Other Name(s): MDR1, Pgp, P-gp, P-glycoprotein
Drug Target Analysis Report Drug Target Analysis Report Content

About the Target

ABCB1, also known as P-glycoprotein (P-gp), plays a crucial role in drug transport and efflux from cells [3]. It is involved in drug resistance and is upregulated in response to various stimuli such as stress or chemotherapy [2]. Pgp can be released from lipid rafts to gain its full functionality [1]. 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 [1].

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 [4]. On the other hand, inhibiting MAPK signaling results in the upregulation of UBE2R1 and downregulation of P-gp expression [4]. Additionally, the interactions between two proteins, SMARCA4 and SMARCB1, within the SWI/SNF complex can influence ABCB1 expression [5]. The loss of SMARCA4 sensitizes cells to drug treatment by downregulating ABCB1 transcription [5].

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. [1][2][3][4][5]
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 [6].

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 [7].

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 [8].

ABCB1 (Pgp) is involved in the transport and metabolism of rosuvastatin, but its main site of action is excluded from the illustrated organs (liver) [9].

The above viewpoints provide insights into the role and regulation of ABCB1 in drug resistance and its involvement in various cellular processes and diseases.

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