Specific CLK inhibitors from a novel chemotype for regulation of alternative splicing.

Specific CLK inhibitors from a novel chemotype for regulation of alternative splicing.

Weitere Versionen anzeigen (1)

There is a growing recognition of the importance of protein kinases in the control of alternative splicing. To define the underlying regulatory mechanisms, highly selective inhibitors are needed. Here, we report the discovery and characterization of the dichloroindolyl enaminonitrile KH-CB19, a pote...

Ausführliche Beschreibung

Bibliographische Detailangaben
Hauptverfasser:	Fedorov, O, Huber, K, Eisenreich, A, Filippakopoulos, P, King, O, Bullock, A, Szklarczyk, D, Jensen, L, Fabbro, D, Trappe, J, Rauch, U, Bracher, F, Knapp, S
Format:	Journal article
Sprache:	English
Veröffentlicht:	2011

Ähnliche Einträge

Specific CLK inhibitors from a novel chemotype for regulation of alternative splicing.
von: Fedorov, O, et al.
Veröffentlicht: (2011)

7,8-dichloro-1-oxo-β-carbolines as a versatile scaffold for the development of potent and selective kinase inhibitors with unusual binding modes.
von: Huber, K, et al.
Veröffentlicht: (2012)

Regulation of influenza A virus mRNA splicing by CLK1
von: Artarini, A, et al.
Veröffentlicht: (2019)

CLK2 blockade modulates alternative splicing compromising MYC‐driven breast tumors
von: Fernando Salvador, et al.
Veröffentlicht: (2018-05-01)

Pharmacological inhibition of CLK2 activates YAP by promoting alternative splicing of AMOTL2
von: Maya L Bulos, et al.
Veröffentlicht: (2023-12-01)

Kinase domain insertions define distinct roles of CLK kinases in SR protein phosphorylation.
von: Bullock, A, et al.
Veröffentlicht: (2009)

Kinase domain insertions define distinct roles of CLK kinases in SR protein phosphorylation
von: Bullock, A, et al.
Veröffentlicht: (2009)

Hypoxia leads to significant changes in alternative splicing and elevated expression of CLK splice factor kinases in PC3 prostate cancer cells
von: Elizabeth Bowler, et al.
Veröffentlicht: (2018-04-01)

Leucettines, a class of potent inhibitors of cdc2-like kinases and dual specificity, tyrosine phosphorylation regulated kinases derived from the marine sponge leucettamine B: modulation of alternative pre-RNA splicing.
von: Debdab, M, et al.
Veröffentlicht: (2011)

Anti‐tumor efficacy of a novel CLK inhibitor via targeting RNA splicing and MYC‐dependent vulnerability
von: Kenichi Iwai, et al.
Veröffentlicht: (2018-05-01)

Inhibitors of CLK protein kinases suppress cell growth and induce apoptosis by modulating pre-mRNA splicing.
von: Shinsuke Araki, et al.
Veröffentlicht: (2015-01-01)

DFG-1 residue controls inhibitor binding mode and affinity, providing a basis for rational design of kinase inhibitor selectivity
von: Schröder, M, et al.
Veröffentlicht: (2020)

Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family.
von: Filippakopoulos, P, et al.
Veröffentlicht: (2012)

Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family
von: Filippakopoulos, P, et al.
Veröffentlicht: (2012)

Clk/STY (cdc2-like kinase 1) and Akt regulate alternative splicing and adipogenesis in 3T3-L1 pre-adipocytes.
von: Pengfei Li, et al.
Veröffentlicht: (2013-01-01)

CLK1/CLK2-driven signalling at the Leishmania kinetochore is captured by spatially referenced proximity phosphoproteomics
von: Vincent Geoghegan, et al.
Veröffentlicht: (2022-11-01)

Dibenzofuran Derivatives Inspired from Cercosporamide as Dual Inhibitors of Pim and CLK1 Kinases
von: Viet Hung Dao, et al.
Veröffentlicht: (2021-10-01)

Targeting the CLK2/SRSF9 splicing axis in prostate cancer leads to decreased ARV7 expression
von: Jasper Van Goubergen, et al.
Veröffentlicht: (2025-02-01)

Synergistic apoptotic effects in cancer cells by the combination of CLK and Bcl-2 family inhibitors.
von: Aiko Murai, et al.
Veröffentlicht: (2020-01-01)

Molecular structures of cdc2-like kinases in complex with a new inhibitor chemotype
von: Walter, A, et al.
Veröffentlicht: (2018)

5-Methoxybenzothiophene-2-Carboxamides as Inhibitors of Clk1/4: Optimization of Selectivity and Cellular Potency
von: Ahmed K. ElHady, et al.
Veröffentlicht: (2021-02-01)

Molecular structures of cdc2-like kinases in complex with a new inhibitor chemotype.
von: Anne Walter, et al.
Veröffentlicht: (2018-01-01)

Inhibition of the SR protein-phosphorylating CLK kinases of Plasmodium falciparum impairs blood stage replication and malaria transmission.
von: Selina Kern, et al.
Veröffentlicht: (2014-01-01)

Structural analysis identifies imidazo[1,2-b]pyridazines as PIM kinase inhibitors with in vitro antileukemic activity.
von: Pogacic, V, et al.
Veröffentlicht: (2007)

CLK-dependent exon recognition and conjoined gene formation revealed with a novel small molecule inhibitor
von: Tyler Funnell, et al.
Veröffentlicht: (2017-02-01)

Diverse inhibitor chemotypes targeting Trypanosoma cruzi CYP51.
von: Shamila S Gunatilleke, et al.
Veröffentlicht: (2012-01-01)

Multicomponent mapping of boron chemotypes furnishes selective enzyme inhibitors
von: Joanne Tan, et al.
Veröffentlicht: (2017-11-01)

CLK3 promotes tumor proliferation by activating MYC signaling
von: Jing Shen, et al.
Veröffentlicht: (2024-09-01)

Identification of novel anti-amoebic pharmacophores from kinase inhibitor chemotypes
von: Lori Ferrins, et al.
Veröffentlicht: (2023-05-01)

Development of selective CBP/P300 benzoxazepine bromodomain inhibitors
von: Popp, T, et al.
Veröffentlicht: (2016)

CLK2 Condensates Reorganize Nuclear Speckles and Induce Intron Retention
von: Bing Wang, et al.
Veröffentlicht: (2024-10-01)

Design and synthesis of a library of lead-like 2,4-bisheterocyclic substituted thiophenes as selective Dyrk/Clk inhibitors.
von: Christian Schmitt, et al.
Veröffentlicht: (2014-01-01)

The design and synthesis of 5-and 6-isoxazolylbenzimidazoles as selective inhibitors of the BET bromodomains
von: Hay, D, et al.
Veröffentlicht: (2013)

Corrigendum: Identification of novel anti-amoebic pharmacophores from kinase inhibitor chemotypes
von: Lori Ferrins, et al.
Veröffentlicht: (2023-10-01)

Discrimination of fennel chemotypes applying IR and Raman spectroscopy – discovery of a new -asarone chemotype
von: Krähmer, Andrea, et al.
Veröffentlicht: (2016-07-01)

Calculation of Splicing Potential from the Alternative Splicing Mutation Database
von: Afonin Kirill A, et al.
Veröffentlicht: (2008-02-01)

Developing small molecule inhibitors of the CREBBP bromodomain-histone interaction
von: Rooney, T, et al.
Veröffentlicht: (2012)

The Alternative Splicing Mutation Database: a hub for investigations of alternative splicing using mutational evidence
von: Afonin Kirill A, et al.
Veröffentlicht: (2008-02-01)

Opposing roles of CLK SR kinases in controlling HIV-1 gene expression and latency
von: Subha Dahal, et al.
Veröffentlicht: (2022-08-01)

In depth investigation of the metabolism of Nectandra megapotamica chemotypes.
von: Katyuce de S Farias, et al.
Veröffentlicht: (2018-01-01)