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ABCC1

Synonyms: ABC29, ABCC, DKFZp686N04233, DKFZp781G125, GS-X, MRP, MRP1

Entrez Gene Link

Expression Data
Substrate Information
Inhibitor Information
Clinical Drug-drug Interactions

Expression Data

Expression data for other tissues could be found in http://pharmacogenetics.ucsf.edu/gtex/index.html

Asterisk indicates important transporters in the organ as identified in the organ diagram.

Organ	Source	Relative Expression
Brain	Nishimura	`0.00855`
Kidney*	Nishimura	`0.0141`
Liver*	Nishimura	`0.00330`
Placenta*	Nishimura	`0.0224`
Small Intestine*	Nishimura	`0.0184`
Kidney*	Mean across all PMT Samples	`7.555`
Liver*	Mean across all PMT Samples	`0.811`

Note that relative expression values should only be compared between entries of the same source.

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In Vitro Substrates

Substrate	Km (μM)	Cell System	Reference
2-chloro-N-(2-methyl-6ethylphenyl)acetamide-SG	23.8	Sf9 cell membrane vesicles	Oosterhuis, 2008
4-hydroxynonenal-glutathione	1.6	MRP1-expressing High Five vesicles	Renes, 2000
Aflatoxin B1-glutathione	0.189	MRP1-expressing HeLa vesicles	Loe, 1997
Citalopram	1.99	MRP1-expressing HEK293 vesicles	Lee, 2010
Estradiol-17beta-glucuronide	2.5	MRP1-expressing HeLa vesicles	Loe, 1996
Estradiol-17beta-glucuronide	1.5	MRP1-expressing HeLa vesicles	Jedlitschky, 1996
Estradiol-17beta-glucuronide	1.5	MRP1-expressing HEK293 vesicles	Cui, 1999
Estrone sulfate	0.73	MRP1-expressing HeLa vesicles	Qian, 2001
Estrone sulfate	2.1	MRP1-expressing HeLa vesicles	Qian, 2001
Estrone sulfate	4.2	MRP1-expressing HEK vesicles	Nunoya, 2003
Leukotriene C4	0.097	MRP1-expressing HeLa vesicles	Leier, 1994
Leukotriene C4	0.167	MRP1-expressing HeLa vesicles	Qian, 2001
Leukotriene C4	0.067	HeLa cell membrane vesicles	Leslie, 2001
Methotrexate	2150	MRP1-expressing HEK293 vesicles	Zeng, 2001
Methotrexate	930	MRP1-expressing MCF7 vesicles	Paumi, 2003
NNAL-O-glucuronide	39	HeLa cell membrane vesicles	Leslie, 2001
Para-aminohippurate	372	MRP1-expressing HeLa vesicles	Leier, 2000
S-(2,4-dinitrophenyl)-glutathione	3.6	MRP1-expressing HeLa vesicles	Jedlitschky, 1996

ND = not determined
1 denotes drugs that can potentially be used as in vitro substrates for studies of the transporter as defined by the FDA as of March 2022
2 denotes drugs that can potentially be used as in vitro inhibitors for studies of the transporter as defined by the FDA as of March 2022
3 denotes drugs that can potentially be used as clinical substrates for studies of the transporter as defined by the FDA as of March 2022
4 denotes drugs that can potentially be used as clinical inhibitors for studies of the transporter as defined by the FDA as of March 2022

In Vitro Inhibitors

Inhibitor	IC50 (μM)	Ki (μM)	Substrate used	Cell System	Reference
17beta-estradiol-3-sulfate		0.38	Leukotriene C4	MRP1-expressing HeLa vesicles	Qian, 2001
Curcumin	15		Ethacrynic acid glutathione	MRP1-expressing Sf9 vesicles	Wortelboer, 2003
Cyclosporine	5		Leukotriene C4	MRP1-expressing HeLa vesicles	Leier, 1994
Estrone sulfate		0.45	Leukotriene C4	MRP1-expressing HeLa vesicles	Qian, 2001
Genistein	80		2',7'-bis-(3-carboxy-propyl)-5-(and-6)-carboxyfluorescein (BCPCF)	human erythrocytes	Lania-Pietrzak, 2005
Indomethacin	7		2',7'-bis-(3-carboxy-propyl)-5-(and-6)-carboxyfluorescein (BCPCF)	human erythrocytes	Lania-Pietrzak, 2005
Ivermectin	3.8		Calcein AM	HL60 cells	Lespine, 2006
Ivermectin	-	0.5	N-ethylmaleimide-GS	Sf9 cell membranes	Lespine, 2006
Kaempferol		2.4	Leukotriene C4	MRP1-expressing HeLa vesicles	Leslie, 2001
MK-571	3.5		2',7'-bis-(3-carboxy-propyl)-5-(and-6)-carboxyfluorescein (BCPCF)	human erythrocytes	Lania-Pietrzak, 2005
MK-571	5		Calcein AM	MDCK II-MRP1	Wortelboer, 2003
MK-571		134.7	Doxorubicin	2008/P-MRP1	Wong, 2009
MK-571	0.6		Leukotriene C4	MRP1-expressing HeLa vesicles	Leier, 1994
MK571	2		Calcein AM	HL60 cells	Lespine, 2006
Myricetin		13.3	Leukotriene C4	MRP1-expressing HeLa vesicles	Leslie, 2001
Quercetin		8.1	Leukotriene C4	MRP1-expressing HeLa vesicles	Leslie, 2001
Valspodar	27		Leukotriene C4	MRP1-expressing HeLa vesicles	Leier, 1994
Verapamil		13.2	Doxorubicin	2008/P-MRP1	Wong, 2009

Clinical Drug-Drug Interactions

DDI	Implicated Transporter	Interacting Drug	Affected Drug	AUC	Cmax	CLR	CL/F	t1/2	Effect on PD	Reference	More Details
DDI	Implicated Transporter	Interacting Drug	Affected Drug	Clinical PK Impact(fold change)					Effect on PD	Reference	More Details
1	MRPs	Probenecid	Cefmetazole	1.6	NS	0.6	0.6	1.5	ND	Ko, 1989	DDI 1
2	OATs/MRPs	Probenecid	Ciprofloxacin	1.7	NS	0.4	0.6	1.5	ND	Jaehde, 1995	DDI 2
3	OATs/MRPs	Probenecid	Furosemide	2.7	1.5	0.3	0.4	1.7	ND	Vree, 1995	DDI 3

The transporters are implicated by in vitro data and/or studies in humans with genetic polymorphisms of the transporter
DDI = Drug Drug Interaction
PK = pharmacokinetic
PD = pharmacodynamic
ND = not determined
NS = not significant
N/A = information not available
Calculation of Fold Change: fold change in the presence of the interacting drug = (value with interacting drug)/(value without interacting drug)
fold change > 1: increase in pharmacokinetic value
fold change < 1: decrease in pharmacokinetic value
1 denotes drugs that can potentially be used as in vitro substrates for studies of the transporter as defined by the FDA as of March 2022
2 denotes drugs that can potentially be used as in vitro inhibitors for studies of the transporter as defined by the FDA as of March 2022
3 denotes drugs that can potentially be used as clinical substrates for studies of the transporter as defined by the FDA as of March 2022
4 denotes drugs that can potentially be used as clinical inhibitors for studies of the transporter as defined by the FDA as of March 2022