Can We Pharmacologically Target Dishevelled: The Key Signal
Transducer in the Wnt Pathways?

C 2021

Can We Pharmacologically Target Dishevelled: The Key Signal Transducer in the Wnt Pathways?

MICKA, Miroslav a Vítězslav BRYJA

Základní údaje

Originální název

Can We Pharmacologically Target Dishevelled: The Key Signal Transducer in the Wnt Pathways?

Autoři

MICKA, Miroslav (203 Česká republika, domácí) a Vítězslav BRYJA (203 Česká republika, domácí)

Vydání

Cham (Švýcarsko), Pharmacology of the WNT Signaling System, od s. 117-135, 19 s. Handbook of Experimental Pharmacology, vol. 269, 2021

Nakladatel

Springer

Další údaje

Jazyk

angličtina

Typ výsledku

Kapitola resp. kapitoly v odborné knize

Obor

30104 Pharmacology and pharmacy

Stát vydavatele

Švýcarsko

Utajení

není předmětem státního či obchodního tajemství

Forma vydání

tištěná verze "print"

Odkazy

URL

Kód RIV

RIV/00216224:14310/21:00123816

Organizační jednotka

Přírodovědecká fakulta

ISBN

978-3-030-85498-0

DOI

http://dx.doi.org/10.1007/164_2021_527

Klíčová slova anglicky

Casein kinase 1; Dishevelled; DIX oligomerization; PDZ inhibitors; Wnt signalling-related diseases

Štítky

rivok, topvydavatel

Příznaky

Mezinárodní význam, Recenzováno

Změněno: 23. 3. 2022 09:16, Mgr. Marie Šípková, DiS.

Anotace

V originále

Dishevelled (DVL) is the central signal transducer in both Wnt/β-catenin-dependent and independent signalling pathways. DVL is required to connect receptor complexes and downstream effectors. Since proximal Wnt pathway components and DVL itself are upregulated in many types of cancer, DVL represents an attractive therapeutic target in the Wnt-addicted cancers and other disorders caused by aberrant Wnt signalling. Here, we discuss progress in several approaches for the modulation of DVL function and hence inhibition of the Wnt signalling. Namely, we sum up the potential of modulation of enzymes that control post-translational modification of DVL - such as inhibition of DVL kinases or promotion of DVL ubiquitination and degradation. In addition, we discuss research directions that can take advantage of direct interaction with the protein domains essential for DVL function: the inhibition of DIX- and DEP-domain mediated polymerization and interaction of DVL PDZ domain with its ligands.

Návaznosti

EF16_025/0007381, projekt VaV

Název: Preklinická progrese nových organických sloučenin s cílenou biologickou aktivitou

Citovat

MICKA, Miroslav a Vítězslav BRYJA. Can We Pharmacologically Target Dishevelled: The Key Signal Transducer in the Wnt Pathways? In Schulte G., Kozielewicz P. Pharmacology of the WNT Signaling System. Cham (Švýcarsko): Springer, 2021, s. 117-135. Handbook of Experimental Pharmacology, vol. 269. ISBN 978-3-030-85498-0. Dostupné z: https://dx.doi.org/10.1007/164_2021_527.

@inbook{1823457,
   author = {Micka, Miroslav and Bryja, Vítězslav},
   address = {Cham (Švýcarsko)},
   booktitle = {Pharmacology of the WNT Signaling System},
   doi = {http://dx.doi.org/10.1007/164_2021_527},
   editor = {Schulte G., Kozielewicz P.},
   keywords = {Casein kinase 1; Dishevelled; DIX oligomerization; PDZ inhibitors; Wnt signalling-related diseases},
   howpublished = {tištěná verze "print"},
   language = {eng},
   location = {Cham (Švýcarsko)},
   isbn = {978-3-030-85498-0},
   pages = {117-135},
   publisher = {Springer},
   title = {Can We Pharmacologically Target Dishevelled: The Key Signal Transducer in the Wnt Pathways?},
   url = {https://link.springer.com/chapter/10.1007/164_2021_527},
   year = {2021}
}

TY  - CHAP
ID  - 1823457
AU  - Micka, Miroslav - Bryja, Vítězslav
PY  - 2021
TI  - Can We Pharmacologically Target Dishevelled: The Key Signal Transducer in the Wnt Pathways?
VL  - Handbook of Experimental Pharmacology, vol. 269
PB  - Springer
CY  - Cham (Švýcarsko)
SN  - 9783030854980
KW  - Casein kinase 1
KW  - Dishevelled
KW  - DIX oligomerization
KW  - PDZ inhibitors
KW  - Wnt signalling-related diseases
UR  - https://link.springer.com/chapter/10.1007/164_2021_527
N2  - Dishevelled (DVL) is the central signal transducer in both Wnt/β-catenin-dependent and independent signalling pathways. DVL is required to connect receptor complexes and downstream effectors. Since proximal Wnt pathway components and DVL itself are upregulated in many types of cancer, DVL represents an attractive therapeutic target in the Wnt-addicted cancers and other disorders caused by aberrant Wnt signalling. Here, we discuss progress in several approaches for the modulation of DVL function and hence inhibition of the Wnt signalling. Namely, we sum up the potential of modulation of enzymes that control post-translational modification of DVL - such as inhibition of DVL kinases or promotion of DVL ubiquitination and degradation. In addition, we discuss research directions that can take advantage of direct interaction with the protein domains essential for DVL function: the inhibition of DIX- and DEP-domain mediated polymerization and interaction of DVL PDZ domain with its ligands.
ER  -

MICKA, Miroslav a Vítězslav BRYJA. Can We Pharmacologically Target Dishevelled: The Key Signal Transducer in the Wnt Pathways? In Schulte G., Kozielewicz P. \textit{Pharmacology of the WNT Signaling System}. Cham (Švýcarsko): Springer, 2021, s.~117-135. Handbook of Experimental Pharmacology, vol. 269. ISBN~978-3-030-85498-0. Dostupné z: https://dx.doi.org/10.1007/164\_{}2021\_{}527.

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