(Q39226865)

10 September 2017

Novel approaches for targeting kinases: allosteric inhibition, allosteric activation and pseudokinases (English)

1 reference

10 September 2017

Stefan Knapp

3

0 references

author name string

Sandra W Cowan-Jacob

series ordinal

1

1 reference

PubMed ID

24649957

10 September 2017

Wolfgang Jahnke

series ordinal

2

1 reference

10 September 2017

1 April 2014

1 reference

Future Medicinal Chemistry

10 September 2017

1 reference

10 September 2017

6

1 reference

10 September 2017

5

1 reference

10 September 2017

541-561

1 reference

The secret life of kinases: functions beyond catalysis

10 September 2017

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

The protein kinase complement of the human genome

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl.

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Imatinib: a selective tyrosine kinase inhibitor

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Comprehensive analysis of kinase inhibitor selectivity

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Discovery and development of sorafenib: a multikinase inhibitor for treating cancer.

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Chaperones as thermodynamic sensors of drug-target interactions reveal kinase inhibitor specificities in living cells

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Structure-based design, synthesis, and biological evaluation of potent and selective macrocyclic checkpoint kinase 1 inhibitors.

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Developing irreversible inhibitors of the protein kinase cysteinome

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

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

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Targeting diverse signaling interaction sites allows the rapid generation of bivalent kinase inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Structure-based discovery of cellular-active allosteric inhibitors of FAK

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Allosteric IGF-1R Inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Fluorophore Labeled Kinase Detects Ligands That Bind within the MAPK Insert of p38α Kinase

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

A guide to picking the most selective kinase inhibitor tool compounds for pharmacological validation of drug targets

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Strategies for the selective regulation of kinases with allosteric modulators: exploiting exclusive structural features.

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Allosteric inhibitors of Bcr-abl-dependent cell proliferation

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Targeting Bcr–Abl by combining allosteric with ATP-binding-site inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Discovery and characterization of novel allosteric FAK inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Characterization of the CHK1 allosteric inhibitor binding site

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

An allosteric kinase inhibitor binds the p21-activated kinase autoregulatory domain covalently.

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

An isoform-selective, small-molecule inhibitor targets the autoregulatory mechanism of p21-activated kinase

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

A Back-to-Front Fragment-Based Drug Design Search Strategy Targeting the DFG-Out Pocket of Protein Tyrosine Kinases

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Inhibition of p38 MAP kinase by utilizing a novel allosteric binding site

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Structures of human MAP kinase kinase 1 (MEK1) and MEK2 describe novel noncompetitive kinase inhibition.

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

A new screening assay for allosteric inhibitors of cSrc

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Direct binding assay for the detection of type IV allosteric inhibitors of Abl.

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Discovery of a Potential Allosteric Ligand Binding Site in CDK2

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

A Novel Approach to the Discovery of Small-Molecule Ligands of CDK2

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Binding or bending: distinction of allosteric Abl kinase agonists from antagonists by an NMR-based conformational assay

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Searching for new allosteric sites in enzymes

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Peptide exosite inhibitors of factor VIIa as anticoagulants

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Biosensor-based approach to the identification of protein kinase ligands with dual-site modes of action.

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Discovery and characterization of non-ATP site inhibitors of the mitogen activated protein (MAP) kinases

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Discovery and optimization of a series of 3-(3-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amines: orally bioavailable, selective, and potent ATP-independent Akt inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

A unique structure for epidermal growth factor receptor bound to GW572016 (Lapatinib): relationships among protein conformation, inhibitor off-rate, and receptor activity in tumor cells

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Identification of allosteric PIF-pocket ligands for PDK1 using NMR-based fragment screening and 1H-15N TROSY experiments

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Fragment based drug design: from experimental to computational approaches.

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Strategies for the NMR-based identification and optimization of allosteric protein kinase inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Screening of protein kinases by ATP-STD NMR spectroscopy

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Development of paramagnetic probes for molecular recognition studies in protein kinases

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Identification of a new JNK inhibitor targeting the JNK-JIP interaction site

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Allosteric activation of the protein kinase PDK1 with low molecular weight compounds

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Design and synthesis of benzoazepin-2-one analogs as allosteric binders targeting the PIF pocket of PDK1.

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

4-benzimidazolyl-3-phenylbutanoic acids as novel PIF-pocket-targeting allosteric inhibitors of protein kinase PKCζ.

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Allosteric regulation of protein kinase PKCζ by the N-terminal C1 domain and small compounds to the PIF-pocket

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Structural basis for the autoinhibition of c-Abl tyrosine kinase

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

The crystal structure of a c-Src complex in an active conformation suggests possible steps in c-Src activation

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

How does a drug molecule find its target binding site?

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Exploring the binding sites of glycogen synthase kinase 3. Identification and characterization of allosteric modulation cavities.

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

ASD v2.0: updated content and novel features focusing on allosteric regulation

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Allosite: a method for predicting allosteric sites

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Exploiting protein flexibility to predict the location of allosteric sites

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Allosteric inhibitors of Akt1 and Akt2: discovery of [1,2,4]triazolo[3,4-f][1,6]naphthyridines with potent and balanced activity

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Development of potent, allosteric dual Akt1 and Akt2 inhibitors with improved physical properties and cell activity

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Development of thioquinazolinones, allosteric Chk1 kinase inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Characterization of ATP-independent ERK inhibitors identified through in silico analysis of the active ERK2 structure

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

First-in-man clinical trial of the oral pan-AKT inhibitor MK-2206 in patients with advanced solid tumors

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

p38α MAP Kinase C-Terminal Domain Binding Pocket Characterized by Crystallographic and Computational Analyses

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

RAS/RAF/MEK inhibitors in oncology

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Drug discovery and the human kinome: recent trends

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Akt inhibitors in clinical development for the treatment of cancer

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Discovery and characterization of a cell-permeable, small-molecule c-Abl kinase activator that binds to the myristoyl binding site

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

c-Abl tyrosine kinase regulates caspase-9 autocleavage in the apoptotic response to DNA damage

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Activated Abl kinase inhibits oncogenic transforming growth factor-beta signaling and tumorigenesis in mammary tumors

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Structure and allosteric effects of low-molecular-weight activators on the protein kinase PDK1

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Substrate-selective inhibition of protein kinase PDK1 by small compounds that bind to the PIF-pocket allosteric docking site

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Discovery of PDK1 kinase inhibitors with a novel mechanism of action by ultrahigh throughput screening

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Structural and biochemical evidence for an autoinhibitory role for tyrosine 984 in the juxtamembrane region of the insulin receptor

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Discovery of a potent, highly selective, and orally efficacious small-molecule activator of the insulin receptor

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Targeting energy metabolic and oncogenic signaling pathways in triple-negative breast cancer by a novel adenosine monophosphate-activated protein kinase (AMPK) activator

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Exploiting the anti-inflammatory effects of AMP-activated protein kinase activation.

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Direct AMP-activated protein kinase activators: a review of evidence from the patent literature

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Bronchodilator and antiulcer phenoxypyrimidinones

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

MLR-1023 is a potent and selective allosteric activator of Lyn kinase in vitro that improves glucose tolerance in vivo.

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Cross talk of pp125(FAK) and pp59(Lyn) non-receptor tyrosine kinases to insulin-mimetic signaling in adipocytes

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Small molecule BDNF mimetics activate TrkB signaling and prevent neuronal degeneration in rodents

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

The (un)targeted cancer kinome

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Specific CLK Inhibitors from a Novel Chemotype for Regulation of Alternative Splicing

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Leucettines, a class of potent inhibitors of cdc2-like kinases and dual specificity, tyrosine phosphorylation regulated kinases derived from the marine sponge leucettamine B: modulation of alternative pre-RNA splicing.

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Topical antiangiogenic SRPK1 inhibitors reduce choroidal neovascularization in rodent models of exudative AMD

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

A novel protein kinase-like domain in a selenoprotein, widespread in the tree of life.

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

FAM20B is a kinase that phosphorylates xylose in the glycosaminoglycan-protein linkage region

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Four-jointed is a Golgi kinase that phosphorylates a subset of cadherin domains

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

The Raine syndrome protein FAM20C is a Golgi kinase that phosphorylates bio-mineralization proteins

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Secreted kinase phosphorylates extracellular proteins that regulate biomineralization

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Crystal structures of the JAK2 pseudokinase domain and the pathogenic mutant V617F

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

CASK Functions as a Mg2+-independent neurexin kinase

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Structure of the Pseudokinase VRK3 Reveals a Degraded Catalytic Site, a Highly Conserved Kinase Fold, and a Putative Regulatory Binding Site

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Large-scale structural analysis of the classical human protein tyrosine phosphatome

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Emerging roles of pseudokinases

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

WNK1, a novel mammalian serine/threonine protein kinase lacking the catalytic lysine in subdomain II

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Crystal structure of the kinase domain of WNK1, a kinase that causes a hereditary form of hypertension

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Kinetic mechanism and inhibitor characterization of WNK1 kinase

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Cloning and characterization of a p53-related protein kinase expressed in interleukin-2-activated cytotoxic T-cells, epithelial tumor cell lines, and the testes

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Divalent metal ions influence catalysis and active-site accessibility in the cAMP-dependent protein kinase

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Physiological concentrations of divalent magnesium ion activate the serine/threonine specific protein kinase ERK2.

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

CASK aberrations in male patients with Ohtahara syndrome and cerebellar hypoplasia

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Phenotypic spectrum associated with CASK loss-of-function mutations

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

A systematic, large-scale resequencing screen of X-chromosome coding exons in mental retardation

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

A missense mutation in CASK causes FG syndrome in an Italian family

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Structural analysis of the catalytically inactive kinase domain of the human EGF receptor 3

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

ErbB3/HER3 intracellular domain is competent to bind ATP and catalyze autophosphorylation

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Oncogenic ERBB3 mutations in human cancers

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Pseudokinases-remnants of evolution or key allosteric regulators?

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

ILK: a pseudokinase in the center stage of cell-matrix adhesion and signaling

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

An integrin-ILK-microtubule network orients cell polarity and lumen formation in glandular epithelium

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Integrin-linked kinase--essential roles in physiology and cancer biology.

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Small interfering RNA targeting ILK inhibits metastasis in human tongue cancer cells through repression of epithelial-to-mesenchymal transition

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Overexpression of integrin-linked kinase (ILK) is associated with tumor progression and an unfavorable prognosis in patients with colorectal cancer

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Targeting ILK and β4 integrin abrogates the invasive potential of ovarian cancer

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

The Pseudoactive Site of ILK Is Essential for Its Binding to α-Parvin and Localization to Focal Adhesions

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Selective bisubstrate inhibitors with sub-nanomolar affinity for protein kinase Pim-1.

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Bisubstrate inhibitors of protein kinases: from principle to practical applications

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

The level of C/EBP protein is critical for cell migration during Drosophila oogenesis and is tightly controlled by regulated degradation

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

COP1 targets C/EBPα for degradation and induces acute myeloid leukemia via Trib1.

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Tribbles in acute leukemia

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Critical role of Trib1 in differentiation of tissue-resident M2-like macrophages

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

FOG-1 and GATA-1 act sequentially to specify definitive megakaryocytic and erythroid progenitors

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Differential ability of Tribbles family members to promote degradation of C/EBPalpha and induce acute myelogenous leukemia

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Trib1 links the MEK1/ERK pathway in myeloid leukemogenesis

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Identification of TRIB1 R107L gain-of-function mutation in human acute megakaryocytic leukemia.

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

SKIP3, a novel Drosophila tribbles ortholog, is overexpressed in human tumors and is regulated by hypoxia

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Transformation by Tribbles homolog 2 (Trib2) requires both the Trib2 kinase domain and COP1 binding

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Structure of a pseudokinase-domain switch that controls oncogenic activation of Jak kinases

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

New insights into the structure and function of the pseudokinase domain in JAK2.

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

JAK2 V617F constitutive activation requires JH2 residue F595: a pseudokinase domain target for specific inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

21 January 2018

Too many roads not taken

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Identification of novel p38alpha MAP kinase inhibitors using fragment-based lead generation.

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD)

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Mutagenesis of p38alpha MAP kinase establishes key roles of Phe169 in function and structural dynamics and reveals a novel DFG-OUT state

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Displacement assay for the detection of stabilizers of inactive kinase conformations

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Switch control pocket inhibitors of p38-MAP kinase. Durable type II inhibitors that do not require binding into the canonical ATP hinge region

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Natural-product-derived fragments for fragment-based ligand discovery

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

The design, synthesis and potential utility of fluorescence probes that target DFG-out conformation of p38alpha for high throughput screening binding assay

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Lipid molecules induce p38α activation via a novel molecular switch

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

2-Alkylamino- and alkoxy-substituted 2-amino-1,3,4-oxadiazoles-O-Alkyl benzohydroxamate esters replacements retain the desired inhibition and selectivity against MEK (MAP ERK kinase)

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Crystal structures of MEK1 binary and ternary complexes with nucleotides and inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

RDEA119/BAY 869766: a potent, selective, allosteric inhibitor of MEK1/2 for the treatment of cancer

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Structure-based design and synthesis of pyrrole derivatives as MEK inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Design and synthesis of novel allosteric MEK inhibitor CH4987655 as an orally available anticancer agent

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Discovery of TAK-733, a potent and selective MEK allosteric site inhibitor for the treatment of cancer

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Novel Carboxamide-Based Allosteric MEK Inhibitors: Discovery and Optimization Efforts toward XL518 (GDC-0973)

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Engineering human MEK-1 for structural studies: A case study of combinatorial domain hunting

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Discovery of novel allosteric mitogen-activated protein kinase kinase (MEK) 1,2 inhibitors possessing bidentate Ser212 interactions

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Optimization of allosteric MEK inhibitors. Part 1: Venturing into underexplored SAR territories

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Turning a protein kinase on or off from a single allosteric site via disulfide trapping

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Roco kinase structures give insights into the mechanism of Parkinson disease-related leucine-rich-repeat kinase 2 mutations

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

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

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Conformational Control Inhibition of the BCR-ABL1 Tyrosine Kinase, Including the Gatekeeper T315I Mutant, by the Switch-Control Inhibitor DCC-2036

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Crystal Structures of ABL-Related Gene (ABL2) in Complex with Imatinib, Tozasertib (VX-680), and a Type I Inhibitor of the Triazole Carbothioamide Class

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Crystal Structure of Human AKT1 with an Allosteric Inhibitor Reveals a New Mode of Kinase Inhibition

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Structure-kinetic relationship study of CDK8/CycC specific compounds

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Identification of novel series of pyrazole and indole-urea based DFG-out PYK2 inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Structural basis of RIP1 inhibition by necrostatins

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

Insights into protein kinase regulation and inhibition by large scale structural comparison

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

2-(3-Oxo-1,3-diphenylpropyl)malonic Acids as Potent Allosteric Ligands of the PIF Pocket of Phosphoinositide-Dependent Kinase-1: Development and Prodrug Concept

21 January 2018

1 reference

https://api.crossref.org/works/10.4155%2FFMC.13.216

21 January 2018

Identifiers

DOI

10.4155/FMC.13.216

1 reference

10 September 2017

1 reference

PubMed ID

24649957