Discovery of small molecule cancer drugs: successes, challenges and opportunities (Q37996113)

26 August 2017

1 reference

8 February 2021

1 reference

PubMed publication ID

22440008

title

Discovery of small molecule cancer drugs: successes, challenges and opportunities (English)

1 reference

26 August 2017

1 reference

14 September 2020

1 reference

8 February 2021

3

Paul Workman

1 reference

26 August 2017

Swen Hoelder

1

1 reference

26 August 2017

Paul A Clarke

series ordinal

2

1 reference

26 August 2017

language of work or name

1 reference

3 March 2012

1 reference

26 August 2017

1 April 2012

3 references

3 April 2019

14 September 2020

8 February 2021

4 references

26 August 2017

3 April 2019

14 September 2020

8 February 2021

6

1 reference

26 August 2017

2

1 reference

26 August 2017

155-176

1 reference

Creative Commons Attribution-NonCommercial-NoDerivatives

26 August 2017

3 references

3 April 2019

14 September 2020

8 February 2021

on focus list of Wikimedia project

ScienceSource

0 references

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6 September 2017

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Functional viability profiles of breast cancer

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A novel ALK secondary mutation and EGFR signaling cause resistance to ALK kinase inhibitors

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Towards systematic functional characterization of cancer genomes

6 September 2017

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Improved survival with vemurafenib in melanoma with BRAF V600E mutation

6 September 2017

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Abiraterone and increased survival in metastatic prostate cancer

6 September 2017

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A molecular informatics view on best practice in multi-parameter compound optimization

6 September 2017

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

6 September 2017

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The resurgence of covalent drugs

6 September 2017

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Exploring the genomes of cancer cells: progress and promise

6 September 2017

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PTEN loss in the continuum of common cancers, rare syndromes and mouse models.

6 September 2017

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Genomics and the continuum of cancer care

6 September 2017

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How genetically engineered mouse tumor models provide insights into human cancers

6 September 2017

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Vigilance and validation: Keys to success in RNAi screening

6 September 2017

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Preclinical development of molecular-targeted agents for cancer

6 September 2017

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Melanomas acquire resistance to B-RAF(V600E) inhibition by RTK or N-RAS upregulation

6 September 2017

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COT drives resistance to RAF inhibition through MAP kinase pathway reactivation

6 September 2017

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Transcript profiling and RNA interference as tools to identify small molecule mechanisms and therapeutic potential

6 September 2017

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Anaplastic lymphoma kinase inhibition in non-small-cell lung cancer

6 September 2017

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Clinical implications of the cancer genome

6 September 2017

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Quo vadis, virtual screening? A comprehensive survey of prospective applications

6 September 2017

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

6 September 2017

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

6 September 2017

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6 September 2017

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Probing the probes: fitness factors for small molecule tools

6 September 2017

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MK-2206, an allosteric Akt inhibitor, enhances antitumor efficacy by standard chemotherapeutic agents or molecular targeted drugs in vitro and in vivo

6 September 2017

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Guidelines for the welfare and use of animals in cancer research

6 September 2017

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Cheminformatics approaches to analyze diversity in compound screening libraries.

6 September 2017

1 reference

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Evolving molecules using multi-objective optimization: applying to ADME/Tox

6 September 2017

1 reference

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Apparent activity in high-throughput screening: origins of compound-dependent assay interference

6 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3476506

Genomic screening with RNAi: results and challenges

6 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3476506

Virtual screening: an endless staircase?

6 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3476506

High-throughput RNAi screening to dissect cellular pathways: a how-to guide.

6 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3476506

Cell line-based platforms to evaluate the therapeutic efficacy of candidate anticancer agents

6 September 2017

1 reference

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How to improve R&D productivity: the pharmaceutical industry's grand challenge

6 September 2017

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

6 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3476506

Biomarker-driven early clinical trials in oncology: a paradigm shift in drug development

6 September 2017

1 reference

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Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling

6 September 2017

1 reference

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RNA interference screening for the discovery of oncology targets

6 September 2017

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Combining hit identification strategies: fragment-based and in silico approaches to orally active 2-aminothieno[2,3-d]pyrimidine inhibitors of the Hsp90 molecular chaperone

6 September 2017

1 reference

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Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103 through PI-540, PI-620 to the oral agent GDC-0941

6 September 2017

1 reference

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Inhibition of poly(ADP-ribose) polymerase in tumors from BRCA mutation carriers

6 September 2017

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Trapping moving targets with small molecules

6 September 2017

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Principles of cancer therapy: oncogene and non-oncogene addiction

6 September 2017

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Covalent modifiers: an orthogonal approach to drug design

6 September 2017

1 reference

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American Society of Clinical Oncology provisional clinical opinion: testing for KRAS gene mutations in patients with metastatic colorectal carcinoma to predict response to anti-epidermal growth factor receptor monoclonal antibody therapy

6 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3476506

Beyond picomolar affinities: quantitative aspects of noncovalent and covalent binding of drugs to proteins

6 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3476506

Predicting druggable binding sites at the protein-protein interface.

6 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3476506

The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer

6 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3476506

Physiochemical drug properties associated with in vivo toxicological outcomes

6 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3476506

Targeted therapy for cancer using PARP inhibitors

6 September 2017

1 reference

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6 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3476506

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

6 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3476506

The challenge of drugging undruggable targets in cancer: lessons learned from targeting BCL-2 family members

6 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3476506

4,5-diarylisoxazole Hsp90 chaperone inhibitors: potential therapeutic agents for the treatment of cancer

6 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3476506

Identification of the transforming EML4-ALK fusion gene in non-small-cell lung cancer

6 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3476506

Inhibition of the heat shock protein 90 molecular chaperone in vitro and in vivo by novel, synthetic, potent resorcinylic pyrazole/isoxazole amide analogues

6 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3476506

Synthetic lethal screen identification of chemosensitizer loci in cancer cells

6 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3476506

A decade of fragment-based drug design: strategic advances and lessons learned

6 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3476506

Economics of new oncology drug development

6 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3476506

Five-year follow-up of patients receiving imatinib for chronic myeloid leukemia

6 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3476506

New approaches to molecular cancer therapeutics

6 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3476506

Drug-target residence time and its implications for lead optimization

6 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3476506

Validating cancer drug targets

6 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3476506

An inhibitor of Bcl-2 family proteins induces regression of solid tumours

6 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3476506

Druggability indices for protein targets derived from NMR-based screening data

6 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3476506

High-throughput drug discovery: what can we expect from HTS?

6 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3476506

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

6 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3476506

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

6 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3476506

Can the pharmaceutical industry reduce attrition rates?

6 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3476506

Pursuing the leadlikeness concept in pharmaceutical research.

6 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3476506

Ligand efficiency: a useful metric for lead selection

6 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3476506

How much gets there and what does it do?: The need for better pharmacokinetic and pharmacodynamic endpoints in contemporary drug discovery and development

6 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3476506

Imatinib compared with interferon and low-dose cytarabine for newly diagnosed chronic-phase chronic myeloid leukemia

6 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3476506

Auditing the pharmacological accounts for Hsp90 molecular chaperone inhibitors: unfolding the relationship between pharmacokinetics and pharmacodynamics.

6 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3476506

6 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3476506

Cancer. Addiction to oncogenes--the Achilles heal of cancer

6 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3476506

Mutations of the BRAF gene in human cancer

6 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3476506

Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings

6 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3476506

Use of chemotherapy plus a monoclonal antibody against HER2 for metastatic breast cancer that overexpresses HER2.

6 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=3476506

6 September 2017

The Hallmarks of Cancer

1 reference

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Use of all-trans retinoic acid in the treatment of acute promyelocytic leukemia

6 September 2017

1 reference

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Studies of the HER-2/neu proto-oncogene in human breast and ovarian cancer

6 September 2017

1 reference

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canSAR: an integrated cancer public translational research and drug discovery resource

6 September 2017

1 reference

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Poly(ADP)-ribose polymerase inhibition: frequent durable responses in BRCA carrier ovarian cancer correlating with platinum-free interval

6 September 2017

1 reference

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GDC-0449-a potent inhibitor of the hedgehog pathway

14 September 2017

1 reference

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Inhibitor hijacking of Akt activation

14 September 2017

1 reference

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Impact of common epidermal growth factor receptor and HER2 variants on receptor activity and inhibition by lapatinib

14 September 2017

1 reference

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The druggable genome: an update

14 September 2017

1 reference

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The identification, synthesis, protein crystal structure and in vitro biochemical evaluation of a new 3,4-diarylpyrazole class of Hsp90 inhibitors

14 September 2017

1 reference

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Imatinib mesylate (Gleevec) inhibits ovarian cancer cell growth through a mechanism dependent on platelet-derived growth factor receptor alpha and Akt inactivation

14 September 2017

1 reference

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Drug development: portals of discovery

14 September 2017

1 reference

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Impact of high-throughput screening in biomedical research

31 August 2018

1 reference

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Advances in the preclinical testing of cancer therapeutic hypotheses.

31 August 2018

1 reference

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Competitiveness in follow-on drug R&D: a race or imitation?

31 August 2018

1 reference

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Envisioning the future of early anticancer drug development.

31 August 2018

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Paul Ehrlich: founder of chemotherapy

31 August 2018

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The influence of drug-like concepts on decision-making in medicinal chemistry

31 August 2018

1 reference

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Interpreting steep dose-response curves in early inhibitor discovery

31 August 2018

1 reference

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Discovery of a potent inhibitor of the antiapoptotic protein Bcl-xL from NMR and parallel synthesis

31 August 2018

1 reference

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Ligand efficiency indices as guideposts for drug discovery.

31 August 2018

1 reference

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Efficacy and safety of imatinib in adult patients with c-kit-positive acute myeloid leukemia

31 August 2018

1 reference

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Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings

31 August 2018

1 reference

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Unswitch-ABL Drugs Overcome Resistance in Chronic Myeloid Leukemia

21 January 2018

1 reference

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Translating cancer research into targeted therapeutics

21 January 2018

1 reference

https://api.crossref.org/works/10.1016%2FJ.MOLONC.2012.02.004

Cancer robustness: Tumour tactics

21 January 2018

1 reference

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21 January 2018

1 reference

12 December 2020

The rise and fall of gatekeeper mutations? TheBCR-ABL1T315I paradigm

1 reference

12 December 2020

A blueprint for advancing genetics-based cancer therapy

1 reference

12 December 2020

Phosphatidylinositide-3-kinase inhibitors: addressing questions of isoform selectivity and pharmacodynamic/predictive biomarkers in early clinical trials

1 reference

12 December 2020

Extracting kinetic rate constants from surface plasmon resonance array systems

1 reference

12 December 2020

Follow-on drugs: how far should chemists look?

1 reference

12 December 2020

Genetic Interactions in Cancer Progression and Treatment

1 reference

12 December 2020

Getting pharmaceutical R&D back on target

1 reference

12 December 2020

Improving the efficacy of translational medicine by optimally integrating health care, academia and industry

1 reference

12 December 2020

10.1016/J.MOLONC.2012.02.004

Identifiers

DOI

1 reference

26 August 2017

1 reference

26 August 2017

PubMed publication ID

22440008

1 reference