ABCB1, P-glycoprotein (P-gp) plays a crucial role in drug transport and efflux from cells

NCBI ID: G5243

ABCB1

ABCB1, P-glycoprotein (P-gp) plays a crucial role in drug transport and efflux from cells

ABCB1 is involved in drug resistance and is upregulated in response to various stimuli such as stress or chemotherapy. Pgp can be released from lipid rafts to gain its full functionality. It has been observed that Pgp can be transferred between cells through cell-to-cell contact, potentially via tunneling nanotubes, or through the transfer of Pgp-containing extracellular vesicles such as exosomes.

In terms of regulation, the degradation of a protein called UBE2R1 through self-ubiquitination, promoted by MAPK signaling activation, leads to the upregulation of P-gp. On the other hand, inhibiting MAPK signaling results in the upregulation of UBE2R1 and downregulation of P-gp expression. Additionally, the interactions between two proteins, SMARCA4 and SMARCB1, within the SWI/SNF complex can influence ABCB1 expression. The loss of SMARCA4 sensitizes cells to drug treatment by downregulating ABCB1 transcription.

Overall, ABCB1/P-gp is essential in drug transport and resistance, and its regulation involves various mechanisms such as stress-induced upregulation, lipid raft involvement, intercellular transfer, and interactions within the SWI/SNF complex. Further research is still needed to fully understand the complex regulation and functional aspects of ABCB1/P-gp.
Based on the provided context information, the key viewpoints related to ABCB1 (also known as MDR1 or P-gp) can be summarized as follows:

Feedback control of TUBB3 through FOXO3a-mediated ABCB1 regulation induces hyperfunctional drug efflux, resulting in acquired cross-resistance to different drugs in cancer cells. This process leads to escape from potential drug inhibition.

CHD1L upregulates ABCB1 expression, partly dependent on c-Jun activation, in non-small cell lung cancer (NSCLC) cells. Silencing c-Jun blocks the transcriptional activity and expression of ABCB1 induced by CHD1L.

Over-expression of Pygo2 increases the expression level of MDR1 (ABCB1), which acts as an efflux pump to pump drug granules out of cells. This upregulated expression of P-gp enhances multidrug resistance.

ABCB1 (Pgp) is involved in the transport and metabolism of rosuvastatin, but its main site of action is excluded from the illustrated organs (liver).

Protein Name: ATP Binding Cassette Subfamily B Member 1

Functions: Translocates drugs and phospholipids across the membrane (PubMed:8898203, PubMed:2897240, PubMed:9038218, PubMed:35970996). Catalyzes the flop of phospholipids from the cytoplasmic to the exoplasmic leaflet of the apical membrane. Participates mainly to the flop of phosphatidylcholine, phosphatidylethanolamine, beta-D-glucosylceramides and sphingomyelins (PubMed:8898203). Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells (PubMed:2897240, PubMed:9038218, PubMed:35970996)

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