ABCG2 (ABCB2) plays a significant role in drug resistance in various types of cancer cells

NCBI ID: G9429

ABCG2

ABCG2 (ABCB2) plays a significant role in drug resistance in various types of cancer cells

Several models have been proposed to explain the mechanisms underlying ABCG2-mediated resistance in different contexts.

CDK7i resistance in triple-negative breast cancer (TNBC) cells: Increased TGF-beta/activin signaling in CDK7i-resistant TNBC cells leads to increased expression of ABCG2 and EMT. Inhibiting TGF-beta/activin signaling or ABCG2 can resensitize the CDK7i-resistant cells to treatment.

Corneal epithelial stem cells: Substrate stiffness affects the behavior of corneal epithelial stem cells. On soft substrates, ABCG2 is highly expressed, contributing to stem cell maintenance. However, substrate stiffening suppresses ABCG2 expression and promotes cell differentiation.

5-FU-resistant colorectal cancer (CRC) cells: The miR-21/PDCD4/JNK/ABCG2 axis is a major molecular mechanism in 5-FU-resistant CRC cells. Understanding this axis may provide insights into combating drug resistance.

Multidrug resistance (MDR) in cancer cells: Overexpression of ABCG2 leads to the efflux of antitumor drugs, resulting in drug resistance. CM082, an inhibitor of ABCG2, can increase drug accumulation in tumor cells and restore drug sensitivity.

Gemcitabine (GEM) resistance in pancreatic cancer cells: PRMT3, when upregulated in GEM-resistant pancreatic cancer cells, stabilizes ABCG2 mRNA through methylation. This upregulation of ABCG2 contributes to gemcitabine resistance.

In summary, ABCG2 is involved in drug resistance in various cancer types through different molecular mechanisms. Modulating ABCG2 expression or activity, either directly or indirectly, may be a viable approach for overcoming drug resistance in these contexts. .
Based on the context information provided, the following key viewpoints can be extracted:

The transporters and enzymes involved in the absorption, distribution, metabolism, and excretion of rosuvastatin were incorporated into a model of various organs and tissues.
The model illustrated the main sites of action for these transporters and enzymes, including the liver for Pgp and the kidney for BCRP.
UCP2, a protein involved in regulating cellular metabolism, is downregulated by hypoxia.
Hypoxia-induced downregulation of UCP2 is linked to chemoresistance in NSCLC cells through the upregulation of ABCG2.
UCP2 knockdown increases glucose uptake and lactate production, while UCP2 overexpression decreases glucose consumption and lactate production.
Hypoxic cells show decreased amounts of components involved in oxidative phosphorylation complexes.
UCP2 downregulation promotes the efflux of chemotherapeutic drugs through the upregulation of ABCG2.

These viewpoints provide a comprehensive summary of the relationship between UCP2, ABCG2, and cellular metabolism under hypoxic conditions.

Protein Name: ATP Binding Cassette Subfamily G Member 2 (Junior Blood Group)

Functions: Broad substrate specificity ATP-dependent transporter of the ATP-binding cassette (ABC) family that actively extrudes a wide variety of physiological compounds, dietary toxins and xenobiotics from cells (PubMed:11306452, PubMed:12958161, PubMed:19506252, PubMed:20705604, PubMed:28554189, PubMed:30405239, PubMed:31003562). Involved in porphyrin homeostasis, mediating the export of protoporphyrin IX (PPIX) from both mitochondria to cytosol and cytosol to extracellular space, it also functions in the cellular export of heme (PubMed:20705604, PubMed:23189181). Also mediates the efflux of sphingosine-1-P from cells (PubMed:20110355). Acts as a urate exporter functioning in both renal and extrarenal urate excretion (PubMed:19506252, PubMed:20368174, PubMed:22132962, PubMed:31003562). In kidney, it also functions as a physiological exporter of the uremic toxin indoxyl sulfate (By similarity). Also involved in the excretion of steroids like estrone 3-sulfate/E1S, 3beta-sulfooxy-androst-5-en-17-one/DHEAS, and other sulfate conjugates (PubMed:12682043, PubMed:28554189, PubMed:30405239). Mediates the secretion of the riboflavin and biotin vitamins into milk (By similarity). Extrudes pheophorbide a, a phototoxic porphyrin catabolite of chlorophyll, reducing its bioavailability (By similarity). Plays an important role in the exclusion of xenobiotics from the brain (Probable). It confers to cells a resistance to multiple drugs and other xenobiotics including mitoxantrone, pheophorbide, camptothecin, methotrexate, azidothymidine, and the anthracyclines daunorubicin and doxorubicin, through the control of their efflux (PubMed:11306452, PubMed:12477054, PubMed:15670731, PubMed:18056989, PubMed:31254042). In placenta, it limits the penetration of drugs from the maternal plasma into the fetus (By similarity). May play a role in early stem cell self-renewal by blocking differentiation (By similarity)

The "ABCG2 Target / Biomarker Review Report" is a customizable review of hundreds up to thousends of related scientific research literature by AI technology, covering specific information about ABCG2 comprehensively, including but not limited to:
•   general information;
•   protein structure and compound binding;
•   protein biological mechanisms;
•   its importance;
•   the target screening and validation;
•   expression level;
•   disease relevance;
•   drug resistance;
•   related combination drugs;
•   pharmacochemistry experiments;
•   related patent analysis;
•   advantages and risks of development, etc.
The report is helpful for project application, drug molecule design, research progress updates, publication of research papers, patent applications, etc. If you are interested to get a full version of this report, please feel free to contact us at BD@silexon.ai

More Common Targets