(Q38042726)

27 August 2017

title

System-based drug discovery within the human kinome (English)

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27 August 2017

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Paul Bamborough

1

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27 August 2017

language of work or name

English

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publication date

13 September 2012

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Expert Opinion on Drug Discovery

27 August 2017

published in

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27 August 2017

volume

7

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27 August 2017

issue

11

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27 August 2017

page(s)

1053-1070

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The protein kinase complement of the human genome

27 August 2017

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EGFR-mutated lung cancer: a paradigm of molecular oncology

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Dasatinib in imatinib-resistant Philadelphia chromosome-positive leukemias

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Nilotinib in imatinib-resistant CML and Philadelphia chromosome-positive ALL

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Molecular determinants of the response of glioblastomas to EGFR kinase inhibitors.

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Coactivation of receptor tyrosine kinases affects the response of tumor cells to targeted therapies

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Targeting the cancer kinome through polypharmacology

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PI3K inhibitors for cancer treatment: where do we stand?

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Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases

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Dual inhibitors of PI3K/mTOR or mTOR-selective inhibitors: which way shall we go?

21 January 2018

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Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity

21 January 2018

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Novel phosphoinositide 3-kinase/mTOR dual inhibitor, NVP-BGT226, displays potent growth-inhibitory activity against human head and neck cancer cells in vitro and in vivo

21 January 2018

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GDC-0980 is a novel class I PI3K/mTOR kinase inhibitor with robust activity in cancer models driven by the PI3K pathway

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Targeting kinases for the treatment of inflammatory diseases

21 January 2018

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Assessment of chemical coverage of kinome space and its implications for kinase drug discovery.

21 January 2018

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A comparison of physiochemical property profiles of development and marketed oral drugs

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

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Lipophilicity in drug discovery

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Glivec (STI571, imatinib), a rationally developed, targeted anticancer drug

21 January 2018

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

21 January 2018

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

21 January 2018

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Application of NMR screening in drug discovery

21 January 2018

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Fragment-based lead discovery using X-ray crystallography.

21 January 2018

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Introduction to fragment-based drug discovery

21 January 2018

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Selectivity of kinase inhibitor fragments

21 January 2018

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Selective p38alpha inhibitors clinically evaluated for the treatment of chronic inflammatory disorders

21 January 2018

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Inhibition of p38: has the fat lady sung?

21 January 2018

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Efficacy, pharmacodynamics, and safety of VX-702, a novel p38 MAPK inhibitor, in rheumatoid arthritis: results of two randomized, double-blind, placebo-controlled clinical studies.

21 January 2018

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Evaluation of the efficacy and safety of pamapimod, a p38 MAP kinase inhibitor, in a double-blind, methotrexate-controlled study of patients with active rheumatoid arthritis

21 January 2018

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https://api.crossref.org/works/10.1517%2F17460441.2012.724056

JAK and STAT signaling molecules in immunoregulation and immune-mediated disease

21 January 2018

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https://api.crossref.org/works/10.1517%2F17460441.2012.724056

Discovery and development of spleen tyrosine kinase (SYK) inhibitors

21 January 2018

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https://api.crossref.org/works/10.1517%2F17460441.2012.724056

Progress towards the development of anti-inflammatory inhibitors of IKKbeta

21 January 2018

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https://api.crossref.org/works/10.1517%2F17460441.2012.724056

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

21 January 2018

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https://api.crossref.org/works/10.1517%2F17460441.2012.724056

mTOR inhibitors in cancer therapy.

21 January 2018

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https://api.crossref.org/works/10.1517%2F17460441.2012.724056

Progress in the preclinical discovery and clinical development of class I and dual class I/IV phosphoinositide 3-kinase (PI3K) inhibitors

21 January 2018

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https://api.crossref.org/works/10.1517%2F17460441.2012.724056

Interaction maps for kinase inhibitors

21 January 2018

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https://api.crossref.org/works/10.1517%2F17460441.2012.724056

Transformation of in vitro tools for kinase profiling: keeping an eye over the off-target liabilities

21 January 2018

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The specificities of protein kinase inhibitors: an update

21 January 2018

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The selectivity of protein kinase inhibitors: a further update

21 January 2018

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A small molecule-kinase interaction map for clinical kinase inhibitors

21 January 2018

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https://api.crossref.org/works/10.1517%2F17460441.2012.724056

Comprehensive analysis of kinase inhibitor selectivity

21 January 2018

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https://api.crossref.org/works/10.1517%2F17460441.2012.724056

Trends in kinase selectivity: insights for target class-focused library screening

21 January 2018

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Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity

21 January 2018

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

21 January 2018

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A small molecule discrimination map of the antibiotic resistance kinome

21 January 2018

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Gini coefficient: a new way to express selectivity of kinase inhibitors against a family of kinases

21 January 2018

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A theoretical entropy score as a single value to express inhibitor selectivity

21 January 2018

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21 January 2018

Navigating the kinome

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Kinomics-structural biology and chemogenomics of kinase inhibitors and targets

21 January 2018

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Cardiotoxicity of kinase inhibitors: the prediction and translation of preclinical models to clinical outcomes.

21 January 2018

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https://api.crossref.org/works/10.1517%2F17460441.2012.724056

Identification of a kinase profile that predicts chromosome damage induced by small molecule kinase inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

Modeling bone marrow toxicity using kinase structural motifs and the inhibition profiles of small molecular kinase inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

Kinase inhibition-related adverse events predicted from in vitro kinome and clinical trial data

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

Inroads to predict in vivo toxicology-an introduction to the eTOX Project

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

Believe it or not: how much can we rely on published data on potential drug targets?

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

Kinase inhibitors: not just for kinases anymore

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

Effect of detergent on "promiscuous" inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

ALARM NMR: a rapid and robust experimental method to detect reactive false positives in biochemical screens

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

New substructure filters for removal of pan assay interference compounds (PAINS) from screening libraries and for their exclusion in bioassays

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

Quantitative analyses of aggregation, autofluorescence, and reactivity artifacts in a screen for inhibitors of a thiol protease

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

Lead-oriented synthesis: a new opportunity for synthetic chemistry

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

A crowdsourcing evaluation of the NIH chemical probes

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

In vivo target validation using gene invalidation, RNA interference and protein functional knockout models: it is the time to combine

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

Comparative kinome analysis to identify putative colon tumor biomarkers

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

Kinomics: methods for deciphering the kinome

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

Kinome-wide RNAi studies in human multiple myeloma identify vulnerable kinase targets, including a lymphoid-restricted kinase, GRK6.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

High-throughput RNAi screening identifies a role for TNK1 in growth and survival of pancreatic cancer cells

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

Kinome screening for regulators of the estrogen receptor identifies LMTK3 as a new therapeutic target in breast cancer.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

High throughput short interfering RNA (siRNA) screening of the human kinome identifies novel kinases controlling the canonical nuclear factor-κB (NF-κB) activation pathway

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

RNAi-based screening of the human kinome identifies Akt-cooperating kinases: a new approach to designing efficacious multitargeted kinase inhibitors.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

Chemical-genetic analysis of cyclin dependent kinase 2 function reveals an important role in cellular transformation by multiple oncogenic pathways

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

Genome editing with engineered zinc finger nucleases

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

Knock-in mutation reveals an essential role for focal adhesion kinase activity in blood vessel morphogenesis and cell motility-polarity but not cell proliferation.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

Design of allele-specific inhibitors to probe protein kinase signaling

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

Chemical genetic strategy for targeting protein kinases based on covalent complementarity

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

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/10.1517%2F17460441.2012.724056

The art of the chemical probe

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

Selectively nonselective kinase inhibition: striking the right balance

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

Multi-pathway cellular analysis of compound selectivity

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

Phenotypic fingerprinting of small molecule cell cycle kinase inhibitors for drug discovery

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

How were new medicines discovered?

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

Developing assays for kinase drug discovery - where have the advances come from?

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

Modern phenotypic drug discovery is a viable, neoclassic pharma strategy

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

Chemical proteomics identifies unanticipated targets of clinical kinase inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

Proteomic methods for drug target discovery

21 January 2018

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https://api.crossref.org/works/10.1517%2F17460441.2012.724056

A chemical and phosphoproteomic characterization of dasatinib action in lung cancer

21 January 2018

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https://api.crossref.org/works/10.1517%2F17460441.2012.724056

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

21 January 2018

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https://api.crossref.org/works/10.1517%2F17460441.2012.724056

Activity-based protein profiling: an enabling technology in chemical biology research

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

In situ kinase profiling reveals functionally relevant properties of native kinases

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

A protein kinase involved in the regulation of inflammatory cytokine biosynthesis

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

Kinase chemogenomics: targeting the human kinome for target validation and drug discovery

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

High-throughput kinase profiling as a platform for drug discovery

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

High-throughput kinase profiling: a more efficient approach toward the discovery of new kinase inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

One target-multiple indications: a call for an integrated common mechanisms strategy

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

Complementarity between public and commercial databases: new opportunities in medicinal chemistry informatics

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

Rapamycin passes the torch: a new generation of mTOR inhibitors

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

Nonclinical antiangiogenesis and antitumor activities of axitinib (AG-013736), an oral, potent, and selective inhibitor of vascular endothelial growth factor receptor tyrosine kinases 1, 2, 3.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

An orally available small-molecule inhibitor of c-Met, PF-2341066, exhibits cytoreductive antitumor efficacy through antiproliferative and antiangiogenic mechanisms

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays.

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

Discovery of 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-benzenesulfonamide (Pazopanib), a novel and potent vascular endothelial growth factor receptor inhibitor

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for the treatment of myeloproliferative neoplasms

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

PLX4032, a potent inhibitor of the B-Raf V600E oncogene, selectively inhibits V600E-positive melanomas

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

Pamapimod, a novel p38 mitogen-activated protein kinase inhibitor: preclinical analysis of efficacy and selectivity

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

Discovery of PH-797804, a highly selective and potent inhibitor of p38 MAP kinase

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

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/10.1517%2F17460441.2012.724056

A randomized, placebo-controlled study of the effects of the p38 MAPK inhibitor SB-681323 on blood biomarkers of inflammation in COPD patients

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

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

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

Discovery of CP-690,550: a potent and selective Janus kinase (JAK) inhibitor for the treatment of autoimmune diseases and organ transplant rejection

21 January 2018

1 reference

https://api.crossref.org/works/10.1517%2F17460441.2012.724056

10.1517/17460441.2012.724056

21 January 2018

Identifiers

DOI

1 reference

27 August 2017

1 reference