Structure-guided design of potent and selective pyrimidylpyrrole inhibitors of extracellular signal-regulated kinase (ERK) using conformational control
about
In-gel activity-based protein profiling of a clickable covalent ERK1/2 inhibitorReactivation of ERK signaling causes resistance to EGFR kinase inhibitors.A genome-scale RNA interference screen implicates NF1 loss in resistance to RAF inhibition.CSAR benchmark exercise 2011-2012: evaluation of results from docking and relative ranking of blinded congeneric seriesDocking challenge: protein sampling and molecular docking performance.Transcription factor Etv5 is essential for the maintenance of alveolar type II cells.Rational design of non-resistant targeted cancer therapiesSmall-molecule inhibitors of the ERK signaling pathway: Towards novel anticancer therapeutics.Chiral kinase inhibitors.Amphiregulin and PTEN evoke a multimodal mechanism of acquired resistance to PI3K inhibitionStructure-based virtual screening of glycogen synthase kinase 3β inhibitors: analysis of scoring functions applied to large true actives and decoy sets.A melanoma cell state distinction influences sensitivity to MAPK pathway inhibitors.Ras/Raf/MEK/ERK and PI3K/PTEN/Akt/mTOR cascade inhibitors: how mutations can result in therapy resistance and how to overcome resistance.The cellular thermal shift assay for evaluating drug target interactions in cells.Inhibition of ERK1/2 down-regulates the Hippo/YAP signaling pathway in human NSCLC cells.Computational design, chemical synthesis, and biological evaluation of a novel ERK inhibitor (BL-EI001) with apoptosis-inducing mechanisms in breast cancer.Regulation of cell proliferation by ERK and signal-dependent nuclear translocation of ERK is dependent on Tm5NM1-containing actin filaments.Small-Molecule Inhibitors of GSK-3: Structural Insights and Their Application to Alzheimer's Disease ModelsCombined Pan-RAF and MEK Inhibition Overcomes Multiple Resistance Mechanisms to Selective RAF Inhibitors.MicroSCALE screening reveals genetic modifiers of therapeutic response in melanoma.Slow inhibition and conformation selective properties of extracellular signal-regulated kinase 1 and 2 inhibitorsPersonalized Preclinical Trials in BRAF Inhibitor-Resistant Patient-Derived Xenograft Models Identify Second-Line Combination Therapies.Targeting RAS-mutant cancers: is ERK the key?Phosphoproteome analysis of the MAPK pathway reveals previously undetected feedback mechanisms.The RAF-MEK-ERK pathway: targeting ERK to overcome obstacles to effective cancer therapy.Phenotypic Characterization of a Comprehensive Set of MAPK1/ERK2 Missense Mutants.Anti-angiogenic activity of thienopyridine derivative LCB03-0110 by targeting VEGFR-2 and JAK/STAT3 Signalling.Cooperative induction of apoptosis in NRAS mutant melanoma by inhibition of MEK and ROCK.ERK mutations confer resistance to mitogen-activated protein kinase pathway inhibitors.A unique inhibitor binding site in ERK1/2 is associated with slow binding kinetics.Vertical inhibition of the MAPK pathway enhances therapeutic responses in NRAS-mutant melanoma.Differential activity of MEK and ERK inhibitors in BRAF inhibitor resistant melanoma.A melanocyte lineage program confers resistance to MAP kinase pathway inhibition.Computation of relative binding free energy for an inhibitor and its analogs binding with Erk kinase using thermodynamic integration MD simulation.Prediction of amino acid positions specific for functional groups in a protein family based on local sequence similarity.Structure, signaling and the drug discovery of the Ras oncogene protein.Structure-Guided Strategy for the Development of Potent Bivalent ERK Inhibitors.Molecular profiling and combinatorial activity of CCT068127: a potent CDK2 and CDK9 inhibitor.A high throughput assay to identify substrate-selective inhibitors of the ERK protein kinases.Differential sensing of MAP kinases using SOX-peptides.
P2860
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P2860
Structure-guided design of potent and selective pyrimidylpyrrole inhibitors of extracellular signal-regulated kinase (ERK) using conformational control
description
2009 nî lūn-bûn
@nan
2009 թուականի Հոկտեմբերին հրատարակուած գիտական յօդուած
@hyw
2009 թվականի հոտեմբերին հրատարակված գիտական հոդված
@hy
2009年の論文
@ja
2009年論文
@yue
2009年論文
@zh-hant
2009年論文
@zh-hk
2009年論文
@zh-mo
2009年論文
@zh-tw
2009年论文
@wuu
name
Structure-guided design of pot ...... ) using conformational control
@ast
Structure-guided design of pot ...... ) using conformational control
@en
Structure-guided design of pot ...... ) using conformational control
@nl
type
label
Structure-guided design of pot ...... ) using conformational control
@ast
Structure-guided design of pot ...... ) using conformational control
@en
Structure-guided design of pot ...... ) using conformational control
@nl
prefLabel
Structure-guided design of pot ...... ) using conformational control
@ast
Structure-guided design of pot ...... ) using conformational control
@en
Structure-guided design of pot ...... ) using conformational control
@nl
P2093
P356
P1476
Structure-guided design of pot ...... ) using conformational control
@en
P2093
Alex M Aronov
Ernst ter Haar
Francois Maltais
Gabriel Martinez-Botella
Guanjing Chen
Guy W Bemis
James W Janetka
Jeremy Green
Jingrong Cao
Judy Straub
P304
P356
10.1021/JM900630Q
P407
P577
2009-10-22T00:00:00Z