Cargando…

Unravelling the effect of the E545K mutation on PI3Kα kinase

PI3Kα controls several cellular processes and its aberrant signalling is implicated in tumorigenesis. One of its hotspot mutations, E545K, increases PI3Kα lipid kinase activity, but its mode of action is only partially understood. Here, we perform biased and unbiased molecular dynamics simulations o...

Descripción completa

Detalles Bibliográficos
Autores principales:	Galdadas, Ioannis, Gervasio, Francesco Luigi, Cournia, Zoe
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	The Royal Society of Chemistry 2020
Materias:	Chemistry
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8493679/ https://www.ncbi.nlm.nih.gov/pubmed/34703536 http://dx.doi.org/10.1039/c9sc05903b

Ejemplares similares

Insights into the mechanism of the PIK3CA E545K activating mutation using MD simulations
por: Leontiadou, Hari, et al.
Publicado: (2018)

The effect of S427F mutation on RXRα activity depends on its dimeric partner
por: Galdadas, Ioannis, et al.
Publicado: (2021)

The orchestrated signaling by PI3Kα and PTEN at the membrane interface
por: Kotzampasi, Danai Maria, et al.
Publicado: (2022)

Prevalence and prognostic role of PIK3CA E545K mutation in Iranian colorectal cancer patients
por: Ranjbar, Reza, et al.
Publicado: (2019)

The mechanism of PI3Kα activation at the atomic level
por: Zhang, Mingzhen, et al.
Publicado: (2019)

The E545K mutation of PIK3CA promotes gallbladder carcinoma progression through enhanced binding to EGFR
por: Zhao, Shuai, et al.
Publicado: (2016)

Phosphatidyl inositol-3 kinase (PIK3CA) E545K mutation confers cisplatin resistance and a migratory phenotype in cervical cancer cells
por: Arjumand, Wani, et al.
Publicado: (2016)

The PIK3CA E542K and E545K mutations promote glycolysis and proliferation via induction of the β-catenin/SIRT3 signaling pathway in cervical cancer
por: Jiang, Wei, et al.
Publicado: (2018)

Mozart K.545 Mimics Mozart K.448 in Reducing Epileptiform Discharges in Epileptic Children
por: Lin, Lung-Chang, et al.
Publicado: (2012)

Elaborating piperazinyl-furopyrimidine based scaffolds as phosphoinositol-3-kinase enzyme alpha (PI3Kα) inhibitors to combat pancreatic cancer
por: Mansour, Mai A., et al.
Publicado: (2020)

Discovery of a novel phosphoinositide 3-kinase gamma (PI3Kγ) inhibitor against hematologic malignancies and theoretical studies on its PI3Kγ-specific binding mechanisms
por: Zhu, Jingyu, et al.
Publicado: (2019)

Allosteric activation of PI3Kα by oncogenic mutations
por: Burke, John E., et al.
Publicado: (2013)

Structural basis of the effect of activating mutations on the EGF receptor
por: Galdadas, Ioannis, et al.
Publicado: (2021)

Cryo-EM structures of cancer-specific helical and kinase domain mutations of PI3Kα
por: Liu, Xiao, et al.
Publicado: (2022)

Synthesis and bioevaluation of thienopyrimidines bearing a pyrazoline unit as selective PI3Kα inhibitors
por: Lai, Luogen, et al.
Publicado: (2019)

The rational design of ARUK2007145, a dual inhibitor of the α and γ isoforms of the lipid kinase phosphatidylinositol 5-phosphate 4-kinase (PI5P4K)
por: Aldred, Gregory G., et al.
Publicado: (2023)

PI3K inhibitors: review and new strategies
por: Zhang, Mingzhen, et al.
Publicado: (2020)

Inhibition of phosphatidylinositol 3‐kinase α (PI3Kα) prevents heterotopic ossification
por: Valer, José Antonio, et al.
Publicado: (2019)

Identification of ARUK2002821 as an isoform-selective PI5P4Kα inhibitor
por: Willems, Henriëtte M. G., et al.
Publicado: (2023)

Molecular docking and dynamics based approach for the identification of kinase inhibitors targeting PI3Kα against non-small cell lung cancer: a computational study
por: Halder, Debojyoti, et al.
Publicado: (2022)

Phosphatidylinositide 3-kinase (PI3K) and PI3K-related kinase (PIKK) activity contributes to radioresistance in thyroid carcinomas
por: Burrows, Natalie, et al.
Publicado: (2016)

Observation of the decay $K_{S} \to\pi^{+}\pi^{-} e^{+} e^{-}$
por: Lai, A, et al.
Publicado: (2000)

ZNF545 suppresses human hepatocellular carcinoma growth by inhibiting NF-kB signaling
por: Yang, Weili, et al.
Publicado: (2017)

Precision measurement of the ratio BR($K_{S} \to \pi^{+}\pi^{-}e^{+}e^{-}$)/BR($K_{L} \to \pi^{+}\pi^{-}\pi^{0}_{D}$)
por: Batley, J R, et al.
Publicado: (2010)

Selection Study for B+- -> (K-+ pi+- pi-+ pi+-)D K+- and B+- -> (K+ K- pi+ pi-)D K+-".
por: Hunt, P, et al.
Publicado: (2009)

Monte Carlo Generator for the Processes e^+e^- \to e^+e^-, \mu^+\mu^-, \pi^+\pi^- and K^+K^-, K_L K_S with precise Radiative Corrections at Low Energies
por: Arbuzov, A B, et al.
Publicado: (2004)

Determination of the branching ratios $\Gamma(K_{L} \to 3\pi^{0}) / \Gamma(K_{L} \to \pi^{+}\pi^{-}\pi^{0})$ and $\Gamma(K_{L} \to 3\pi^{0}) / \Gamma(K_{L} \to \pi e\nu)$
por: Kreutz, A., et al.
Publicado: (1994)

Differential Effects of Phosphatidylinositol 4-Kinase (PI4K) and 3-Kinase (PI3K) Inhibitors on Stomatal Responses to Environmental Signals
por: Takahashi, Sho, et al.
Publicado: (2017)

Study of E/i Decays into $K\overline{K}\pi$ in the reaction $\overline{p}p$ --> E/i $\pi\pi$
por: Bertin, A, et al.
Publicado: (1996)

Determination of the relative decay rate $K_{S} \to \pi e \nu$ / $K_{L} \to \pi e \nu$
por: Batley, J R, et al.
Publicado: (2007)

Measurements of $K_{e4}$ and $K^{\pm} \to \pi^{0} \pi^{0} \pi^{\pm}$ decays
por: Masetti, L.
Publicado: (2006)

PI3Kα Inhibitors That Inhibit Metastasis
por: Schmidt-Kittler, Oleg, et al.
Publicado: (2010)

The role of PI3Kα isoform in cardioprotection
por: Rossello, Xavier, et al.
Publicado: (2017)

The investigation of $K^+\pi^−, \pi^+K^−$ and $\pi^+\pi^−$ atoms
por: Yazkov, Valeriy
Publicado: (2016)

$K_{A} \rightarrow K^{*} \pi and K^{*} \rightarrow K \pi$ decays
por: Srivastava, P P
Publicado: (1967)

Activation of PKCα and PI3K Kinases in Hypertrophic and Nodular Port Wine Stain Lesions
por: Yin, Rong, et al.
Publicado: (2017)

Measurement of $Br(K_{s} \to \pi^{\pm}e^{\mp} \nu_{e})$ and $\Delta m = m_{K_{L}} - m_{K_{S}}$ in $K_{S,L} \to \pi^{\pm}e^{\mp}\nu_{e}$ decays
por: Morales Cristina
Publicado: (2013)

Prospects for the search of $K^{0}_{S} \to \pi^{+}\pi^{-}e^{+}e^{-}$ at LHCb
por: Marin Benito, C
Publicado: (2017)

Prospects for the search of$ K^0_S \to \pi^+ \pi^- e^+ e^-$ at LHCb
por: Marin Benito, Carla
Publicado: (2016)

Investigation of $K_{L,S} \rightarrow \pi^{+}\pi^{-}e^{+}e^{-}$ decays
por: Lai, A, et al.
Publicado: (2003)

Cannot write session to /tmp/vufind_sessions/sess_amcme2htv0kslqskjmr4r358da