phkineticaФармакокинетика и ФармакодинамикаPharmacokinetics and Pharmacodynamics2587-78362686-8830ООО «Издательство ОКИ»10.37489/2587-7836-2019-4-3-17phkinetica-226Research ArticleОБЗОРЫREVIEWSЛиганды сигнальных белков Ерас как инструменты для изучения их биологической активности и создания новых оригинальных лекарственных средствEpac signaling protein ligands as tools for studying their biological activity and creating new original drugshttps://orcid.org/0000-0003-2617-0334МокровГ. В.MokrovG. V.

Мокров Григорий Владимирович, SPIN-код: 8755-7666, к. х. н., в. н. с. лаборатории тонкого органического синтеза отдела химии лекарственных средств, Москва

Mokrov Grigory, SPIN code: 8755-7666, Candidate of Chemical Sciences, Leading researcher of the fine organic synthesis laboratory at the medicinal chemistry department, Moscow

g.mokrov@gmail.comhttps://orcid.org/0000-0003-1717-4659НикифороваТ. Д.NikiforovaT. D.

Никифорова Татьяна Дмитриевна, SPIN-код: 8593-9450, лаборант-исследователь лабаротории фармакологического скрининга, Москва

Nikiforova Tatiana, SPIN code: 8593-9450, Laboratory assistant-researcher of laboratory of pharmacological screening, Moscow

https://orcid.org/0000-0003-2832-4739КрыжановскийС. А.KryzhanovskiyS. A.

Крыжановский Сергей Александрович, SPIN-код: 6596-4865, д. м. н., заведующий лабораторией фармакологического скрининга, Москва

Kryzhanovskii Sergey, SPIN code: 6596-4865, Doctor of Medical Sciences, Head of laboratory of pharmacological screening, Moscow

ФГБНУ «НИИ фармакологии имени В.В. Закусова»РоссияFSBI «Zakusov Institute of Pharmacology»Russian Federation20192704202004317Copyright © Мокров Г.В., Никифорова Т.Д., Крыжановский С.А., 20202020Мокров Г.В., Никифорова Т.Д., Крыжановский С.А.Mokrov G.V., Nikiforova T.D., Kryzhanovskiy S.A.Данная работа распространяется под лицензией Creative Commons Attribution 4.0.This work is licensed under a Creative Commons Attribution 4.0 License.https://www.pharmacokinetica.ru/jour/article/view/226

В обзоре рассмотрены современные представления о строении и функциях белков Ерас (exchange proteins directly activated by cAMP, обменные белки, напрямую активируемые циклическим аденозинмонофосфатом). Вовлечённость белков Ерас как в регуляцию физиологических функций организма, так и в инициации различных патологических процессов позволяет рассматривать их как принципиально новую биомишень для создания оригинальных, высокоэффективных лекарственных средств. Собраны сведения о существующих агонистах и антагонистах белков Ерас, проанализировано влияние строения лигандов Ерас на значения их аффинности и селективности. Представлены предполагаемые механизмы взаимодействия лигандов с белками Ерас.

The review discusses modern views about the structure and functions of Epac proteins (exchange proteins directly activated by cyclic adenosine monophosphate). The involvement of Epac proteins both in the regulation of the physiological functions of the body and in the initiation of various pathological processes allows to consider them as a fundamentally new biological target for creating original, highly effective drugs. Information on existing Epac protein agonists and antagonists was collected, and the influence of Epac ligands structure on the values of their affinity and selectivity was analyzed. Presumptive mechanisms of the interaction of ligands with Epac proteins are presented.

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The authors declare that there are no conflicts of interest present.