Reverse Translational Research of ABCG2 (BCRP) in Human Disease and Drug Response
Open accessAbstract
Reverse translational research takes a bedside‐to‐bench approach, using sophisticated basic research to explain the biological mechanisms behind observed clinical data. For transporters, which play a role in human disease and drug response, this approach offers a distinct advantage over the typical translational research, which often falters due to inadequate in vitro and preclinical animal models. Research on ABCG2, which encodes the Breast Cancer Resistance Protein, has benefited immensely from a reverse translational approach due to its broad implications for disease susceptibility and both therapeutic and adverse drug response. In this review, we describe the success of reverse translational research for ABCG2 and opportunities for further studies.
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ABCG2 plays an important role in ABC-dependent drug efflux, is capable of transporting chemotherapeutic agents such as paclitaxel and doxorubicin, and confers drug resistance leading to high recurrence and poor survival in hepatocellular carcinoma patients.
“Among them, ABCG2, one of the initially discovered transporters, plays an important role in the ABC-dependent drug efflux, and is capable of transporting a broad range of chemotherapeutic agents such as paclitaxel and doxorubicin (DOX), thus conferring the drug resistance and further leading to high recurrence and poor survival of patients bearing HCC.11–13”
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Kulkarni, C. P., Yang, J. Y., Koleske, M. L., Lara, G., Alam, K., Raw, A., Rege, B. D., Zhao, L. Y., Lu, D., Zhang, L., et al. (2024) · Pharmaceutics · doi:10.3390/pharmaceutics16050647 · Cited by 9 · see citing works
Self-citationReverse Translation: The Art of Cyclical Learning
Kasichayanula, S., & Venkatakrishnan, K. (2018) · Clinical Pharmacology & Therapeutics · doi:10.1002/cpt.952 · Cited by 9 · see citing works
“Advances in genomics have enabled a deeper understanding of mechanisms and shed light on the functional impact of genetic variations that are associated with disease susceptibility and drug response, as illustrated in two State of the Art reviews.(12,13) Brackman and Giacomini(12) offer a compelling value proposition…”
BackgroundRole of transporters in drug disposition and drug-drug interactions
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Self-citationABCG2 plays a central role in the dysregulation of 25-hydrovitamin D in Crohn's disease
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How to optimize the immune checkpoint blockade therapy for cancers?
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“Reverse translational research, also known as bedside-to-bench research or reverse translation, refers to a scienti fi c approach that involves translating clinical observations or fi ndings from patient populations back into laboratory-based studies [54].”
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TRANSPORTERS AS THERAPEUTIC TARGETS IN HUMAN DISEASES
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Navigating drug–drug interactions with apalutamide
Siddiqui, B. A., Tawagi, K., Caulfield, S. E., Aggarwal, P., & Dorff, T. B. (2026) · Prostate Cancer and Prostatic Diseases · doi:10.1038/s41391-026-01086-8
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- Authors
- Brackman, D. J., & Giacomini, K. M.
- Affiliations
- University of California, San Francisco (US)
- Corresponding author
- Giacomini, Kathleen M.
- Venue
- Clinical Pharmacology & Therapeutics
- Publisher
- Wiley
- Published
- 2017-11-28
- Volume
- 103
- Issue
- 2
- Pages
- 233-242
- ISSN
- 0009-9236 (ISSN-L)
- 1532-6535
- PMC
- PMC5760319
- OpenAlex
- W2762317645
- Cited by
- 31
- References
- 71
- Citations by year
- 2026: 1 · 2025: 3 · 2024: 3 · 2023: 2 · 2022: 4 · 2021: 4 · 2020: 7 · 2019: 3 · 2018: 4
- FWCI
- 0.40
- Type
- journal article
- Language
- en
- Open access
- green
- www.ncbi.nlm.nih.gov
- Locations
- Clinical Pharmacology & Therapeutics (publishedVersion)
- PubMed (publishedVersion)
- Europe PMC (PubMed Central) (acceptedVersion)
- PubMed Central (acceptedVersion)
- eScholarship (California Digital Library) (submittedVersion)
- Funders
- NIDDK (R01DK103729)
- Topics
- Health Sciences › Medicine › Oncology › Drug Transport and Resistance Mechanisms
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Pharmacogenetics and Drug Metabolism
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Medicine › Antibiotic Resistance in Bacteria
- Keywords
- ABCG2, reverse translational research, drug transporters, drug response, disease susceptibility, transporter pharmacology
- MeSH terms
- ATP Binding Cassette Transporter, Subfamily G, Member 2, Pharmacogenomic Variants, Drug Development, Animals, Antineoplastic Agents, Humans, Models, Theoretical, Neoplasm Proteins, Neoplasms, Databases, Factual, Risk Assessment, Drug Resistance, Neoplasm, Evidence-Based Medicine, Models, Animal, Drug Discovery, Translational Research, Biomedical, Data Mining, Patient Safety
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