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BIOMARKER:

ABCB1 overexpression

i
Other names: ABCB1, ABC20, CD243, CLCS, GP170, MDR1, P-gp, PGY1, ATP-binding cassette, sub-family B (MDR/TAP), member 1
Entrez ID:
Related biomarkers:
18d
Solasodine Downregulates ABCB1 Overexpression in Multidrug Resistant Cancer Cells Via Inhibiting Nrf2/Keap1 Signaling Pathway. (PubMed, J Cell Biochem)
In this investigation, the treatment with solasodine and doxorubicin combination showed a notable increase in intracellular ROS generation in KBChR-8-5 cells...Additionally, the combination therapy increased the lipid peroxidation levels while simultaneously reducing the activities of antioxidant enzymes such as superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GPx), and the levels of glutathione (GSH). These results demonstrated that solasodine disrupts redox balance, and overcomes drug resistance by downregulating P-gp via regulating Nrf2/Keap1 signaling pathway in MDR cancer cells.
Journal
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ABCB1 (ATP Binding Cassette Subfamily B Member 1) • NFE2L2 (Nuclear Factor, Erythroid 2 Like 2) • CAT (Catalase)
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ABCB1 overexpression • ABCB1 expression
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doxorubicin hydrochloride
28d
Identification of flavonol derivatives inhibiting MDR1: a strategy to overcome multidrug resistance in cancer. (PubMed, Nat Prod Res)
These potent MDR1 inhibitors were found to enhance chemosensitivity to doxorubicin in MDR1-overexpressing cells...Furthermore, the total number of methoxy groups in the flavonol backbone was found to be a significant factor in determining the potency of MDR1 inhibition. These observations provide fundamental insights into the structure-activity relationship between flavonol derivatives and MDR1 inhibition, potentially aiding in overcoming drug resistance in cancer.
Journal
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ABCB1 (ATP Binding Cassette Subfamily B Member 1) • ABCC1 (ATP Binding Cassette Subfamily C Member 1)
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ABCB1 overexpression
|
doxorubicin hydrochloride
1m
Mobocertinib antagonizes multidrug resistance in ABCB1- and ABCG2-overexpressing cancer cells: in vitro and in vivo studies. (PubMed, Cancer Lett)
In the tumor-bearing mouse model, mobocertinib boosted the antitumor effect of paclitaxel and topotecan, resulting in tumor regression. In summary, our study uncovers a novel potential for repurposing mobocertinib as a dual inhibitor of ABCB1 and ABCG2, and suggests the combination of mobocertinib with substrate drugs as a strategy to counteract MDR.
Preclinical • Journal
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ABCB1 (ATP Binding Cassette Subfamily B Member 1) • ABCG2 (ATP Binding Cassette Subfamily G Member 2)
|
EGFR mutation • EGFR exon 20 insertion • EGFR exon 20 mutation • ABCB1 overexpression • ABCG2 expression
|
paclitaxel • topotecan • Exkivity (mobocertinib)
1m
Gilteritinib reverses ABCB1-mediated multidrug resistance: Preclinical in vitro and animal investigations. (PubMed, Biomed Pharmacother)
In vivo studies have shown that gilteritinib improves the antitumor efficacy of paclitaxel in nude mice without obvious toxic effects. In conclusion, our preclinical investigations show that gilteritinib has the potential to successfully overcome ABCB1-mediated MDR in a clinical environment when combined with substrate medicines.
Preclinical • Journal
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FLT3 (Fms-related tyrosine kinase 3) • ABCB1 (ATP Binding Cassette Subfamily B Member 1)
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ABCB1 overexpression • ABCB1 expression
|
paclitaxel • Xospata (gilteritinib)
1m
Antiproliferative Activity of Cephalotaxus Esters: Overcoming Chemoresistance. (PubMed, Comb Chem High Throughput Screen)
Taken together, our results confirm that HHT is a substrate for MDR1. It opens the door to a new opportunity to clinically evaluate HHT and its derivatives for the treatment of AML and other cancers.
Journal
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ABCB1 (ATP Binding Cassette Subfamily B Member 1) • ABCG2 (ATP Binding Cassette Subfamily G Member 2) • CASP3 (Caspase 3) • CDC7 (Cell Division Cycle 7)
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ABCB1 overexpression
|
mitoxantrone • dactinomycin • Synribo (omacetaxine mepesuccinate)
2ms
Synthesis and evaluation of novel tetrahydroisoquinoline-benzo[h]chromen-4-one conjugates as dual ABCB1/CYP1B1 inhibitors for overcoming MDR in cancer. (PubMed, Bioorg Med Chem)
In parallel, this dual ABCB1/CYP1B1 inhibitory effect drives compound A10 exhibiting prominent drug resistance reversal activity to doxorubicin (IC50 = 4.7 μM, RF = 13.7) in ABCB1/CYP1B1-overexpressing DOX-SW620/AD300-1B1 resistant cells, which is more potent than that of the CYP1B1 inhibitor ANF. Furthermore, although compound A2 possessed moderate ABCB1/CYP1B1 inhibitory activity, it showed considerable antiproliferative activity towards drug-resistant SW620/AD300 and MKN45-DDP-R cells, which may be partly related to the increase of PUMA expression to promote the apoptosis of the drug-resistant MKN45-DDP-R cells as confirmed by proteomics and western blot assay. These results indicated that the tetrahydroisoquinoline-benzo[h]chromen-4-one conjugates may provide a fundamental scaffold reference for further discovery of MDR reversal agents.
Journal
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ABCB1 (ATP Binding Cassette Subfamily B Member 1) • BBC3 (BCL2 Binding Component 3) • CYP1B1 (Cytochrome P450 Family 1 Subfamily B Member 1)
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ABCB1 overexpression
|
doxorubicin hydrochloride
2ms
Epertinib counteracts multidrug resistance in cancer cells by antagonizing the drug efflux function of ABCB1 and ABCG2. (PubMed, Biomed Pharmacother)
In summary, our study demonstrates an additional pharmacological capability of epertinib against the activity of ABCB1 and ABCG2. These findings suggest that incorporating epertinib into combination therapy could be advantageous for a specific patient subset with tumors exhibiting high levels of ABCB1 or ABCG2, warranting further exploration.
Journal
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EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2) • ABCB1 (ATP Binding Cassette Subfamily B Member 1) • ABCG2 (ATP Binding Cassette Subfamily G Member 2)
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ABCB1 overexpression • ABCG2 expression
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epertinib (S-222611)
7ms
Impact of ABCB1 and ABCG2 Transporter in Outcome of Gallbladder Cancer. (PubMed, J Clin Exp Hepatol)
Altered expression of ABCB1 and ABCG2 may not be a useful prognostic marker for survival or response to chemotherapy in GBC. Presently, histo-pathological characteristics and associated gallstones are the important predictors for survival and recurrence in GBC.
Journal
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ABCB1 (ATP Binding Cassette Subfamily B Member 1) • ABCG2 (ATP Binding Cassette Subfamily G Member 2)
|
ABCB1 overexpression
7ms
Evaluation of Novel Benzo-annelated 1,4-dihydropyridines as MDR Modulators in Cancer Cells. (PubMed, Anticancer Agents Med Chem)
Novel MDR modulators could be identified with favorable methoxy and ester group functions. Their use in both ABCB1 non-expressing and overexpressing cells proves a selective toxicity-increasing effect of the applied anticancer agent in the ABCB1 overexpressing cells, whereas the toxicity effect of the anticancer drug was almost unchanged in the non-expressing cells. These results qualify our novel compounds as perspective anticancer drugs compared to MDR modulators with nonselective toxicity properties.
Journal
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ABCB1 (ATP Binding Cassette Subfamily B Member 1)
|
ABCB1 overexpression • ABCB1 expression
7ms
Morphological and Molecular Biological Characteristics of Experimental Rat Glioblastoma Tissue Strains Induced by Different Carcinogenic Chemicals. (PubMed, Biomedicines)
GBM 101.8 is a reliable model for further investigation due to its similarity to high-grade human GBMs, while GBM 11-9-2 and GBM 14-4-5 correspond to Grade 2-3 gliomas.
Preclinical • Journal
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TP53 (Tumor protein P53) • PTEN (Phosphatase and tensin homolog) • CDKN2A (Cyclin Dependent Kinase Inhibitor 2A) • PDGFRA (Platelet Derived Growth Factor Receptor Alpha) • MGMT (6-O-methylguanine-DNA methyltransferase) • ABCB1 (ATP Binding Cassette Subfamily B Member 1) • HIF1A (Hypoxia inducible factor 1, alpha subunit) • SOX2
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ABCB1 overexpression • HIF1A expression • VEGFA expression • MGMT expression • SOX2 expression
8ms
Phenylspirodrimane with Moderate Reversal Effect of Multidrug Resistance Isolated from the Deep-Sea Fungus Stachybotrys sp. 3A00409. (PubMed, Molecules)
Stachybotrysin B (8) can reverse multidrug resistance (MDR) in ABCB1-overexpression cells (KBv200, Hela/VCR) at the non-cytotoxic concentration. Doxorubicin accumulation assay and molecular-docking analysis reveal that the mechanism of its reversal MDR effect may be related to the increase in the intracellular concentration of substrate anticancer drugs.
Journal
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ABCB1 (ATP Binding Cassette Subfamily B Member 1)
|
ABCB1 overexpression • ABCB1 expression
|
doxorubicin hydrochloride
8ms
SiRNA-Mediated Knockdown of ABCB1 Enhances the Efficacy of Doxorubicin and Vinorelbine in Breast Cancer Cells. (PubMed, Curr Pharm Biotechnol)
these findings suggest that combining siRNA, doxorubicin, and vinorelbine holds promise as a therapeutic strategy to overcome ABCB1-mediated multidrug resistance in breast cancer. Further investigations and clinical trials are warranted to evaluate its clinical efficacy rigorously.
Journal
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ABCB1 (ATP Binding Cassette Subfamily B Member 1)
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ABCB1 overexpression • ABCB1 expression
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doxorubicin hydrochloride • vinorelbine tartrate
8ms
Schiff bases and their metal complexes to target and overcome (multidrug) resistance in cancer. (PubMed, Eur J Med Chem)
The areas of drug resistance covered in this article involve: 1) Modulation of ABC transporter function, 2) Targeting lysosomal ABCB1 overexpression, 3) Circumvention of ABC transporter-mediated drug efflux by alternative routes of drug uptake, 4) Selective activity against MDR cancer models (collateral sensitivity), 5) Targeting GSH-detoxifying systems, 6) Overcoming apoptosis resistance by inducing necrosis and paraptosis, 7) Reactivation of mutated p53, 8) Restoration of sensitivity to DNA-damaging anticancer therapy, and 9) Overcoming drug resistance through modulation of the immune system. Through this approach, we would like to draw attention to Schiff bases and their metal complexes representing highly interesting anticancer drug candidates with the ability to overcome MDR.
Review • Journal
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TP53 (Tumor protein P53) • ABCB1 (ATP Binding Cassette Subfamily B Member 1)
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TP53 mutation • ABCB1 overexpression • ABCB1 expression
8ms
Development of an orally bioavailable mSWI/SNF ATPase degrader and acquired mechanisms of resistance in prostate cancer. (PubMed, Proc Natl Acad Sci U S A)
AU-24118 demonstrated tumor regression in a model of castration-resistant prostate cancer (CRPC) which was further enhanced with combination enzalutamide treatment, a standard of care androgen receptor (AR) antagonist used in CRPC patients. The ABCB1 inhibitor, zosuquidar, reversed resistance to all three PROTAC degraders tested. Combined, these findings position mSWI/SNF degraders for clinical translation for patients with enhancer-driven cancers and define strategies to overcome resistance mechanisms that may arise.
Journal
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AR (Androgen receptor) • PBRM1 (Polybromo 1) • SMARCA4 (SWI/SNF related, matrix associated, actin dependent regulator of chromatin, subfamily A, member 4) • ABCB1 (ATP Binding Cassette Subfamily B Member 1) • SMARCA2 (SWI/SNF Related, Matrix Associated, Actin Dependent Regulator Of Chromatin, Subfamily A, Member 2)
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SMARCA4 mutation • ABCB1 overexpression • ABCB1 expression
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Xtandi (enzalutamide capsule)
8ms
Zosuquidar: An Effective Molecule for Intracellular Ca2+ Measurement in P-gp Positive Cells. (PubMed, Int J Mol Sci)
The solution is to use a proper inhibitor of P-gp efflux activity to ensure the retention of the tracer inside the cells. The present study showed that Zosuquidar and Tariquidar (P-gp inhibitors) are suitable for monitoring intracellular calcium, either by flow cytometry or confocal microscopy, in cells overexpressing P-gp.
Journal
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ABCB1 (ATP Binding Cassette Subfamily B Member 1)
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ABCB1 overexpression
8ms
Valproate modulates the activity of multidrug resistance efflux pumps, as a chemoresistance factor in gastric cancer cells. (PubMed, Mol Biol Rep)
Valproate can affect drug resistance in gastric cancer via a unique mechanism independent of MDR1 expression.
Journal • IO biomarker
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PTEN (Phosphatase and tensin homolog) • BCL2 (B-cell CLL/lymphoma 2) • ABCB1 (ATP Binding Cassette Subfamily B Member 1) • CASP3 (Caspase 3) • CDKN1A (Cyclin-dependent kinase inhibitor 1A)
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ABCB1 overexpression • TP53 expression
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daunorubicin
9ms
The SMAC mimetic GDC-0152 is a direct ABCB1-ATPase activity modulator and BIRC5 expression suppressor in cancer cells. (PubMed, Toxicol Appl Pharmacol)
Co-treatment with GDC-0152 restored the sensitivity to the known ABCB1 substrates, including paclitaxel, vincristine, and YM155 in ABCB1-expressing multidrug-resistant cancer cells, and it also restored the sensitivity to tamoxifen in BIRC5-overexpressing tamoxifen-resistant breast cancer cells in vitro...In conclusion, GDC-0152 has the potential for use in the management of cancer patients with ABCB1 and BIRC5-related drug resistance. The findings of our study provide essential information to physicians for designing a more patient-specific GDC-0152 clinical trial program in the future.
Journal
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ABCB1 (ATP Binding Cassette Subfamily B Member 1) • BIRC5 (Baculoviral IAP repeat containing 5)
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ABCB1 overexpression • ABCB1 expression • BIRC5 expression
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paclitaxel • tamoxifen • vincristine • sepantronium bromide (PC-002)
9ms
NAT10-mediated mRNA N4-acetylcytidine modification of MDR1 and BCRP promotes breast cancer progression. (PubMed, Thorac Cancer)
The results of our study demonstrated the essential role of NAT10-mediated ac4c-modification in breast cancer progression and provide a novel strategy for overcoming chemoresistance challenges.
Journal
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ABCB1 (ATP Binding Cassette Subfamily B Member 1) • ABCC1 (ATP Binding Cassette Subfamily C Member 1)
|
ABCB1 overexpression
|
capecitabine
10ms
In ovarian cancer maraviroc potentiates the antitumoral activity and further inhibits the formation of a tumor-promoting microenvironment by trabectedin. (PubMed, Biomed Pharmacother)
Maraviroc treatment did not affect OC cell viability, but strongly potentiated the antiproliferative activity, apoptosis induction, cell cycle blockage, DNA damage, and ROS formation by trabectedin. In A2780cis cisplatin-resistant cells, the cross-resistance to trabectedin was overcame by the combination with maraviroc. Maraviroc enhanced trabectedin cytotoxicity in OC 3Dimensional spheroids and THP-1-monocytes. Both maraviroc and trabectedin interact with drug efflux pump MDR1/P-gp, overexpressed in recurrent OC patients. Maraviroc increased trabectedin intracellular accumulation and the MDR1-inhibitor verapamil, like maraviroc, increased trabectedin cytotoxicity. In OC tumor xenografts the combination with maraviroc further reduced tumor growth, angiogenesis, and monocyte infiltration by trabectedin. In conclusion, this study offers a preclinical rationale for the use of maraviroc as new option to improve trabectedin activity in relapsed chemoresistant OC patients.
Journal
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ABCB1 (ATP Binding Cassette Subfamily B Member 1) • CCR5 (C-C Motif Chemokine Receptor 5)
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ABCB1 overexpression • CCR5 expression
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cisplatin • Yondelis (trabectedin)
10ms
Foretinib, a c-MET receptor tyrosine kinase inhibitor, tackles multidrug resistance in cancer cells by inhibiting ABCB1 and ABCG2 transporters. (PubMed, Toxicol Appl Pharmacol)
Overall, our results suggest that foretinib can target MDR-linked ABCB1 and ABCG2 transporters in clinical cancer therapy.
Journal
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MET (MET proto-oncogene, receptor tyrosine kinase) • ABCB1 (ATP Binding Cassette Subfamily B Member 1) • ABCG2 (ATP Binding Cassette Subfamily G Member 2)
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ABCB1 overexpression • ABCB1 expression • ABCG2 expression
|
doxorubicin hydrochloride • mitoxantrone • foretinib (GSK1363089)
10ms
ABCB1-dependent collateral sensitivity of multidrug-resistant colorectal cancer cells to the survivin inhibitor MX106-4C. (PubMed, Drug Resist Updat)
MX106-4C selectively kills ABCB1-positive MDR colorectal cancer cells via a novel ABCB1-dependent survivin inhibition mechanism, providing a clue for designing CS compound as an alternative strategy to overcome ABCB1-mediated colorectal cancer MDR.
Journal
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ABCB1 (ATP Binding Cassette Subfamily B Member 1) • CDK4 (Cyclin-dependent kinase 4) • BIRC5 (Baculoviral IAP repeat containing 5) • CASP7 (Caspase 7) • CDKN1A (Cyclin-dependent kinase inhibitor 1A)
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ABCB1 overexpression • ABCB1 expression • ABCB1 mutation
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doxorubicin hydrochloride
11ms
Overexpression of ABCB1 confers resistance to FLT3 inhibitor FN-1501 in cancer cells: in vitro and in vivo characterization. (PubMed, Am J Cancer Res)
In sum, we demonstrate that FN-1501 is a substrate of ABCB1 transporter from both in vivo and in vitro studies. Therefore, our findings provide new insight on the mechanism of chemoresistance due to ABCB1 overexpression.
Preclinical • Journal
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FLT3 (Fms-related tyrosine kinase 3) • ABCB1 (ATP Binding Cassette Subfamily B Member 1)
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ABCB1 overexpression • ABCB1 expression
|
FN-1501
11ms
ABCB1 overexpression through locus amplification represents an actionable target to combat paclitaxel resistance in pancreatic cancer cells. (PubMed, J Exp Clin Cancer Res)
Upregulation of ABCB1 through locus amplification represents a novel, conserved mechanism of PDAC paclitaxel resistance. Kinase inhibitors identified in this study can be further (pre) clinically explored as therapeutic strategies to overcome paclitaxel resistance in PDAC.
Journal
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ABCB1 (ATP Binding Cassette Subfamily B Member 1)
|
ABCB1 overexpression • ABCB1 expression
|
gemcitabine • albumin-bound paclitaxel
1year
PYGO2-MDR1 Axis in Multiple Myeloma Patients with 1q21 Amplification As Promising Target to Overcome Carfilzomib Resistance (ASH 2023)
In conclusion, our results show that PYGO2 expression is significantly upregulated in MM patients carrying 1q21+ and that its expression is correlated with 1q21 copy number. Moreover, we found that the PYGO2-MDR1 axis is involved in the CFZ resistance in HMCLs MM cells suggesting that PYGO2 could be a possible future druggable target in 1q21+ MM patients.
Clinical
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ABCB1 (ATP Binding Cassette Subfamily B Member 1) • CTNNB1 (Catenin (cadherin-associated protein), beta 1) • SDC1 (Syndecan 1) • BCL9 (BCL9 Transcription Coactivator)
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ABCB1 overexpression
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carfilzomib
1year
Combining Inotuzumab Ozogamicin (IO) with PARP Inhibitors, Olaparib and Talazoparib, Exerts Synergistic Cytotoxicity By Inhibiting the Repair of IO-Induced DNA Strand Breaks in IO-Resistant ALL Cells (ASH 2023)
This would be because the PARP inhibitors were still effective in inhibiting the DNA repair in Reh-IO-R cells where the DNA repair function was not augmented. [Conclusion]The combination of IO with PARP inhibitors synergized the antileukemic effect of IO by inhibiting DNA strand break repair in CD22-positive ALL cell lines and IO-resistant ALL cells, suggesting that these results may contribute to overcoming the IO resistance mechanisms.
BRCA Biomarker • PARP Biomarker
|
BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • ATM (ATM serine/threonine kinase) • ABCB1 (ATP Binding Cassette Subfamily B Member 1) • ERCC1 (Excision repair cross-complementation group 1) • CD22 (CD22 Molecule) • CHEK1 (Checkpoint kinase 1) • ANXA5 (Annexin A5)
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ABCB1 overexpression • CD22 positive • CD22 expression • ATM expression
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Lynparza (olaparib) • Talzenna (talazoparib) • Besponsa (inotuzumab ozogamicin)
1year
Pemigatinib, a selective FGFR inhibitor overcomes ABCB1-mediated multidrug resistance in cancer cells. (PubMed, Biochem Biophys Res Commun)
In addition, Docking analysis revealed that Pemigatinib and ABCB1 have a high affinity for one another. This study concludes that Pemigatinib is capable of reversing the multidrug resistance mediated by ABCB1, offering ideas and references for the clinical application of Pemigatinib.
Journal
|
FGFR (Fibroblast Growth Factor Receptor) • ABCB1 (ATP Binding Cassette Subfamily B Member 1)
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ABCB1 overexpression • ABCB1 expression
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Pemazyre (pemigatinib)
1year
Second-site suppressor mutations reveal connection between the drug-binding pocket and nucleotide-binding domain 1 of human P-glycoprotein (ABCB1). (PubMed, Drug Resist Updat)
Although both the mutants were expressed at normal levels at the cell surface, the 6Y mutant failed to transport all the tested substrates except Bodipy-verapamil, whereas the 9Y mutant effluxed all tested substrates in a manner very similar to that of the wild-type protein...This is the first evidence for the existence of second-site suppressors in human P-gp that allow recovery of the loss of transport function caused by primary mutations. Further study of such mutations could facilitate mapping of the communication pathway between the substrate-binding pocket and the NBDs of P-gp and possibly other ABC drug transporters.
Journal
|
ABCB1 (ATP Binding Cassette Subfamily B Member 1)
|
ABCB1 overexpression
1year
Design, Synthesis, and Biological Evaluation of SSE1806, a Microtubule Destabilizer That Overcomes Multidrug Resistance. (PubMed, ACS Med Chem Lett)
Importantly, SSE1806 overcame multidrug resistance in a cell line overexpressing MDR-1. Thus, SSE1806 represents a potential anticancer agent that can overcome multidrug resistance.
Journal
|
TP53 (Tumor protein P53) • ABCB1 (ATP Binding Cassette Subfamily B Member 1)
|
ABCB1 overexpression • TP53 expression
1year
Activity of Lysosomal ABCC3, ABCC5 and ABCC10 is Responsible for Lysosomal Sequestration of Doxorubicin and Paclitaxel-Oregongreen488 in Paclitaxel-Resistant Cancer Cell Lines. (PubMed, Cell Physiol Biochem)
The results suggest that lysosome membranes anchored ABCC proteins which remained functionally active and were capable to load chemotherapeutics into lysosomes in paclitaxel-resistant cancer cells. Therefore, targeting of lysosomal ABCC transporters may help to overcome paclitaxel-induced resistance by reducing the accumulation of drugs in lysosomes.
Preclinical • Journal
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ABCB1 (ATP Binding Cassette Subfamily B Member 1) • ABCC10 (ATP Binding Cassette Subfamily C Member 10) • ABCC3 (ATP Binding Cassette Subfamily C Member 3) • ABCC5 (ATP Binding Cassette Subfamily C Member 5)
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ABCB1 overexpression
|
paclitaxel • doxorubicin hydrochloride
1year
Journal
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ABCB1 (ATP Binding Cassette Subfamily B Member 1)
|
ABCB1 overexpression
1year
Pharmacokinetics of the KRAS inhibitor adagrasib is limited by CYP3A and ABCB1, and influenced by binding to mouse plasma carboxylesterase 1c. (PubMed, Biomed Pharmacother)
The influence of ABC transporters was completely reversed by coadministration of the dual ABCB1/ABCG2 inhibitor elacridar, increasing the brain penetration in wild-type mice by 41-fold while no signs of acute CNS toxicity were observed. This binding could complicate interpretation of mouse studies, especially since humans lack circulating CES1 enzyme(s). Our results may be useful to further optimize the clinical safety and efficacy of adagrasib, and give more insight into potential drug-drug interactions risks.
PK/PD data • Preclinical • Journal
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KRAS (KRAS proto-oncogene GTPase) • ABCB1 (ATP Binding Cassette Subfamily B Member 1) • ABCG2 (ATP Binding Cassette Subfamily G Member 2) • CES1 (Carboxylesterase 1) • CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4)
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ABCB1 overexpression • ABCB1 expression
|
Krazati (adagrasib) • elacridar (GF120918)
over1year
Establishment and Characterization of Multi-Drug Resistant p53-Negative Osteosarcoma SaOS-2 Subline. (PubMed, Diagnostics (Basel))
An acquired resistance of OS to the chemotherapeutic agents might be due to the several mechanisms undergoing simultaneously on the single-cell level. This reveals the complexity of the mechanisms involved in the secondary resistance of OS to chemotherapies.
Journal • PARP Biomarker
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ABCB1 (ATP Binding Cassette Subfamily B Member 1) • MSH2 (MutS Homolog 2) • ABCG2 (ATP Binding Cassette Subfamily G Member 2) • CHEK2 (Checkpoint kinase 2) • RAD51 (RAD51 Homolog A) • ABCC1 (ATP Binding Cassette Subfamily C Member 1) • CHEK1 (Checkpoint kinase 1) • CASP3 (Caspase 3) • MRE11A (MRE11 homolog, double strand break repair nuclease)
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ABCB1 overexpression
|
paclitaxel • doxorubicin hydrochloride • vinblastine • cyclosporine
over1year
Overexpression of MRP1/ABCC1, Survivin and BCRP/ABCC2 Predicts the Resistance of Diffuse Large B-Cell Lymphoma to R-CHOP Treatment. (PubMed, Cancers (Basel))
DLBCL might harbor certain molecular signatures such as MRP1/ABCC1, survivin, and BCRP/ABCC2 overexpression that can predict resistance to R-CHOP.
Journal • IO biomarker
|
BCL2 (B-cell CLL/lymphoma 2) • ABCB1 (ATP Binding Cassette Subfamily B Member 1) • ABCG2 (ATP Binding Cassette Subfamily G Member 2) • BIRC5 (Baculoviral IAP repeat containing 5) • ABCC1 (ATP Binding Cassette Subfamily C Member 1) • ABCC2 (ATP Binding Cassette Subfamily C Member 2)
|
BCL2 expression • ABCB1 overexpression • BIRC5 expression • ABCC2 overexpression
|
Rituxan (rituximab)
over1year
Targeting MAGI2-AS3-modulated Akt-dependent ATP-binding cassette transporters as a possible strategy to reverse temozolomide resistance in temozolomide-resistant glioblastoma cells. (PubMed, Drug Dev Res)
MAGI2-AS3 inhibited tumor growth and enhanced the suppressive effect of TMZ on glioma tumorigenesis in vivo. In conclusion, MAGI2-AS3 reverses TMZ resistance in glioma cells by inactivating the Akt pathway.
Journal
|
ABCB1 (ATP Binding Cassette Subfamily B Member 1) • ABCG2 (ATP Binding Cassette Subfamily G Member 2) • MAGI2-AS3 (MAGI2 Antisense RNA 3)
|
ABCB1 overexpression • ABCG2 expression
|
temozolomide
over1year
Efficacy of retreatment with polatuzumab vedotin in combination with rituximab in polatuzumab vedotin-resistant DLBCL models. (PubMed, Leuk Lymphoma)
Additionally, treatment with Pola + Rit significantly enhanced antitumor activity in Pola-resistant STR-428 xenograft mouse models. Based on these results, Pola + Rit retreatment could have preserved efficacy because of the effect of Pola on sensitizing cells to Rit.
Journal • Combination therapy
|
MCL1 (Myeloid cell leukemia 1) • ABCB1 (ATP Binding Cassette Subfamily B Member 1) • BCL2L11 (BCL2 Like 11)
|
ABCB1 overexpression • MCL1 expression
|
Rituxan (rituximab) • Polivy (polatuzumab vedotin-piiq)
over1year
The AKT inhibitor, MK-2206, attenuates ABCG2-mediated drug resistance in lung and colon cancer cells. (PubMed, Front Pharmacol)
The compound, MK-2206, an inhibitor of the protein kinases AKT1/2/3, is undergoing evaluation in multiple clinical trials for the treatment of certain types of cancers, including those resistant to erlotinib...Methodology: The efficacy of MK-2206 (0.03-1 μM), in combination with the ABCB1 transporter sub-strates doxorubicin and paclitaxel, and ABCG2 transporter substrates mitoxantrone, SN-38 and topotecan, were determined in the cancer cell lines, KB-C2 and SW620/Ad300, which overexpress the ABCB1 transporter or H460/MX20 and S1-M1-80, which overexpress the ABCG2 transporter, respectively... These in vitro data indicated that MK-2206 surmounts resistance to mitoxantrone, SN-38 and topotecan in cancer cells overexpressing the ABCG2 transporter. If these results can be translated to humans, it is possible that MK-2206 could be used to surmount MDR in cancer cells overexpressing the ABCG2 transporter.
Journal
|
AKT1 (V-akt murine thymoma viral oncogene homolog 1) • ABCB1 (ATP Binding Cassette Subfamily B Member 1) • ABCG2 (ATP Binding Cassette Subfamily G Member 2)
|
ABCB1 overexpression • ABCG2 expression
|
erlotinib • paclitaxel • doxorubicin hydrochloride • MK-2206 • mitoxantrone • topotecan
over1year
Bixin and Fuxoxanthin Alone and in Combination with Cisplatin Regulate ABCC1 and ABCC2 Transcription in A549 Lung Cancer Cells. (PubMed, J Pharm Bioallied Sci)
The administration of bixin or fucoxanthin decreases the expression of ABCC1 and ABCC2. Both carotenoids, either alone or in combination with cisplatin, upregulated p53 gene expression indicating the mechanism of proliferation inhibition and apoptosis occurs via the p53 caspase-independent pathway.
Journal • Combination therapy
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ABCB1 (ATP Binding Cassette Subfamily B Member 1) • ABCG2 (ATP Binding Cassette Subfamily G Member 2) • ABCC1 (ATP Binding Cassette Subfamily C Member 1) • ABCC2 (ATP Binding Cassette Subfamily C Member 2) • ABCC3 (ATP Binding Cassette Subfamily C Member 3)
|
ABCB1 overexpression • TP53 expression • ABCC1 expression
|
cisplatin
over1year
METTL3-mediated mA modification of lnc KCNQ1OT1 promotes doxorubicin resistance in breast cancer by regulating miR-103a-3p/MDR1 axis. (PubMed, Epigenetics)
Overexpression of MDR1 abolished the impacts of lnc KCNQ1OT1 depletion on DOX resistance in BC. In conclusion, our results unveiled that in BC cells and DOX-resistant BC cells, lnc KCNQ1OT1 could be mediated by METTL3 through mA modification to elevate and stabilize its expression, further inhibiting miR-103a-3p/MDR1 axis to promote DOX resistance, which might provide novel thought to overcome DOX resistance in BC.
Journal
|
ABCB1 (ATP Binding Cassette Subfamily B Member 1) • KCNQ1OT1 (KCNQ1 Opposite Strand/Antisense Transcript 1) • METTL3 (Methyltransferase Like 3)
|
ABCB1 overexpression • KCNQ1OT1 overexpression
|
doxorubicin hydrochloride
over1year
MDR1 Inhibition Reverses Doxorubicin-Resistance in Six Doxorubicin-Resistant Canine Prostate and Bladder Cancer Cell Lines. (PubMed, Int J Mol Sci)
Chemoresistance to doxorubicin, cross-resistance to carboplatin, and the reversibility of the acquired resistance by the specific MDR1-inhibitor tariquidar were quantified in metabolic assays. Combination therapies aiming to inhibit MDR1 activity can now be screened for synergistic effects using our resistant sublines. Nevertheless, detailed resistance mechanisms and maintained molecular target expression in the resistant sublines are still to be examined.
Preclinical • Journal
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TOP2A (DNA topoisomerase 2-alpha) • ABCB1 (ATP Binding Cassette Subfamily B Member 1)
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ABCB1 overexpression
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carboplatin • doxorubicin hydrochloride
over1year
Effect of overexpression of ERK1/2 and MDR1 on chemoresistance in advanced gastric cancer patients. (ASCO 2023)
NACT group treated with docetaxel (60 mg/m2), oxaliplatin (85 mg/m2), leucovorin (200 mg/m2), and 5-fluorouracil (2,600 mg/m2 as a 24 hr infusion), all given on day 1 and administered every 2 weeks before surgery. ERK1/2 and MDR1 found to over-express in stage III, predicts the degree of resistance and MDR phenotype in the GC patients.
Clinical • Metastases
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ABCB1 (ATP Binding Cassette Subfamily B Member 1)
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ABCB1 overexpression
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docetaxel • 5-fluorouracil • oxaliplatin • leucovorin calcium
over1year
Overcoming acquired resistance to PROTAC degraders (AACR 2023)
Our study found that the mechanisms of resistance of PROTAC degraders can vary and may be dependent on drug concentrations. Such concepts may inform future clinical decision-making regarding drug dosing.
Preclinical
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PBRM1 (Polybromo 1) • SMARCA4 (SWI/SNF related, matrix associated, actin dependent regulator of chromatin, subfamily A, member 4) • ABCB1 (ATP Binding Cassette Subfamily B Member 1) • ABCC1 (ATP Binding Cassette Subfamily C Member 1)
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ABCB1 overexpression • ABCB1 expression • ABCC1 expression
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AU-15330
almost2years
Overexpression of BCL2, BCL6, VEGFR1 and TWIST1 in Circulating Tumor Cells Derived from Patients with DLBCL Decreases Event-Free Survival. (PubMed, Onco Targets Ther)
More than half of patients with DLBCL can achieve remission with standard R-CHOP regimes; however, approximately 30-40% of patients are still failing this standard therapy, which remains as an important cause of progression and mortality of this disease...The overexpression of BCL2, BCL6, VEGFR1 and TWIST1 was related to a minor EFS (p = 0.001). This study showed that in liquid biopsies analyzed, the presence of CTCs can be confirmed through molecular biomarkers, and it has an impact on OS and EFs, making this detection useful in the follow-up and prognosis of patients with DLBCL.
Journal • Circulating tumor cells • IO biomarker • Tumor cell
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BCL2 (B-cell CLL/lymphoma 2) • BCL6 (B-cell CLL/lymphoma 6) • ABCB1 (ATP Binding Cassette Subfamily B Member 1) • FLT1 (Fms-related tyrosine kinase 1) • MAGEA4 (Melanoma antigen family A, 4) • EPCAM (Epithelial cell adhesion molecule) • KRT19 (Keratin 19) • TWIST1 (Twist Family BHLH Transcription Factor 1)
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BCL2 overexpression • ABCB1 overexpression • BCL6 overexpression • EPCAM expression • FLT1 expression
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Rituxan (rituximab)