(Q37859008)

24 August 2017

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title

Targeting the DFG-in kinase conformation: a new trend emerging from a patent analysis (English)

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24 August 2017

Mauro Angiolini

1

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24 August 2017

publication date

1 March 2011

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Future Medicinal Chemistry

24 August 2017

published in

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24 August 2017

volume

3

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24 August 2017

issue

3

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24 August 2017

page(s)

309-337

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The (un)targeted cancer kinome

24 August 2017

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21 January 2018

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21 January 2018

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Small-molecule inhibitors binding to protein kinase. Part II: the novel pharmacophore approach of type II and type III inhibition

21 January 2018

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Targeting the unactivated conformations of protein kinases for small molecule drug discovery

21 January 2018

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A quantitative analysis of kinase inhibitor selectivity

21 January 2018

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Kinase mutations in human disease: interpreting genotype-phenotype relationships

21 January 2018

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Biochemical mechanisms of resistance to small-molecule protein kinase inhibitors

21 January 2018

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Kinase domain mutations in cancer: implications for small molecule drug design strategies.

21 January 2018

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Through the "gatekeeper door": exploiting the active kinase conformation

21 January 2018

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Mutations of the BRAF gene in human cancer

21 January 2018

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Mechanism of activation of the RAF-ERK signaling pathway by oncogenic mutations of B-RAF

21 January 2018

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Sorafenib for treatment of renal cell carcinoma: Final efficacy and safety results of the phase III treatment approaches in renal cancer global evaluation trial.

21 January 2018

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Phase II, multicenter, uncontrolled trial of single-agent sorafenib in patients with relapsed or refractory, advanced non-small-cell lung cancer

21 January 2018

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Phase II trial of sorafenib in advanced thyroid cancer

21 January 2018

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Rearrangements of the RAF kinase pathway in prostate cancer, gastric cancer and melanoma

21 January 2018

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RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth

21 January 2018

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Discovery of highly potent and selective type I B-Raf kinase inhibitors

21 January 2018

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Potent and selective pyrazole-based inhibitors of B-Raf kinase

21 January 2018

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Antitumor efficacy of the novel RAF inhibitor GDC-0879 is predicted by BRAFV600E mutational status and sustained extracellular signal-regulated kinase/mitogen-activated protein kinase pathway suppression.

21 January 2018

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The identification of potent and selective imidazole-based inhibitors of B-Raf kinase

21 January 2018

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Indazolylpyrazolopyrimidine as highly potent B-Raf inhibitors with in vivo activity

21 January 2018

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Novel pyrazolopyrimidines as highly potent B-Raf inhibitors

21 January 2018

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Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity

21 January 2018

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RG7204 (PLX4032), a selective BRAFV600E inhibitor, displays potent antitumor activity in preclinical melanoma models

21 January 2018

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The RAF inhibitor PLX4032 inhibits ERK signaling and tumor cell proliferation in a V600E BRAF-selective manner

21 January 2018

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Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma

21 January 2018

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MKK3- and MKK6-regulated gene expression is mediated by the p38 mitogen-activated protein kinase signal transduction pathway

21 January 2018

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The biology of p38 kinase: a central role in inflammation

21 January 2018

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Small molecule p38 MAP kinase inhibitors for the treatment of inflammatory diseases: novel structures and developments during 2006-2008.

21 January 2018

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Pyrazolo-pyrimidines: a novel heterocyclic scaffold for potent and selective p38 alpha inhibitors

21 January 2018

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Biphenyl amide p38 kinase inhibitors 1: Discovery and binding mode

21 January 2018

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Biphenyl amide p38 kinase inhibitors 2: Optimisation and SAR.

21 January 2018

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https://api.crossref.org/works/10.4155%2FFMC.10.294

Biphenyl amide p38 kinase inhibitors 3: Improvement of cellular and in vivo activity

21 January 2018

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https://api.crossref.org/works/10.4155%2FFMC.10.294

Design, synthesis, and anti-inflammatory properties of orally active 4-(phenylamino)-pyrrolo[2,1-f][1,2,4]triazine p38alpha mitogen-activated protein kinase inhibitors

21 January 2018

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https://api.crossref.org/works/10.4155%2FFMC.10.294

p38alpha mitogen-activated protein kinase inhibitors: optimization of a series of biphenylamides to give a molecule suitable for clinical progression

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.10.294

Discovery of highly selective and potent p38 inhibitors based on a phthalazine scaffold

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.10.294

Discovery and evaluation of 7-alkyl-1,5-bis-aryl-pyrazolopyridinones as highly potent, selective, and orally efficacious inhibitors of p38alpha mitogen-activated protein kinase

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.10.294

Part 1: Structure-Activity Relationship (SAR) investigations of fused pyrazoles as potent, selective and orally available inhibitors of p38alpha mitogen-activated protein kinase

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.10.294

Part 2: Structure-activity relationship (SAR) investigations of fused pyrazoles as potent, selective and orally available inhibitors of p38alpha mitogen-activated protein kinase

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.10.294

Discovery of pyridazinopyridinones as potent and selective p38 mitogen-activated protein kinase inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.10.294

Prospect of JAK2 inhibitor therapy in myeloproliferative neoplasms

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.10.294

A novel chemotype of kinase inhibitors: Discovery of 3,4-ring fused 7-azaindoles and deazapurines as potent JAK2 inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.10.294

Janus kinase 2 inhibitors. Synthesis and characterization of a novel polycyclic azaindole

21 January 2018

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https://api.crossref.org/works/10.4155%2FFMC.10.294

Vascular patterning by Eph receptor tyrosine kinases and ephrins

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.10.294

Eph/ephrin signaling: networks.

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.10.294

Eph-ephrin bidirectional signaling in physiology and disease

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.10.294

Inhibitors of the tyrosine kinase EphB4. Part 1: Structure-based design and optimization of a series of 2,4-bis-anilinopyrimidines

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.10.294

Inhibitors of the tyrosine kinase EphB4. Part 2: structure-based discovery and optimisation of 3,5-bis substituted anilinopyrimidines

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.10.294

The discovery of substituted 4-(3-hydroxyanilino)-quinolines as potent RET kinase inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.10.294

Novel synthesis and structural characterization of a high-affinity paramagnetic kinase probe for the identification of non-ATP site binders by nuclear magnetic resonance

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.10.294

Inhibitors of the tyrosine kinase EphB4. Part 3: Identification of non-benzodioxole-based kinase inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.10.294

Structure-based optimization of potent and selective inhibitors of the tyrosine kinase erythropoietin producing human hepatocellular carcinoma receptor B4 (EphB4).

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.10.294

Activation of tyrosine kinases by mutation of the gatekeeper threonine

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.10.294

Equally Potent Inhibition of c-Src and Abl by Compounds that Recognize Inactive Kinase Conformations

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.10.294

Hybrid compound design to overcome the gatekeeper T338M mutation in cSrc

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.10.294

Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase includ

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.10.294

Broad spectrum alkynyl inhibitors of T315I Bcr-Abl

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.10.294

Novel mutant-selective EGFR kinase inhibitors against EGFR T790M

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.10.294

21 January 2018

Identifiers

DOI

10.4155/FMC.10.294

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24 August 2017

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