Targeting Mitogen-Activated Protein Kinase-Activated Protein Kinase 2 (MAPKAPK2, MK2): Medicinal Chemistry Efforts To Lead Small Molecule Inhibitors to Clinical Trials (Q36849634)

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scientific article published on 26 October 2015

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English	Targeting Mitogen-Activated Protein Kinase-Activated Protein Kinase 2 (MAPKAPK2, MK2): Medicinal Chemistry Efforts To Lead Small Molecule Inhibitors to Clinical Trials	scientific article published on 26 October 2015

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28 February 2020

Targeting Mitogen-Activated Protein Kinase-Activated Protein Kinase 2 (MAPKAPK2, MK2): Medicinal Chemistry Efforts To Lead Small Molecule Inhibitors to Clinical Trials (English)

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Europe PubMed Central

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https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:26502061%20AND%20SRC:MED&resulttype=core&format=json

28 February 2020

Fabrizio Manetti

3

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28 February 2020

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Mario Fiore

1

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28 February 2020

Stefano Forli

2

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28 February 2020

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9 November 2015

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28 February 2020

Journal of Medicinal Chemistry

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28 February 2020

59

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28 February 2020

8

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28 February 2020

3609-3634

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28 February 2020

Design, synthesis, and biological evaluation of aminopyrazine derivatives as inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2).

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Sonic hedgehog stimulates glycolysis and proliferation of breast cancer cells: Modulation of PFKFB3 activation

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Investigational p38 inhibitors for the treatment of chronic obstructive pulmonary disease

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MMI-0100 inhibits cardiac fibrosis in myocardial infarction by direct actions on cardiomyocytes and fibroblasts via MK2 inhibition

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Discovery of a Potent Dihydrooxadiazole Series of Non-ATP-Competitive MK2 (MAPKAPK2) Inhibitors

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Discovery and Hit-to-Lead Optimization of Non-ATP Competitive MK2 (MAPKAPK2) Inhibitors

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Matrix stiffness affects endocytic uptake of MK2-inhibitor peptides

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Structure of the β-form of human MK2 in complex with the non-selective kinase inhibitor TEI-L03090

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Inhibition of hepatobiliary transporters by a novel kinase inhibitor contributes to hepatotoxicity in beagle dogs.

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Crystal structure of human cyclin-dependent kinase-2 complex with MK2 inhibitor TEI-I01800: insight into the selectivity

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Potency switch between CHK1 and MK2: discovery of imidazo[1,2-a]pyrazine- and imidazo[1,2-c]pyrimidine-based kinase inhibitors

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Peptide-mediated inhibition of mitogen-activated protein kinase-activated protein kinase-2 ameliorates bleomycin-induced pulmonary fibrosis

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LIM kinases are attractive targets with many macromolecular partners and only a few small molecule regulators

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Mitogen-activated protein kinase-activated protein kinase 2 (MAPKAP-K2) as an antiinflammatory target: discovery and in vivo activity of selective pyrazolo[1,5-a]pyrimidine inhibitors using a focused library and structure-based optimization approach

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Novel ATP competitive MK2 inhibitors with potent biochemical and cell-based activity throughout the series

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29 September 2017

Inhibition of Mitogen Activated Protein Kinase Activated Protein Kinase II with MMI-0100 reduces intimal hyperplasia ex vivo and in vivo

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29 September 2017

Inhibition of the protein kinase MK-2 protects podocytes from nephrotic syndrome-related injury

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29 September 2017

Cell-penetrating peptides can confer biological function: Regulation of inflammatory cytokines in human monocytes by MK2 inhibitor peptides

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29 September 2017

Structure-based lead identification of ATP-competitive MK2 inhibitors

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29 September 2017

Peptide inhibitors of MK2 show promise for inhibition of abdominal adhesions

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Enlarging the NSAIDs family: ether, ester and acid derivatives of the 1,5-diarylpyrrole scaffold as novel anti-inflammatory and analgesic agents.

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Low-molecular-weight MK2 inhibitors: a tough nut to crack!

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Identification and Mechanism of Action of the Acylguanidine MRT-83, a Novel Potent Smoothened Antagonist

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29 September 2017

A novel cell permeant peptide inhibitor of MAPKAP kinase II inhibits intimal hyperplasia in a human saphenous vein organ culture model

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29 September 2017

Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases

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29 September 2017

Virtual screening-based discovery and mechanistic characterization of the acylthiourea MRT-10 family as smoothened antagonists.

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29 September 2017

4-Anilino-6-phenyl-quinoline inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK2).

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29 September 2017

MAPKAP kinases MK2 and MK3 in inflammation: complex regulation of TNF biosynthesis via expression and phosphorylation of tristetraprolin

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29 September 2017

In vivo and in vitro SAR of tetracyclic MAPKAP-K2 (MK2) inhibitors. Part II

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29 September 2017

MAPK-activated protein kinase-2 in cardiac hypertrophy and cyclooxygenase-2 regulation in heart

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29 September 2017

A benzothiophene inhibitor of mitogen-activated protein kinase-activated protein kinase 2 inhibits tumor necrosis factor alpha production and has oral anti-inflammatory efficacy in acute and chronic models of inflammation

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29 September 2017

Novel 3-aminopyrazole inhibitors of MK-2 discovered by scaffold hopping strategy

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29 September 2017

Structural analysis of an MK2-inhibitor complex: insight into the regulation of the secondary structure of the Gly-rich loop by TEI-I01800

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29 September 2017

2,4-Diaminopyrimidine MK2 inhibitors. Part I: Observation of an unexpected inhibitor binding mode

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29 September 2017

Design of a bioactive cell-penetrating peptide: when a transduction domain does more than transduce

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29 September 2017

Benzothiophene inhibitors of MK2. Part 1: structure-activity relationships, assessments of selectivity and cellular potency

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29 September 2017

Benzothiophene inhibitors of MK2. Part 2: improvements in kinase selectivity and cell potency

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Targeting innate immunity protein kinase signalling in inflammation

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29 September 2017

Novel 1-(2-aminopyrazin-3-yl)methyl-2-thioureas as potent inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2).

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29 September 2017

Identification and SAR of squarate inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2)

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Rational mutagenesis to support structure-based drug design: MAPKAP kinase 2 as a case study

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Targeting protein kinases for the development of anti-inflammatory drugs

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Synthesis and in vivo activity of MK2 and MK2 substrate-selective p38alpha(MAPK) inhibitors in Werner syndrome cells

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Lack of MK2 inhibits myofibroblast formation and exacerbates pulmonary fibrosis

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The discovery of carboline analogs as potent MAPKAP-K2 inhibitors

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Pyrrolopyridine inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2)

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29 September 2017

Structural basis for a high affinity inhibitor bound to protein kinase MK2

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29 September 2017

Molecular basis of MAPK-activated protein kinase 2:p38 assembly

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29 September 2017

Crystal structure of the p38 alpha-MAPKAP kinase 2 heterodimer

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29 September 2017

Mitogen-activated protein kinase-activated protein kinase 2 regulates tumor necrosis factor mRNA stability and translation mainly by altering tristetraprolin expression, stability, and binding to adenine/uridine-rich element

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29 September 2017

Meroterpenoid MAPKAP (MK2) inhibitors isolated from the indonesian marine sponge Acanthodendrilla sp.

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29 September 2017

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29 September 2017

Feedback control of the protein kinase TAK1 by SAPK2a/p38

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29 September 2017

Catalytically active MAP KAP kinase 2 structures in complex with staurosporine and ADP reveal differences with the autoinhibited enzyme

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29 September 2017

Structure of mitogen-activated protein kinase-activated protein (MAPKAP) kinase 2 suggests a bifunctional switch that couples kinase activation with nuclear export

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29 September 2017

FRET-based detection of different conformations of MK2.

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29 September 2017

The Protein Data Bank

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29 September 2017

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29 September 2017

Characterization of an autoinhibitory domain in human mitogen-activated protein kinase-activated protein kinase 2.

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29 September 2017

The Role of Mitogen-Activated Protein Kinase-Activated Protein Kinases (MAPKAPKs) in Inflammation

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27 June 2018

The effect of small-molecule inhibition of MAPKAPK2 on cell ageing phenotypes of fibroblasts from human Werner syndrome

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27 June 2018

A computational study on thiourea analogs as potent MK-2 inhibitors

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27 June 2018

Binding affinity prediction for ligands and receptors forming tautomers and ionization species: inhibition of mitogen-activated protein kinase-activated protein kinase 2 (MK2).

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27 June 2018

Inhibition of HSP27 phosphorylation by a cell-permeant MAPKAP Kinase 2 inhibitor

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27 June 2018

Discovery of ((4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methylpyrrolo[1,2-f][1,2,4]triazine-6-carbonyl)(propyl)carbamoyloxy)methyl-2-(4-(phosphonooxy)phenyl)acetate (BMS-751324), a Clinical Prodrug of p38α MAP Kinase Inhibitor.

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5 September 2018

Discovery and characterization of MAPK-activated protein kinase-2 prevention of activation inhibitors.

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5 September 2018

Discovery of a novel series of potent MK2 non-ATP competitive inhibitors using 1,2-substituted azoles as cis-amide isosteres

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5 September 2018

Conformation constraint of anilides enabling the discovery of tricyclic lactams as potent MK2 non-ATP competitive inhibitors

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5 September 2018

SnapShot: p38 MAPK substrates.

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5 September 2018

Acylthiourea, acylurea, and acylguanidine derivatives with potent hedgehog inhibiting activity.

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5 September 2018

Facile synthesis of tetracyclic azepine and oxazocine derivatives and their potential as MAPKAP-K2 (MK2) inhibitors.

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5 September 2018

Discovery of selective and orally available spiro-3-piperidyl ATP-competitive MK2 inhibitors.

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5 September 2018

In vivo and in vitro SAR of tetracyclic MAPKAP-K2 (MK2) inhibitors. Part I.

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5 September 2018

2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization

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5 September 2018

Assessment of the putative binding conformation of a pyrazolopyridine class of inhibitors of MAPKAPK2 using computational studies

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5 September 2018

Inhibition of p38: has the fat lady sung?

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5 September 2018

Structural analysis of carboline derivatives as inhibitors of MAPKAP K2 using 3D QSAR and docking studies.

1 reference

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5 September 2018

Pyrrolo-pyrimidones: a novel class of MK2 inhibitors with potent cellular activity.

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5 September 2018

Synthesis and SAR studies of indole-based MK2 inhibitors

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4850115

5 September 2018

Aminocyanopyridine inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2).

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4850115

5 September 2018

Catalysis and function of the p38 alpha.MK2a signaling complex

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=4850115

5 September 2018

A three-step protocol for lead optimization: quick identification of key conformational features and functional groups in the SAR studies of non-ATP competitive MK2 (MAPKAPK2) inhibitors

1 reference

https://pubmed.ncbi.nlm.nih.gov/26502061

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Aqueous versus non-aqueous salt delivery strategies to enhance oral bioavailability of a mitogen-activated protein kinase-activated protein kinase (MK-2) inhibitor in rats

1 reference

https://pubmed.ncbi.nlm.nih.gov/26502061

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Pyrazinoindolone inhibitors of MAPKAP-K2

1 reference

https://pubmed.ncbi.nlm.nih.gov/26502061

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Novel tetrahydro-beta-carboline-1-carboxylic acids as inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2)

1 reference

https://pubmed.ncbi.nlm.nih.gov/26502061

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Identifiers

10.1021/ACS.JMEDCHEM.5B01457

1 reference

Europe PubMed Central

PMC publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:26502061%20AND%20SRC:MED&resulttype=core&format=json

28 February 2020

PMC publication ID

1 reference

Europe PubMed Central

PMC publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:26502061%20AND%20SRC:MED&resulttype=core&format=json

28 February 2020

PubMed publication ID

1 reference

Europe PubMed Central

PMC publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:26502061%20AND%20SRC:MED&resulttype=core&format=json

28 February 2020

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