Beyond ADME: The Endogenous Functions of Drug Transporters and Its Impact on Human Disease

Drug transporters are crucial for facilitating the distribution and elimination of drugs from the body, yet their broader physiological functions remain underexplored. Beyond drug handling, these transporters regulate key biological processes, including barrier integrity, metabolic homeostasis, deto...

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Main Authors: Christine Blaze, Yan Shu
Format: Article
Language:English
Published: MDPI AG 2025-05-01
Series:Pharmaceutics
Subjects:
Online Access:https://www.mdpi.com/1999-4923/17/6/685
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author Christine Blaze
Yan Shu
author_facet Christine Blaze
Yan Shu
author_sort Christine Blaze
collection DOAJ
description Drug transporters are crucial for facilitating the distribution and elimination of drugs from the body, yet their broader physiological functions remain underexplored. Beyond drug handling, these transporters regulate key biological processes, including barrier integrity, metabolic homeostasis, detoxification, and immune response. Here we examine the endogenous roles of representative drug transporters along with their involvement in disease pathophysiology, particularly in neurological disorders, cancer, metabolic syndromes, kidney disease, and hepatic disorders. Given the complex interplay between transporters and various physiological processes, a comprehensive understanding of their roles beyond drug transport is imperative for advancing therapeutic strategies and fully grasping their impact on human health. By elucidating their mechanistic roles, researchers can refine drug development and identify novel therapeutic targets. This review underscores the need for continued research into transporters’ diverse functions and their potential as key modulators in disease prevention and treatment.
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spelling doaj-art-91ffed53ac734753bdc991df035a53db2025-08-20T03:27:41ZengMDPI AGPharmaceutics1999-49232025-05-0117668510.3390/pharmaceutics17060685Beyond ADME: The Endogenous Functions of Drug Transporters and Its Impact on Human DiseaseChristine Blaze0Yan Shu1Department of Pharmaceutical Sciences, School of Pharmacy, University of Maryland, Baltimore, MD 21201, USADepartment of Pharmaceutical Sciences, School of Pharmacy, University of Maryland, Baltimore, MD 21201, USADrug transporters are crucial for facilitating the distribution and elimination of drugs from the body, yet their broader physiological functions remain underexplored. Beyond drug handling, these transporters regulate key biological processes, including barrier integrity, metabolic homeostasis, detoxification, and immune response. Here we examine the endogenous roles of representative drug transporters along with their involvement in disease pathophysiology, particularly in neurological disorders, cancer, metabolic syndromes, kidney disease, and hepatic disorders. Given the complex interplay between transporters and various physiological processes, a comprehensive understanding of their roles beyond drug transport is imperative for advancing therapeutic strategies and fully grasping their impact on human health. By elucidating their mechanistic roles, researchers can refine drug development and identify novel therapeutic targets. This review underscores the need for continued research into transporters’ diverse functions and their potential as key modulators in disease prevention and treatment.https://www.mdpi.com/1999-4923/17/6/685drug transportersendogenous substratesendogenous functiontransporter-mediated pathophysiologydetoxificationimmune modulation
spellingShingle Christine Blaze
Yan Shu
Beyond ADME: The Endogenous Functions of Drug Transporters and Its Impact on Human Disease
Pharmaceutics
drug transporters
endogenous substrates
endogenous function
transporter-mediated pathophysiology
detoxification
immune modulation
title Beyond ADME: The Endogenous Functions of Drug Transporters and Its Impact on Human Disease
title_full Beyond ADME: The Endogenous Functions of Drug Transporters and Its Impact on Human Disease
title_fullStr Beyond ADME: The Endogenous Functions of Drug Transporters and Its Impact on Human Disease
title_full_unstemmed Beyond ADME: The Endogenous Functions of Drug Transporters and Its Impact on Human Disease
title_short Beyond ADME: The Endogenous Functions of Drug Transporters and Its Impact on Human Disease
title_sort beyond adme the endogenous functions of drug transporters and its impact on human disease
topic drug transporters
endogenous substrates
endogenous function
transporter-mediated pathophysiology
detoxification
immune modulation
url https://www.mdpi.com/1999-4923/17/6/685
work_keys_str_mv AT christineblaze beyondadmetheendogenousfunctionsofdrugtransportersanditsimpactonhumandisease
AT yanshu beyondadmetheendogenousfunctionsofdrugtransportersanditsimpactonhumandisease