Protein kinase inhibitors: contributions from structure to clinical compounds (Q37417742)

20 August 2017

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title

Protein kinase inhibitors: contributions from structure to clinical compounds (English)

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20 August 2017

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1

Louise N Johnson

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20 August 2017

publication date

1 February 2009

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Quarterly Reviews of Biophysics

20 August 2017

published in

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20 August 2017

volume

42

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20 August 2017

issue

1

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20 August 2017

page(s)

1-40

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Nilotinib (formerly AMN107), a highly selective BCR-ABL tyrosine kinase inhibitor, is active in patients with imatinib-resistant or -intolerant accelerated-phase chronic myelogenous leukemia

20 August 2017

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Surface comparison of active and inactive protein kinases identifies a conserved activation mechanism

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Structure of a peptide inhibitor bound to the catalytic subunit of cyclic adenosine monophosphate-dependent protein kinase

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Crystal Structure of the Catalytic Subunit of Cyclic Adenosine Monophosphate-Dependent Protein Kinase

21 January 2018

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A quantitative analysis of kinase inhibitor selectivity

21 January 2018

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Active and inactive protein kinases: structural basis for regulation

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Structural basis for control by phosphorylation

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The structure of dimeric ROCK I reveals the mechanism for ligand selectivity

21 January 2018

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The conformational plasticity of protein kinases

21 January 2018

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Temsirolimus, interferon alfa, or both for advanced renal-cell carcinoma

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Target spectrum of the BCR-ABL inhibitors imatinib, nilotinib and dasatinib

21 January 2018

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Paradoxical activation of Raf by a novel Raf inhibitor

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Patterns of somatic mutation in human cancer genomes

21 January 2018

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Inhibition of the EGF receptor by binding of MIG6 to an activating kinase domain interface

21 January 2018

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An allosteric mechanism for activation of the kinase domain of epidermal growth factor receptor

21 January 2018

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The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP

21 January 2018

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Structures of Lung Cancer-Derived EGFR Mutants and Inhibitor Complexes: Mechanism of Activation and Insights into Differential Inhibitor Sensitivity

21 January 2018

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Efficacy and safety of lapatinib as first-line therapy for ErbB2-amplified locally advanced or metastatic breast cancer

21 January 2018

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PI3K pathway alterations in cancer: variations on a theme

21 January 2018

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Post-transcriptional regulation of vascular endothelial growth factor mRNA by the product of the VHL tumor suppressor gene

21 January 2018

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Specific protection against breast cancers by cyclin D1 ablation

21 January 2018

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A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development

21 January 2018

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The ground state of embryonic stem cell self-renewal

21 January 2018

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Lapatinib plus capecitabine for HER2-positive advanced breast cancer

21 January 2018

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Structure-function studies of two synthetic anti-vascular endothelial growth factor Fabs and comparison with the Avastin Fab.

21 January 2018

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Temsirolimus, an inhibitor of mammalian target of rapamycin

21 January 2018

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Regulation of mTOR by phosphatidic acid?

21 January 2018

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Downregulation of death-associated protein kinase 1 (DAPK1) in chronic lymphocytic leukemia

21 January 2018

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Phase I dose-finding study of weekly docetaxel followed by flavopiridol for patients with advanced solid tumors.

21 January 2018

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Design, synthesis, and evaluation of orally active benzimidazoles and benzoxazoles as vascular endothelial growth factor-2 receptor tyrosine kinase inhibitors

21 January 2018

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Insights for the development of specific kinase inhibitors by targeted structural genomics

21 January 2018

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Kinase inhibitors and the case for CH...O hydrogen bonds in protein-ligand binding

21 January 2018

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

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

EGF receptor gene mutations are common in lung cancers from "never smokers" and are associated with sensitivity of tumors to gefitinib and erlotinib

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

EGFR mutations in lung cancer: correlation with clinical response to gefitinib therapy

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

Identification of N-(4-piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide (AT7519), a novel cyclin dependent kinase inhibitor using fragment-based X-ray crystallography and structure based drug design

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

TOR signaling in growth and metabolism

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

EGFR and cancer prognosis

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

Structural basis for the autoinhibition of c-Abl tyrosine kinase

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

Sunitinib efficacy against advanced renal cell carcinoma

21 January 2018

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Atomic structure of FKBP-FK506, an immunophilin-immunosuppressant complex

21 January 2018

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Solution conformations and dynamics of ABL kinase-inhibitor complexes determined by NMR substantiate the different binding modes of imatinib/nilotinib and dasatinib

21 January 2018

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Targeting checkpoint kinase 1 in cancer therapeutics

21 January 2018

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Discovery of a potent and selective inhibitor of cyclin-dependent kinase 4/6.

21 January 2018

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The structure of Dasatinib (BMS-354825) bound to activated ABL kinase domain elucidates its inhibitory activity against imatinib-resistant ABL mutants

21 January 2018

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Gefitinib plus best supportive care in previously treated patients with refractory advanced non-small-cell lung cancer: results from a randomised, placebo-controlled, multicentre study (Iressa Survival Evaluation in Lung Cancer)

21 January 2018

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Renal cell carcinoma: new developments in molecular biology and potential for targeted therapies

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

Proliferation of cancer cells despite CDK2 inhibition.

21 January 2018

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Protein kinases--the major drug targets of the twenty-first century?

21 January 2018

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Structure of the epidermal growth factor receptor kinase domain alone and in complex with a 4-anilinoquinazoline inhibitor

21 January 2018

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Structure of the FKBP12-rapamycin complex interacting with the binding domain of human FRAP

21 January 2018

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A new pharmacologic action of CCI-779 involves FKBP12-independent inhibition of mTOR kinase activity and profound repression of global protein synthesis

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

Structure of the extracellular region of HER2 alone and in complex with the Herceptin Fab

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

A novel pathway regulating the mammalian target of rapamycin (mTOR) signaling

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

Activity of SU11248, a multitargeted inhibitor of vascular endothelial growth factor receptor and platelet-derived growth factor receptor, in patients with metastatic renal cell carcinoma

21 January 2018

1 reference

https://api.crossref.org/works/10.1017%2FS0033583508004745

Flavopiridol inhibits P-TEFb and blocks HIV-1 replication

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

Structure of a c-kit product complex reveals the basis for kinase transactivation

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

Mutations of the epidermal growth factor receptor in non-small cell lung cancer -- search and destroy

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

Structural basis for the autoinhibition and STI-571 inhibition of c-Kit tyrosine kinase

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

Flavopiridol administered using a pharmacologically derived schedule is associated with marked clinical efficacy in refractory, genetically high-risk chronic lymphocytic leukemia

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

Structures of the tyrosine kinase domain of fibroblast growth factor receptor in complex with inhibitors

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

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

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https://api.crossref.org/works/10.1017%2FS0033583508004745

The development of HKI-272 and related compounds for the treatment of cancer

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

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

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

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

21 January 2018

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Phosphatidic acid-mediated mitogenic activation of mTOR signaling

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

Kinomics: characterizing the therapeutically validated kinase space.

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

A small molecule-kinase interaction map for clinical kinase inhibitors

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

Structural characterization of the interaction of mTOR with phosphatidic acid and a novel class of inhibitor: compelling evidence for a central role of the FRB domain in small molecule-mediated regulation of mTOR

21 January 2018

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Protein kinases as targets for anticancer agents: from inhibitors to useful drugs

21 January 2018

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

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

Cyclin-dependent kinase 2 is essential for meiosis but not for mitotic cell division in mice.

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

Effects of a selective inhibitor of the Abl tyrosine kinase on the growth of Bcr-Abl positive cells

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

H-series protein kinase inhibitors and potential clinical applications

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

Structural basis for specificity and potency of a flavonoid inhibitor of human CDK2, a cell cycle kinase.

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

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

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

Structure-based design of cyclin-dependent kinase inhibitors

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

Regulation of protein kinases; controlling activity through activation segment conformation

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

Mutations of the BRAF gene in human cancer

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

Protein kinase inhibitors: insights into drug design from structure.

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

Specificity and mechanism of action of some commonly used protein kinase inhibitors

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

Protein kinase A in complex with Rho-kinase inhibitors Y-27632, Fasudil, and H-1152P: structural basis of selectivity

21 January 2018

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EGFR-targeting drugs in combination with cytotoxic agents: from bench to bedside, a contrasted reality

21 January 2018

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Two distinct signal transmission pathways in T lymphocytes are inhibited by complexes formed between an immunophilin and either FK506 or rapamycin

21 January 2018

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A novel therapeutic combination using PD 0332991 and bortezomib: study in the 5T33MM myeloma model.

21 January 2018

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Peptidomimetic design of CDK inhibitors targeting the recruitment site of the cyclin subunit

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

Doing more than just the structure-structural genomics in kinase drug discovery.

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

Targeting phosphoinositide 3-kinase: moving towards therapy

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

Somatic mutations of epidermal growth factor receptor signaling pathway in lung cancers

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

Cyclin-dependent kinase pathways as targets for cancer treatment

21 January 2018

1 reference

https://api.crossref.org/works/10.1017%2FS0033583508004745

A phase I clinical trial of the sequential combination of irinotecan followed by flavopiridol

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

First-line gefitinib in patients with advanced non-small-cell lung cancer harboring somatic EGFR mutations

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

EGFR tyrosine kinase inhibitors in lung cancer: an evolving story

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

Mechanisms of drug inhibition of signalling molecules

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

Advances in the development of cancer therapeutics directed against the RAS-mitogen-activated protein kinase pathway

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

CR8, a potent and selective, roscovitine-derived inhibitor of cyclin-dependent kinases

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

Cell signaling by receptor tyrosine kinases

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

Cdk2 knockout mice are viable

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

Structural mechanism for STI-571 inhibition of abelson tyrosine kinase

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

The structure of P-TEFb (CDK9/cyclin T1), its complex with flavopiridol and regulation by phosphorylation

21 January 2018

1 reference

https://api.crossref.org/works/10.1017%2FS0033583508004745

Management of renal cancer in the tyrosine kinase inhibitor era: a view from 3 years on.

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

Identification and characterization of pleckstrin-homology-domain-dependent and isoenzyme-specific Akt inhibitors

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

Studies leading to the identification of ZD1839 (IRESSA): an orally active, selective epidermal growth factor receptor tyrosine kinase inhibitor targeted to the treatment of cancer

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

Quantitative chemical proteomics reveals mechanisms of action of clinical ABL kinase inhibitors

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

The protein kinase complement of the human genome

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

Characterization of the FKBP.rapamycin.FRB ternary complex

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

CDK inhibitors in cancer therapy: what is next?

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

The selectivity of protein kinase inhibitors: a further update

21 January 2018

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https://api.crossref.org/works/10.1017%2FS0033583508004745

Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib

21 January 2018

1 reference

https://api.crossref.org/works/10.1017%2FS0033583508004745

Mechanisms of autoinhibition and STI-571/imatinib resistance revealed by mutagenesis of BCR-ABL.

21 January 2018

1 reference

https://api.crossref.org/works/10.1017%2FS0033583508004745

Toward understanding the structural basis of cyclin-dependent kinase 6 specific inhibition

21 January 2018

1 reference

https://api.crossref.org/works/10.1017%2FS0033583508004745

Rational design of inhibitors that bind to inactive kinase conformations

21 January 2018

1 reference

https://api.crossref.org/works/10.1017%2FS0033583508004745

Drug-like properties and the causes of poor solubility and poor permeability

21 January 2018

1 reference

https://api.crossref.org/works/10.1017%2FS0033583508004745

Molecular recognition of protein kinase binding pockets for design of potent and selective kinase inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.1017%2FS0033583508004745

Refined structure of the FKBP12-rapamycin-FRB ternary complex at 2.2 A resolution

21 January 2018

1 reference

https://api.crossref.org/works/10.1017%2FS0033583508004745

Structural basis for inhibition of the epidermal growth factor receptor by cetuximab

21 January 2018

1 reference

https://api.crossref.org/works/10.1017%2FS0033583508004745

Drugging the Plasmodium kinome: the benefits of academia-industry synergy

21 January 2018

1 reference

https://api.crossref.org/works/10.1017%2FS0033583508004745

Fasudil inhibits vascular endothelial growth factor-induced angiogenesis in vitro and in vivo

21 January 2018

1 reference

https://api.crossref.org/works/10.1017%2FS0033583508004745

7 January 2021

Inflammation of actinic keratoses subsequent to therapy with sorafenib, a multitargeted tyrosine-kinase inhibitor

1 reference

https://api.crossref.org/works/10.1017%2FS0033583508004745

7 January 2021

Insights into cyclin groove recognition: complex crystal structures and inhibitor design through ligand exchange

1 reference

https://api.crossref.org/works/10.1017%2FS0033583508004745

7 January 2021

MK-0457, a novel kinase inhibitor, is active in patients with chronic myeloid leukemia or acute lymphocytic leukemia with the T315I BCR-ABL mutation

1 reference

https://api.crossref.org/works/10.1017%2FS0033583508004745

7 January 2021

Lessons from Tarceva in pancreatic cancer: where are we now, and how should future trials be designed in pancreatic cancer?

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https://api.crossref.org/works/10.1017%2FS0033583508004745

7 January 2021

https://api.crossref.org/works/10.1017%2FS0033583508004745

1 reference

7 January 2021

10.1017/S0033583508004745

Identifiers

DOI

1 reference

20 August 2017

1 reference