Cargando…

Small molecule induced reactivation of mutant p53 in cancer cells

The p53 cancer mutant Y220C is an excellent paradigm for rescuing the function of conformationally unstable p53 mutants because it has a unique surface crevice that can be targeted by small-molecule stabilizers. Here, we have identified a compound, PK7088, which is active in vitro: PK7088 bound to t...

Descripción completa

Detalles Bibliográficos
Autores principales:	Liu, Xiangrui, Wilcken, Rainer, Joerger, Andreas C., Chuckowree, Irina S., Amin, Jahangir, Spencer, John, Fersht, Alan R.
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	Oxford University Press 2013
Materias:	Gene Regulation, Chromatin and Epigenetics
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3695503/ https://www.ncbi.nlm.nih.gov/pubmed/23630318 http://dx.doi.org/10.1093/nar/gkt305

Ejemplares similares

Modulation of gene expression in U251 glioblastoma cells by binding of mutant p53 R273H to intronic and intergenic sequences
por: Brázdová, Marie, et al.
Publicado: (2009)

Testing mechanisms of DNA sliding by architectural DNA-binding proteins: dynamics of single wild-type and mutant protein molecules in vitro and in vivo
por: Kamagata, Kiyoto, et al.
Publicado: (2021)

Optimisation of TP53 reporters by systematic dissection of synthetic TP53 response elements
por: Trauernicht, Max, et al.
Publicado: (2023)

Diverse targets of SMN2-directed splicing-modulating small molecule therapeutics for spinal muscular atrophy
por: Ottesen, Eric W, et al.
Publicado: (2023)

STAT1:DNA sequence-dependent binding modulation by phosphorylation, protein:protein interactions and small-molecule inhibition
por: Bonham, Andrew J., et al.
Publicado: (2013)

Critical role for p53-serine 15 phosphorylation in stimulating transactivation at p53-responsive promoters
por: Loughery, Jayne, et al.
Publicado: (2014)

Inhibition of p53 acetylation by INHAT subunit SET/TAF-Iβ represses p53 activity
por: Kim, Ji-Young, et al.
Publicado: (2012)

Single-molecule compaction of megabase-long chromatin molecules by multivalent cations
por: Zinchenko, Anatoly, et al.
Publicado: (2018)

The complex architecture of p53 binding sites
por: Senitzki, Alon, et al.
Publicado: (2021)

Formation of stress-specific p53 binding patterns is influenced by chromatin but not by modulation of p53 binding affinity to response elements(†)
por: Millau, Jean-François, et al.
Publicado: (2011)

Genome-wide characterization reveals complex interplay between TP53 and TP63 in response to genotoxic stress
por: McDade, Simon S., et al.
Publicado: (2014)

KDM4B/JMJD2B is a p53 target gene that modulates the amplitude of p53 response after DNA damage
por: Castellini, Laura, et al.
Publicado: (2017)

p53 regulates enhancer accessibility and activity in response to DNA damage
por: Younger, Scott T., et al.
Publicado: (2017)

Distinctive Klf4 mutants determine preference for DNA methylation status
por: Hashimoto, Hideharu, et al.
Publicado: (2016)

Exploiting Transient Protein States for the Design of Small-Molecule Stabilizers of Mutant p53
por: Joerger, Andreas C., et al.
Publicado: (2015)

Two p53 tetramers bind one consensus DNA response element
por: Kearns, Sinéad, et al.
Publicado: (2016)

Sam68 functions as a transcriptional coactivator of the p53 tumor suppressor
por: Li, Naomi, et al.
Publicado: (2016)

Genome-wide DNA methylation analysis in cohesin mutant human cell lines
por: Liu, Jinglan, et al.
Publicado: (2010)

MEF/ELF4 transactivation by E2F1 is inhibited by p53
por: Taura, Manabu, et al.
Publicado: (2011)

Transcriptional repressor NIR interacts with the p53-inhibiting ubiquitin ligase MDM2
por: Heyne, Kristina, et al.
Publicado: (2014)

Heat shock factor-1 modulates p53 activity in the transcriptional response to DNA damage
por: Logan, Ian R., et al.
Publicado: (2009)

Integrative genomic analysis reveals widespread enhancer regulation by p53 in response to DNA damage
por: Younger, Scott T., et al.
Publicado: (2015)

Locally acting transcription factors regulate p53-dependent cis-regulatory element activity
por: Catizone, Allison N, et al.
Publicado: (2020)

Phosphorylation and ubiquitination-dependent degradation of CABIN1 releases p53 for transactivation upon genotoxic stress
por: Choi, Soo-Youn, et al.
Publicado: (2013)

DREAM and RB cooperate to induce gene repression and cell-cycle arrest in response to p53 activation
por: Uxa, Sigrid, et al.
Publicado: (2019)

Transcription factor RFX7 governs a tumor suppressor network in response to p53 and stress
por: Coronel, Luis, et al.
Publicado: (2021)

P-TEFb promotes cell survival upon p53 activation by suppressing intrinsic apoptosis pathway
por: Wang, Zhijia, et al.
Publicado: (2023)

Promiscuous DNA-binding of a mutant zinc finger protein corrupts the transcriptome and diminishes cell viability
por: Gillinder, Kevin R., et al.
Publicado: (2017)

Quantitative analysis of single-molecule force spectroscopy on folded chromatin fibers
por: Meng, He, et al.
Publicado: (2015)

Diverse stresses dramatically alter genome-wide p53 binding and transactivation landscape in human cancer cells
por: Menendez, Daniel, et al.
Publicado: (2013)

Rotational positioning of nucleosomes facilitates selective binding of p53 to response elements associated with cell cycle arrest
por: Cui, Feng, et al.
Publicado: (2014)

Ablation of PRMT6 reveals a role as a negative transcriptional regulator of the p53 tumor suppressor
por: Neault, Mathieu, et al.
Publicado: (2012)

p53-Independent regulation of p21Waf1/Cip1 expression and senescence by PRMT6
por: Phalke, Sameer, et al.
Publicado: (2012)

A dominant-negative SOX18 mutant disrupts multiple regulatory layers essential to transcription factor activity
por: McCann, Alex J, et al.
Publicado: (2021)

Linking folding dynamics and function of SAM/SAH riboswitches at the single molecule level
por: Liao, Ting-Wei, et al.
Publicado: (2023)

DNA damage induced p53 downregulates Cdc20 by direct binding to its promoter causing chromatin remodeling
por: Banerjee, Taraswi, et al.
Publicado: (2009)

The p53-p21-DREAM-CDE/CHR pathway regulates G(2)/M cell cycle genes
por: Fischer, Martin, et al.
Publicado: (2016)

R-loops do not accumulate in transcription-defective hpr1-101 mutants: implications for the functional role of THO/TREX
por: Gómez-González, Belén, et al.
Publicado: (2009)

Construction and functional analyses of a comprehensive σ(54) site-directed mutant library using alanine–cysteine mutagenesis
por: Xiao, Yan, et al.
Publicado: (2009)

RNA polymerase III mutants in TFIIFα-like C37 that cause terminator readthrough with no decrease in transcription output
por: Rijal, Keshab, et al.
Publicado: (2013)

Cannot write session to /tmp/vufind_sessions/sess_d7d6rnt4doitmidmmp3mbki1aj