Breast Cancer Resistance Protein: Structure, Localization, Functions, Significance for Rational Pharmacotherapy

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Abstract

INTRODUCTION: Currently, investigation of efflux transport systems of an organism is an important scientific and practical task permitting to more deeply investigate the pharmacokinetics of medical drugs and to optimize pharmacotherapy of a number of diseases. The super family of ABC transporters plays a significant role in transport of biobiotics, the processes of absorption, distribution and excretion of medical drugs from an organism, in realization of undesired drug-drug interactions and development of pharmacoresistance. An important representative of this super family is breast cancer resistance protein (BCRP).

AIM: Systematization of the data on BCRP structure, localization, functions, substrates and modulators of its activity.

This literature review presents modern data on the molecular and spatial structure of BCRP, its localization in the cell, in organs and tissues. The data from studies of the functions of BCRP in an organism, of its role in the development of undesired drug-drug interactions at different stages of pharmacokinetics are summarized. An up-to-date list of medicinal drugs that are substrates and inhibitors of BCRP is given. Modern approaches to testing medical drugs for belonging to BCRP substrates or modulators of its activity are disclosed.

CONCLUSION: The significance of BCRP consists in the existence of a wide range of drugs that are its substrates or modulators of its activity. Upon that, of increasing significance is the investigation both of new and long-known medicinal substances for their belonging to substrates, inducers or inhibitors of breast cancer resistance protein, in order to increase the effectiveness of pharmacotherapy and reduce the risk of undesired drug interactions. Search for non-drug substrates and modulators of BCRP activity permits to obtain new markers for conducting effective studies of safe pharmacokinetics both in vitro and in vivo.

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About the authors

Natal’ya M. Popova

Ryazan State Medical University

Author for correspondence.
Email: p34-66@yandex.ru
ORCID iD: 0000-0002-5166-8372
SPIN-code: 7553-9852

MD, Cand. Sci. (Med.), Associate Professor

Russian Federation, Ryazan

Aleksey V. Shchul’kin

Ryazan State Medical University

Email: alekseyshulkin@rambler.ru
ORCID iD: 0000-0003-1688-0017
SPIN-code: 2754-1702

MD, Dr. Sci. (Med.), Associate Professor

Russian Federation, Ryazan

Yuliya S. Tranova

Ryazan State Medical University

Email: yulyatran@gmail.com
ORCID iD: 0000-0001-5068-1201
SPIN-code: 2732-8760
Russian Federation, Ryazan

Mariya I. Povetko

Ryazan State Medical University

Email: masha-povetko@mail.ru
ORCID iD: 0000-0003-1273-520X
SPIN-code: 2307-4064
Russian Federation, Ryazan

Aleksandr S. Polupanov

Ryazan State Medical University

Email: alexpol81@yandex.ru
ORCID iD: 0000-0003-4065-7544
SPIN-code: 8568-0766

MD, Cand. Sci. (Med.)

Russian Federation, Ryazan

Sergey K. Pravkin

Ryazan State Medical University

Email: psco@mail.ru
ORCID iD: 0000-0002-2088-6350
SPIN-code: 3672-6695

MD, Cand. Sci. (Med.), Associate Professor

Russian Federation, Ryazan

Alexandr A. Slepnev

Ryazan State Medical University

Email: p34-66@yandex.ru
ORCID iD: 0000-0003-0696-6554

к.б.н., доцент кафедры фармакологии

Russian Federation, Ryazan

Elena N. Yakusheva

Ryazan State Medical University

Email: e.yakusheva@rzgmu.ru
ORCID iD: 0000-0001-6887-4888
SPIN-code: 2865-3080

MD, Dr. Sci. (Med.), Professor

Russian Federation, Ryazan

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