulfate			[42]
Regulation Mechanism				Transcription Factor Info
Cholecalciferol	7 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Cholecalciferol binds to VDR protein which results in increased expression of SLCO1A2 mRNA			[20]
Regulation Mechanism				Transcription Factor Info
DT Modulation2	Cholecalciferol co-treated with Tretinoin promotes the reaction VDR protein binds to RXRA protein which binds to SLCO1A2 promoter			[20]
Regulation Mechanism				Transcription Factor Info
DT Modulation3	Cholecalciferol promotes the reaction VDR protein binds to SLCO1A2 promoter			[20]
Regulation Mechanism				Transcription Factor Info
DT Modulation4	Cholecalciferol promotes the reaction VDR protein binds to SLCO1A2 promoter which results in increased expression of SLCO1A2 mRNA			[20]
Regulation Mechanism				Transcription Factor Info
DT Modulation5	Cholecalciferol results in increased expression of SLCO1A2 mRNA			[20]
Regulation Mechanism				Transcription Factor Info
DT Modulation6	Cholecalciferol results in increased expression of SLCO1A2 protein			[20]
Regulation Mechanism				Transcription Factor Info
DT Modulation7	VDR protein affects the reaction Cholecalciferol results in increased expression of SLCO1A2 mRNA			[20]
Regulation Mechanism				Transcription Factor Info
diosmetin	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	diosmetin inhibits the reaction SLCO1A2 protein results in increased uptake of Rosuvastatin Calcium			[45]
Regulation Mechanism				Transcription Factor Info
dorsomorphin	2 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	NOG protein co-treated with Phenylmercuric Acetate co-treated with dorsomorphin co-treated with 4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide results in decreased expression of SLCO1A2 mRNA			[24]
Regulation Mechanism				Transcription Factor Info
DT Modulation2	NOG protein co-treated with Valproic Acid co-treated with dorsomorphin co-treated with 4-(5-benzo(1,3)dioxol-5-yl-4-pyridin-2-yl-1H-imidazol-2-yl)benzamide results in increased expression of SLCO1A2 mRNA			[24]
Regulation Mechanism				Transcription Factor Info
estrone sulfate	15 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	7-hydroxymethotrexate inhibits the reaction SLCO1A2 mRNA results in increased import of estrone sulfate			[40]
Regulation Mechanism				Transcription Factor Info
DT Modulation2	artemisinin inhibits the reaction SLCO1A2 protein results in increased uptake of estrone sulfate			[42]
Regulation Mechanism				Transcription Factor Info
DT Modulation3	Chloroquine inhibits the reaction SLCO1A2 protein results in increased uptake of estrone sulfate			[42]
Regulation Mechanism				Transcription Factor Info
DT Modulation4	Mefloquine inhibits the reaction SLCO1A2 protein results in increased uptake of estrone sulfate			[42]
Regulation Mechanism				Transcription Factor Info
DT Modulation5	Methotrexate inhibits the reaction SLCO1A2 mRNA results in increased import of estrone sulfate			[40]
Regulation Mechanism				Transcription Factor Info
DT Modulation6	naringin inhibits the reaction SLCO1A2 protein alternative form results in increased uptake of estrone sulfate			[46]
Regulation Mechanism				Transcription Factor Info
DT Modulation7	naringin inhibits the reaction SLCO1A2 protein results in increased transport of estrone sulfate			[46]
Regulation Mechanism				Transcription Factor Info
DT Modulation8	perfluorodecanoic acid inhibits the reaction SLCO1A2 protein results in increased import of estrone sulfate			[47]
Regulation Mechanism				Transcription Factor Info
DT Modulation9	Pyrimethamine inhibits the reaction SLCO1A2 protein results in increased uptake of estrone sulfate			[42]
Regulation Mechanism				Transcription Factor Info
DT Modulation10	Quinine inhibits the reaction SLCO1A2 protein results in increased uptake of estrone sulfate			[42]
Regulation Mechanism				Transcription Factor Info
DT Modulation11	SLCO1A2 mRNA results in increased import of estrone sulfate			[40]
Regulation Mechanism				Transcription Factor Info
DT Modulation12	SLCO1A2 protein alternative form results in increased uptake of estrone sulfate			[46]
Regulation Mechanism				Transcription Factor Info
DT Modulation13	SLCO1A2 protein results in increased import of estrone sulfate			[47]
Regulation Mechanism				Transcription Factor Info
DT Modulation14	SLCO1A2 protein results in increased transport of estrone sulfate			[46]
Regulation Mechanism				Transcription Factor Info
DT Modulation15	SLCO1A2 protein results in increased uptake of estrone sulfate			[42]
Regulation Mechanism				Transcription Factor Info
Hydroxyurea	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	SLCO1A2 protein results in increased uptake of Hydroxyurea			[48]
Regulation Mechanism				Transcription Factor Info
lithocholic acid acetate	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	lithocholic acid acetate results in increased expression of SLCO1A2 mRNA			[20]
Regulation Mechanism				Transcription Factor Info
Mefloquine	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Mefloquine inhibits the reaction SLCO1A2 protein results in increased uptake of estrone sulfate			[42]
Regulation Mechanism				Transcription Factor Info
Methotrexate	4 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Methotrexate inhibits the reaction SLCO1A2 mRNA results in increased import of estrone sulfate			[40]
Regulation Mechanism				Transcription Factor Info
DT Modulation2	SLCO1A2 gene polymorphism affects the susceptibility to Methotrexate			[40]
Regulation Mechanism				Transcription Factor Info
DT Modulation3	SLCO1A2 mRNA results in increased import of Methotrexate			[40]
Regulation Mechanism				Transcription Factor Info
DT Modulation4	SLCO1A2 polymorphism affects the susceptibility to Methotrexate			[49]
Regulation Mechanism				Transcription Factor Info
methylmercuric chloride	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	methylmercuric chloride results in decreased expression of SLCO1A2 mRNA			[27]
Regulation Mechanism				Transcription Factor Info
naringin	4 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	naringin inhibits the reaction SLCO1A2 protein alternative form results in increased uptake of estrone sulfate			[46]
Regulation Mechanism				Transcription Factor Info
DT Modulation2	naringin inhibits the reaction SLCO1A2 protein results in increased transport of estrone sulfate			[46]
Regulation Mechanism				Transcription Factor Info
DT Modulation3	naringin inhibits the reaction SLCO1A2 protein results in increased uptake of Quercetin			[50]
Regulation Mechanism				Transcription Factor Info
DT Modulation4	naringin inhibits the reaction SLCO1A2 protein results in increased uptake of Quinine			[42]
Regulation Mechanism				Transcription Factor Info
perfluorodecanoic acid	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	perfluorodecanoic acid inhibits the reaction SLCO1A2 protein results in increased import of estrone sulfate			[47]
Regulation Mechanism				Transcription Factor Info
Pyrimethamine	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Pyrimethamine inhibits the reaction SLCO1A2 protein results in increased uptake of estrone sulfate			[42]
Regulation Mechanism				Transcription Factor Info
Quinine	3 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	naringin inhibits the reaction SLCO1A2 protein results in increased uptake of Quinine			[42]
Regulation Mechanism				Transcription Factor Info
DT Modulation2	Quinine inhibits the reaction SLCO1A2 protein results in increased uptake of estrone sulfate			[42]
Regulation Mechanism				Transcription Factor Info
DT Modulation3	SLCO1A2 protein results in increased uptake of Quinine			[42]
Regulation Mechanism				Transcription Factor Info
Rosuvastatin Calcium	2 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	diosmetin inhibits the reaction SLCO1A2 protein results in increased uptake of Rosuvastatin Calcium			[45]
Regulation Mechanism				Transcription Factor Info
DT Modulation2	SLCO1A2 protein results in increased uptake of Rosuvastatin Calcium			[45]
Regulation Mechanism				Transcription Factor Info
sodium arsenite	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	sodium arsenite affects the methylation of SLCO1A2 gene			[53]
Regulation Mechanism				Transcription Factor Info
Sulfobromophthalein	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Sulfobromophthalein inhibits the reaction SLCO1A2 protein results in increased uptake of Quercetin			[50]
Regulation Mechanism				Transcription Factor Info
testosterone enanthate	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	testosterone enanthate affects the expression of SLCO1A2 mRNA			[22]
Regulation Mechanism				Transcription Factor Info
theaflavin-3,3'-digallate	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	theaflavin-3,3'-digallate affects the expression of SLCO1A2 mRNA			[54]
Regulation Mechanism				Transcription Factor Info
Tretinoin	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Cholecalciferol co-treated with Tretinoin promotes the reaction VDR protein binds to RXRA protein which binds to SLCO1A2 promoter			[20]
Regulation Mechanism				Transcription Factor Info
trospium chloride	3 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	SLCO1A2 protein results in increased metabolism of trospium chloride			[46]
Regulation Mechanism				Transcription Factor Info
DT Modulation2	trospium chloride results in decreased activity of SLCO1A2 protein			[46]
Regulation Mechanism				Transcription Factor Info
DT Modulation3	trospium chloride results in decreased activity of SLCO1A2 protein alternative form			[46]
Regulation Mechanism				Transcription Factor Info
zearalenol	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	zearalenol results in decreased activity of SLCO1A2 protein			[56]
Regulation Mechanism				Transcription Factor Info
Mycotoxins
Aflatoxin B1	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Aflatoxin B1 results in decreased methylation of SLCO1A2 gene			[41]
Regulation Mechanism				Transcription Factor Info
ochratoxin A	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	SLCO1A2 protein results in increased uptake of ochratoxin A			[51]
Regulation Mechanism				Transcription Factor Info
Zearalenone	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Zearalenone results in decreased activity of SLCO1A2 protein			[56]
Regulation Mechanism				Transcription Factor Info
Approved Drug
Rifampicin	3 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Rifampicin inhibits the transportation of Bromsulphthalein by SLCO1A2 (Ki = 51 microM)			[1]
Affected Drug/Substrate	Bromsulphthalein	Modulation Type	Inhibition
Cell System	Oocytes-OATP1A2
DT Modulation2	Rifampicin inhibits the transportation of Sulfobromophthalein by SLCO1A2 (Ki = 51 microM)			[1]
Affected Drug/Substrate	Sulfobromophthalein	Modulation Type	Inhibition
Cell System	Oocytes-OATP1A2
DT Modulation3	Rifampicin induces the activity of SLCO1A2			[4], [5]
Rifamycin SV	2 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Rifamycin SV inhibits the transportation of Bromsulphthalein by SLCO1A2 (Ki = 11 microM)			[1]
Affected Drug/Substrate	Bromsulphthalein	Modulation Type	Inhibition
Cell System	Oocytes-OATP1A2
DT Modulation2	Rifamycin SV inhibits the activity of SLCO1A2			[4]
Ritonavir	2 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Ritonavir inhibits the transportation of Fexofenadine by SLCO1A2 (IC50 < 10 microM)			[8]
Affected Drug/Substrate	Fexofenadine	Modulation Type	Inhibition
Cell System	Human cervical cancer cell line (Hela)-OATP1A2
DT Modulation2	Ritonavir inhibits the activity of SLCO1A2			[12]
Indocyanine green	2 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Indocyanine green inhibits the transportation of Sodium taurocholate by SLCO1A2			[9]
Affected Drug/Substrate	Sodium taurocholate	Modulation Type	Inhibition
Cell System	Oocytes-OATP1A2
DT Modulation2	Indocyanine green inhibits the transportation of Sulfobromophthalein by SLCO1A2			[9]
Affected Drug/Substrate	Sulfobromophthalein	Modulation Type	Inhibition
Cell System	Oocytes-OATP1A2
Quercetin	5 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Quercetin inhibits the transportation of Atorvastatin by SLCO1A2 (IC50 = 13.5 microM; Ki = 32.4 microM)			[6]
Affected Drug/Substrate	Atorvastatin	Modulation Type	Inhibition
Cell System	Human embryonic kidney 293 cells (HEK293)-OATP1A2
Saquinavir	2 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Saquinavir inhibits the transportation of Fexofenadine by SLCO1A2 (IC50 < 10 microM)			[8]
Affected Drug/Substrate	Fexofenadine	Modulation Type	Inhibition
Cell System	Human cervical cancer cell line (Hela)-OATP1A2
Hesperidin	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Hesperidin inhibits the transportation of Fexofenadine by SLCO1A2 (IC50 = 2.7 microM)			[2]
Affected Drug/Substrate	Fexofenadine	Modulation Type	Inhibition
Cell System	Human cervical cancer cell line (Hela)-OATP1A2
Verapamil	2 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Verapamil inhibits the transportation of Fexofenadine by SLCO1A2 (IC50 = 2.6 microM)			[2]
Affected Drug/Substrate	Fexofenadine	Modulation Type	Inhibition
Cell System	Human cervical cancer cell line (Hela)-OATP1A2
Mesalazine	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Mesalazine inhibits the transportation of Bromsulphthalein by SLCO1A2			[15]
Affected Drug/Substrate	Bromsulphthalein	Modulation Type	Inhibition
Cell System	Human embryonic kidney 293 cells (HEK293)-OATP1A2
Naloxone	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Naloxone inhibits the transportation of Deltorphin by SLCO1A2			[16]
Affected Drug/Substrate	Deltorphin	Modulation Type	Inhibition
Cell System	Oocytes-OATP1A2
Lovastatin	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Lovastatin inhibits the transportation of Fexofenadine by SLCO1A2			[8]
Affected Drug/Substrate	Fexofenadine	Modulation Type	Inhibition
Cell System	Oocytes-OATP1A2
Hesperetin	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Hesperetin inhibits the transportation of Fexofenadine by SLCO1A2			[2]
Affected Drug/Substrate	Fexofenadine	Modulation Type	Inhibition
Cell System	Human cervical cancer cell line (Hela)-OATP1A2
Probenecid	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Probenecid inhibits the transporation of ginkolide B by SLCO1A2			[18]
Affected Drug/Substrate	Ginkgolide B	Modulation Type	Inhibition
Cell System	Human enterocyte-like 2 cell (Caco-2)
Carbamazepine	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Carbamazepine increases the expression of SLCO1A2			[19]
Regulation Mechanism	via enhancement of Nuclear receptor subfamily 1 group I member 2 (NR1I2)			Transcription Factor Info
Cell System	Human liver samples
Vitamin D	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Vitamin D increases the expression of SLCO1A2			[20]
Regulation Mechanism	via enhancement of Vitamin D3 receptor (VDR)			Transcription Factor Info
Cell System	Human colon adenocarcinoma cells (Caco-2)
Carmustine	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Carmustine inhibits the expression of SLCO1A2			[21]
Testosterone enanthate	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Testosterone enanthate affects the expression of SLCO1A2			[22]
Omeprazole	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Omeprazole increases the expression of SLCO1A2			[23]
Vorinostat	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Vorinostat increases the expression of SLCO1A2			[24]
Ethinyl Estradiol	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Ethinyl Estradiol inhibits the expression of SLCO1A2			[25]
Calcitriol	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Calcitriol increases the expression of SLCO1A2			[26]
Valproic Acid	4 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Valproic Acid inhibits the expression of SLCO1A2			[27]
Clarithromycin	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Clarithromycin inhibits the activity of SLCO1A2			[7]
Rifaximin	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Rifaximin inhibits the activity of SLCO1A2			[28]
Pravastatin	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Pravastatin inhibits the activity of SLCO1A2			[29], [30]
Mifepristone	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Mifepristone inhibits the activity of SLCO1A2			[31]
Cyclosporine	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Cyclosporine inhibits the activity of SLCO1A2			[31], [32]
Drug in Phase 3 Trial
Curcumin	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Curcumin increases the expression of SLCO1A2			[34]
Drug in Phase 1/2 Trial
PRI-724	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	PRI-724 inhibits the activity of SLCO1A2			[33]
Cell System	Human embryonic kidney 293 cells (HEK293)-
Discontinued Drug
Valspodar	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Valspodar inhibits the transportation of Fexofenadine by SLCO1A2			[8]
Affected Drug/Substrate	Fexofenadine	Modulation Type	Inhibition
Cell System	Oocytes-OATP1A2
Investigative Drug
Naringin	3 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Naringin inhibits the transportation of Fexofenadine by SLCO1A2 (IC50 = 3.6 microM)			[2]
Affected Drug/Substrate	Fexofenadine	Modulation Type	Inhibition
Cell System	Human cervical cancer cell line (Hela)-OATP1A2
DT Modulation2	Naringin inhibits the activity of SLCO1A2 (IC50 = 343 microM)			[3]
Cell System	Oocytes-OATP1A2
DT Modulation3	Naringin inhibits the transportation of Fexofenadine by SLCO1A2			[2]
Affected Drug/Substrate	Fexofenadine	Modulation Type	Inhibition
Cell System	Human cervical cancer cell line (Hela)-OATP1A2
Bromsulphthalein	2 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Bromsulphthalein inhibits the transportation of Estrone sulfate by SLCO1A2 (IC50 = 3.75 microM)			[7]
Affected Drug/Substrate	Estrone sulfate	Modulation Type	Inhibition
Cell System	Monkey kidney tissue Fibroblast-like cell lines (COS1)-OATP1A2
DT Modulation2	Bromsulphthalein inhibits the activity of SLCO1A2			[13]
Apigenin	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Apigenin inhibits the transportation of Atorvastatin by SLCO1A2 (IC50 = 9.3 microM; Ki = 22 microM)			[6]
Affected Drug/Substrate	Atorvastatin	Modulation Type	Inhibition
Cell System	Human embryonic kidney 293 cells (HEK293)-OATP1A2
Kaempferol	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Kaempferol inhibits the transportation of Atorvastatin by SLCO1A2 (IC50 = 37.3 microM; Ki = 25.2 microM)			[6]
Affected Drug/Substrate	Atorvastatin	Modulation Type	Inhibition
Cell System	Human embryonic kidney 293 cells (HEK293)-OATP1A2
Pregnenolone Carbonitrile	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Pregnenolone Carbonitrile increases the expression of SLCO1A2			[23]
Phenylmercuric Acetate	2 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Phenylmercuric Acetate inhibits the expression of SLCO1A2			[35]
21H7	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	21H7 inhibits the activity of SLCO1A2			[33]
Cell System	Human embryonic kidney 293 cells (HEK293)-
FH535	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	FH535 inhibits the activity of SLCO1A2			[33]
Cell System	Human embryonic kidney 293 cells (HEK293)-
Natural Product
DT Modulation1	naringin inhibits the reaction SLCO1A2 protein results in increased uptake of Quercetin			[50]
Regulation Mechanism				Transcription Factor Info
DT Modulation2	SLCO1A2 protein results in increased uptake of Quercetin			[50]
Regulation Mechanism				Transcription Factor Info
DT Modulation3	Sulfobromophthalein inhibits the reaction SLCO1A2 protein results in increased uptake of Quercetin			[50]
Regulation Mechanism				Transcription Factor Info
DT Modulation4	Verapamil inhibits the reaction SLCO1A2 protein results in increased uptake of Quercetin			[50]
Regulation Mechanism				Transcription Factor Info
Epicatechin gallate	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	(-)-epicatechin-3-gallate inhibits the activity of SLCO1A2 in a substrate-dependent manner (IC50 = 10 microM)			[14]
Cell System	Human embryonic kidney 293 cells (HEK293)-OATP1A2
Epigallocatechin gallate	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	(-)-epigallocatechin-3-gallate inhibits the activity of SLCO1A2 in a substrate-dependent manner (IC50 = 55 microM)			[14]
Cell System	Human embryonic kidney 293 cells (HEK293)-OATP1A2
Green tea	2 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Green tea inhibits the uptake of estrone sulphate by SLCO1A2 (IC50 = 10.2 microM)			[14]
Affected Drug/Substrate	Estrone Sulfate	Modulation Type	Inhibition
Cell System	Human embryonic kidney 293 cells (HEK293)
DT Modulation2	Green tea inhibits the transportation of Nadolol by SLCO1A2			[17]
Affected Drug/Substrate	Nadolol	Modulation Type	Inhibition
Cell System	Human embryonic kidney 293 cells (HEK293)-OATP1A2
Dietary Constituent
Apple juice	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Apple juice inhibits the uptake of Bromosulphophthalein by SLCO1A2 (Ki = 22 microM)			[6]
Affected Drug/Substrate	Bromosulphophthalein	Modulation Type	Inhibition
Cell System	Human embryonic kidney 293 cells (HEK293)
Grapefruit juice	2 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Grapefruit inhibits the transportation of Fexofenadine by SLCO1A2			[10]
Affected Drug/Substrate	Fexofenadine	Modulation Type	Inhibition
Cell System	Human enterocyte-like 2 cell (Caco-2)-OATP1A2
DT Modulation2	Grapefruit juice inhibits the activity of SLCO1A2			[11]
Cell System	Human cervical cancer cell line (Hela)-OATP1A2
Orange juice	2 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Orange juice inhibits the transportation of Fexofenadine by SLCO1A2			[10]
Affected Drug/Substrate	Fexofenadine	Modulation Type	Inhibition
Cell System	Human enterocyte-like 2 cell (Caco-2)-OATP1A2
DT Modulation2	Orange juice inhibits the activity of SLCO1A2			[11]
Cell System	Human cervical cancer cell line (Hela)-OATP1A2
Acute Toxic Substance
Okadaic Acid	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Okadaic Acid inhibits the expression of SLCO1A2			[37]
Acrylamide	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Acrylamide inhibits the expression of SLCO1A2			[38]
Health and Environmental Toxicant
Diethylhexyl Phthalate	1 DT Activity Modulations Related to This Exogenous Factor		Click to Show/Hide the Full List
DT Modulation1	Diethylhexyl Phthalate inhibits the expression of SLCO1A2			[36]

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