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Small-molecule inhibitors of cyclophilin D as potential therapeutics in mitochondria-related diseases

The result's identifiers

  • Result code in IS VaVaI

    <a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00179906%3A_____%2F22%3A10446725" target="_blank" >RIV/00179906:_____/22:10446725 - isvavai.cz</a>

  • Alternative codes found

    RIV/62690094:18470/22:50019183

  • Result on the web

    <a href="https://verso.is.cuni.cz/pub/verso.fpl?fname=obd_publikace_handle&handle=lPrb5aR5BA" target="_blank" >https://verso.is.cuni.cz/pub/verso.fpl?fname=obd_publikace_handle&handle=lPrb5aR5BA</a>

  • DOI - Digital Object Identifier

    <a href="http://dx.doi.org/10.1002/med.21892" target="_blank" >10.1002/med.21892</a>

Alternative languages

  • Result language

    angličtina

  • Original language name

    Small-molecule inhibitors of cyclophilin D as potential therapeutics in mitochondria-related diseases

  • Original language description

    Cyclophilin D (CypD) is a key regulator of mitochondrial permeability transition pore (mPTP) opening. This pathophysiological phenomenon is associated with the development of several human diseases, including ischemia-reperfusion injury and neurodegeneration. Blocking mPTP opening through CypD inhibition could be a novel and promising therapeutic approach for these conditions. While numerous CypD inhibitors have been discovered to date, none have been introduced into clinical practice, mostly owing to their high toxicity, unfavorable pharmacokinetics, and low selectivity for CypD over other cyclophilins. This review summarizes current knowledge of CypD inhibitors, with a particular focus on small-molecule compounds with regard to their in vitro activity, their selectivity for CypD, and their binding mode within the enzyme&apos;s active site. Finally, approaches for improving the molecular design of CypD inhibitors are discussed.

  • Czech name

  • Czech description

Classification

  • Type

    J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database

  • CEP classification

  • OECD FORD branch

    30104 - Pharmacology and pharmacy

Result continuities

  • Project

    Result was created during the realization of more than one project. More information in the Projects tab.

  • Continuities

    P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Others

  • Publication year

    2022

  • Confidentiality

    S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Data specific for result type

  • Name of the periodical

    Medicinal Research Reviews

  • ISSN

    0198-6325

  • e-ISSN

    1098-1128

  • Volume of the periodical

    42

  • Issue of the periodical within the volume

    5

  • Country of publishing house

    US - UNITED STATES

  • Number of pages

    34

  • Pages from-to

    1822-1855

  • UT code for WoS article

    000795933400001

  • EID of the result in the Scopus database

    2-s2.0-85132598116