ATP-Binding Cassette (ABC)

The ATP-binding cassette (ABC) transporter family (ATP-dependent pumps) consist of ubiquitously membrane-bound proteins, present in all prokaryotes, as well as plants, fungi, yeast and animals. These pumps can move substrates in (influx) or out (efflux) of cells, using the favorable chemical energy of ATP hydrolysis to translocate molecules across membranes in a thermodynamically unfavorable direction[1]. In mammals, ABC transporters are expressed predominantly in the liver, intestine, blood-brain barrier, blood-testis barrier, placenta and kidney. Besides, the nucleotide binding domain (NBD or ATP binding cassette), these transporters also contain trans-membrane domains (TMDs), each of which comprises several hydrophobic α-helices. The ABC transporter core unit consists of four domains, two NBDs and two TMDs. The two NBDs together bind and hydrolyze ATP (thereby providing the driving force for transport), while the TMDs participate in substrate recognition and translocation across the lipid membrane[2]. To date, 48 different ABC transporters have been identified in the human genome, divided into seven different classes (A–G; ABC1, MDR/TAP, MRP, ALD, OABP, GCN20, White) based on sequence similarities[3].
The p-glycoprotein (PGP, P-gp) and the breast cancer resistance protein (BCRP) both are members of this large family of transporters. P-gp is known as the multidrug resistance protein 1 (MDR1), or cluster of differentiation 243 (CD243), and transports neutral and cationic hydrophobic compounds across the cell membrane to the cells exterior. It is expressed in only a limited number of tissues with barrier function, including epithelia of the liver, kidney, small and large intestine and capillary endothelial cells in brain, ovary, and testis. As P-gp is one of the important proteins involved in multidrug resistance of tumors, extensive research has been undertaken to find drugs that can reverse the resistance.

[1] D.C. Rees, E. Johnson, O. Lewinson. ABC transporters: the power to change. Nat. Rev. Mol. Cell Biol. 2009, 10, 218-227.
[2] V. Vasiliou et al. Human ATP-binding cassette (ABC) transporter family. Hum. Genomics. 2009, 3, 281-290.
[3] S.V. Ambudkar et al. P-glycoprotein: from genomics to mechanism. Oncogene 2003, 22, 7468-7485. 

10 Item(s)

per page
Axon ID Name Description From price
3564 ABCA1 inducer compound G ABCA1 inducer targeting OSBPL7 €150.00
1654 CP 100356 hydrochloride P-gp inhibitor €90.00
1896 Elacridar hydrochloride P-gp inhibitor (3rd generation ABCB1 modulator) €80.00
1409 KO 143 BCRP inhibitor €60.00
2508 KS 176 Inhibitor of the ABC-transporter BCRP €135.00
2591 MC70 hydrochloride Potent P-gp inhibitor with good selectivity towards BCRP pump €125.00
3784 PGP-4008 Selective P-glycoprotein (Pgp) inhibitor €120.00
3222 Reversan Potent, selective and non-toxic MRP1 inhibitor €90.00
1960 Tariquidar Inhibitor of P-glycoprotein (P-gp, ABCB1) €135.00
1839 Zosuquidar trihydrochloride Inhibitor of P-glycoprotein €95.00

10 Item(s)

per page
Please wait...