Discovery of small molecule cancer drugs: Successes, challenges and opportunities
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[1] Paul Workman,et al. HSP90 inhibition: two-pronged exploitation of cancer dependencies. , 2012, Drug discovery today.
[2] David R. Jones,et al. New regulatory framework for cancer drug development. , 2012, Drug discovery today.
[3] Michele De Palma,et al. The biology of personalized cancer medicine: Facing individual complexities underlying hallmark capabilities , 2012, Molecular oncology.
[4] Channa K. Hattotuwagama,et al. Lead-oriented synthesis: a new opportunity for synthetic chemistry. , 2012, Angewandte Chemie.
[5] T. Blundell,et al. Structural biology and drug discovery of difficult targets: the limits of ligandability. , 2012, Chemistry & biology.
[6] P. Workman,et al. Phosphatidylinositide-3-kinase inhibitors: addressing questions of isoform selectivity and pharmacodynamic/predictive biomarkers in early clinical trials. , 2012, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.
[7] H. Kantarjian,et al. The rise and fall of gatekeeper mutations? The BCR‐ABL1 T315I paradigm , 2012, Cancer.
[8] P. Workman,et al. Exploiting the cancer genome: strategies for the discovery and clinical development of targeted molecular therapeutics. , 2012, Annual review of pharmacology and toxicology.
[9] Melanie Leveridge,et al. Configuration of a High-Content Imaging Platform for Hit Identification and Pharmacological Assessment of JMJD3 Demethylase Enzyme Inhibitors , 2012, Journal of biomolecular screening.
[10] G. Giaccone,et al. Drug Development: Portals of Discovery , 2012, Clinical Cancer Research.
[11] Paul Workman,et al. Hsp90 Molecular Chaperone Inhibitors: Are We There Yet? , 2012, Clinical Cancer Research.
[12] E. Scott,et al. CYTOCHROME P450 17A1 STRUCTURES WITH PROSTATE CANCER DRUGS ABIRATERONE AND TOK-001 , 2011, Nature.
[13] Bissan Al-Lazikani,et al. canSAR: an integrated cancer public translational research and drug discovery resource , 2011, Nucleic Acids Res..
[14] E. Scott,et al. Structures of cytochrome P 450 17 A 1 with prostate cancer drugs abiraterone and TOK-001 , 2012 .
[15] R. A. Thompson,et al. Hypothesis driven drug design: improving quality and effectiveness of the design-make-test-analyse cycle. , 2012, Drug discovery today.
[16] J. Licinio,et al. Improving the efficacy of translational medicine by optimally integrating health care, academia and industry , 2011, Nature Medicine.
[17] Tom Misteli,et al. RAF inhibitor resistance is mediated by dimerization of aberrantly spliced BRAF(V600E) , 2011, Nature.
[18] W. Sellers. A Blueprint for Advancing Genetics-Based Cancer Therapy , 2011, Cell.
[19] Wei Zheng,et al. A novel ALK secondary mutation and EGFR signaling cause resistance to ALK kinase inhibitors. , 2011, Cancer research.
[20] F. Prinz,et al. Believe it or not: how much can we rely on published data on potential drug targets? , 2011, Nature Reviews Drug Discovery.
[21] J. Christensen,et al. Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). , 2011, Journal of medicinal chemistry.
[22] Jonas Boström,et al. Follow-on drugs: how far should chemists look? , 2011, Drug discovery today.
[23] Alan Mackay,et al. Functional viability profiles of breast cancer. , 2011, Cancer discovery.
[24] Sarat Chandarlapaty,et al. mTOR kinase inhibition causes feedback-dependent biphasic regulation of AKT signaling. , 2011, Cancer discovery.
[25] William C. Hahn,et al. Towards systematic functional characterization of cancer genomes , 2011, Nature Reviews Genetics.
[26] Ross McGuire,et al. A molecular informatics view on best practice in multi-parameter compound optimization. , 2011, Drug discovery today.
[27] A. Hauschild,et al. Improved survival with vemurafenib in melanoma with BRAF V600E mutation. , 2011, The New England journal of medicine.
[28] W. Pao,et al. How genetically engineered mouse tumor models provide insights into human cancers. , 2011, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.
[29] M. Bunnage. Getting pharmaceutical R&D back on target. , 2011, Nature chemical biology.
[30] Arturo Molina,et al. Abiraterone and increased survival in metastatic prostate cancer. , 2011, The New England journal of medicine.
[31] M. Hann. Molecular obesity, potency and other addictions in drug discovery , 2011 .
[32] L. Packer,et al. Unswitch-ABL drugs overcome resistance in chronic myeloid leukemia. , 2011, Cancer cell.
[33] L. Stewart,et al. Conformational control inhibition of the BCR-ABL1 tyrosine kinase, including the gatekeeper T315I mutant, by the switch-control inhibitor DCC-2036. , 2011, Cancer cell.
[34] Lillian L. Siu,et al. Preclinical development of molecular-targeted agents for cancer , 2011, Nature Reviews Clinical Oncology.
[35] P. Dennis,et al. PTEN loss in the continuum of common cancers, rare syndromes and mouse models , 2011, Nature Reviews Cancer.
[36] Adrian Whitty,et al. The resurgence of covalent drugs , 2011, Nature Reviews Drug Discovery.
[37] A. Ashworth,et al. Genetic Interactions in Cancer Progression and Treatment , 2011, Cell.
[38] M. Stratton. Exploring the Genomes of Cancer Cells: Progress and Promise , 2011, Science.
[39] D. Bojanic,et al. Impact of high-throughput screening in biomedical research , 2011, Nature Reviews Drug Discovery.
[40] William R. Sellers,et al. Advances in the preclinical testing of cancer therapeutic hypotheses , 2011, Nature Reviews Drug Discovery.
[41] Michael R Stratton,et al. Genomics and the continuum of cancer care. , 2011, The New England journal of medicine.
[42] R. King,et al. Vigilance and validation: Keys to success in RNAi screening. , 2011, ACS chemical biology.
[43] P. Hergenrother,et al. Transcript profiling and RNA interference as tools to identify small molecule mechanisms and therapeutic potential. , 2011, ACS chemical biology.
[44] J. DiMasi,et al. Competitiveness in follow-on drug R&D: a race or imitation? , 2011, Nature Reviews Drug Discovery.
[45] L. Neckers,et al. Hsp 90 Molecular Chaperone Inhibitors : Are We There Yet ? , 2011 .
[46] S. Nelson,et al. Melanomas acquire resistance to B-RAF(V600E) inhibition by RTK or N-RAS upregulation , 2010, Nature.
[47] C. Der. Faculty Opinions recommendation of COT drives resistance to RAF inhibition through MAP kinase pathway reactivation. , 2010 .
[48] L. Garraway,et al. Clinical implications of the cancer genome. , 2010, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.
[49] Jeffrey W. Clark,et al. Anaplastic lymphoma kinase inhibition in non-small-cell lung cancer. , 2010, The New England journal of medicine.
[50] J. Bajorath,et al. Quo vadis, virtual screening? A comprehensive survey of prospective applications. , 2010, Journal of medicinal chemistry.
[51] Alan Ashworth,et al. Translating cancer research into targeted therapeutics , 2010, Nature.
[52] B. Brandhuber,et al. Crystal Structure of Human AKT1 with an Allosteric Inhibitor Reveals a New Mode of Kinase Inhibition , 2010, PloS one.
[53] Kam Y. J. Zhang,et al. Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma , 2010, Nature.
[54] Paul Workman,et al. Envisioning the future of early anticancer drug development , 2010, Nature Reviews Cancer.
[55] Shin-ichi Sato,et al. Biochemical target isolation for novices: affinity-based strategies. , 2010, Chemistry & biology.
[56] Ian Collins,et al. Probing the Probes: Fitness Factors For Small Molecule Tools , 2010, Chemistry & biology.
[57] P. Majumder,et al. MK-2206, an Allosteric Akt Inhibitor, Enhances Antitumor Efficacy by Standard Chemotherapeutic Agents or Molecular Targeted Drugs In vitro and In vivo , 2010, Molecular Cancer Therapeutics.
[58] C. Bakal,et al. Genomic screening with RNAi: results and challenges. , 2010, Annual review of biochemistry.
[59] David DeCaprio,et al. Cheminformatics approaches to analyze diversity in compound screening libraries. , 2010, Current opinion in chemical biology.
[60] James Inglese,et al. Apparent activity in high-throughput screening: origins of compound-dependent assay interference. , 2010, Current opinion in chemical biology.
[61] Sean Ekins,et al. Evolving molecules using multi-objective optimization: applying to ADME/Tox. , 2010, Drug discovery today.
[62] A. Balmain,et al. Guidelines for the welfare and use of animals in cancer research , 2010, British Journal of Cancer.
[63] Jan Lubinski,et al. Poly(ADP)-ribose polymerase inhibition: frequent durable responses in BRCA carrier ovarian cancer correlating with platinum-free interval. , 2010, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.
[64] Michael Boutros,et al. High‐throughput RNAi screening to dissect cellular pathways: A how‐to guide , 2010, Biotechnology journal.
[65] Gisbert Schneider,et al. Virtual screening: an endless staircase? , 2010, Nature Reviews Drug Discovery.
[66] D. Haber,et al. Cell line-based platforms to evaluate the therapeutic efficacy of candidate anticancer agents , 2010, Nature Reviews Cancer.
[67] Charles C. Persinger,et al. How to improve R&D productivity: the pharmaceutical industry's grand challenge , 2010, Nature Reviews Drug Discovery.
[68] J. Baell,et al. New substructure filters for removal of pan assay interference compounds (PAINS) from screening libraries and for their exclusion in bioassays. , 2010, Journal of medicinal chemistry.
[69] J. Salk. Clonal evolution in cancer , 2010 .
[70] A. Ashworth,et al. Inhibition of poly(ADP-ribose) polymerase in tumors from BRCA mutation carriers. , 2009, The New England journal of medicine.
[71] K. Kotkow,et al. GDC-0449-a potent inhibitor of the hedgehog pathway. , 2009, Bioorganic & medicinal chemistry letters.
[72] Marc W. Kirschner,et al. Tankyrase inhibition stabilizes axin and antagonizes Wnt signalling , 2009, Nature.
[73] P. Workman,et al. Biomarker-Driven Early Clinical Trials in Oncology: A Paradigm Shift in Drug Development , 2009, Cancer journal.
[74] P. Kassner,et al. RNA interference screening for the discovery of oncology targets , 2009, Expert opinion on therapeutic targets.
[75] X. Barril,et al. 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. , 2009, Journal of medicinal chemistry.
[76] P. Workman,et al. 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 , 2009, Molecular Cancer Therapeutics.
[77] Chao Zhang,et al. Inhibitor Hijacking of Akt Activation , 2009, Nature chemical biology.
[78] M. Somerfield,et al. 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. , 2009, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.
[79] C. Craik,et al. Trapping Moving Targets with Small Molecules , 2009, Science.
[80] Ji Luo,et al. Principles of Cancer Therapy: Oncogene and Non-oncogene Addiction , 2009, Cell.
[81] M. Potashman,et al. Covalent modifiers: an orthogonal approach to drug design. , 2009, Journal of medicinal chemistry.
[82] Jonathan C. Fuller,et al. Predicting druggable binding sites at the protein-protein interface. , 2009, Drug discovery today.
[83] Andrew G. Leach,et al. Beyond picomolar affinities: quantitative aspects of noncovalent and covalent binding of drugs to proteins. , 2009, Journal of medicinal chemistry.
[84] J. McNamara. Cancer Stem Cells , 2007, Methods in Molecular Biology.
[85] S. Elledge,et al. Principles of Cancer Therapy: Oncogene and Non-oncogene Addiction , 2009, Cell.
[86] J. Hughes,et al. Physiochemical drug properties associated with in vivo toxicological outcomes. , 2008, Bioorganic & medicinal chemistry letters.
[87] Gary Box,et al. 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 . , 2008, Journal of medicinal chemistry.
[88] A. Ashworth,et al. Targeted therapy for cancer using PARP inhibitors. , 2008, Current opinion in pharmacology.
[89] Stefan H. E. Kaufmann,et al. Paul Ehrlich: founder of chemotherapy , 2008, Nature Reviews Drug Discovery.
[90] Kam Y. J. Zhang,et al. Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity , 2008, Proceedings of the National Academy of Sciences.
[91] J. Jenkins,et al. Extracting kinetic rate constants from surface plasmon resonance array systems. , 2008, Analytical biochemistry.
[92] L. Shewchuk,et al. Impact of common epidermal growth factor receptor and HER2 variants on receptor activity and inhibition by lapatinib. , 2008, Cancer research.
[93] Mike Wood,et al. 4,5-diarylisoxazole Hsp90 chaperone inhibitors: potential therapeutic agents for the treatment of cancer. , 2007, Journal of medicinal chemistry.
[94] A. Joe,et al. Oncogene addiction. , 2008, Cancer research.
[95] G. Verdine,et al. The Challenge of Drugging Undruggable Targets in Cancer: Lessons Learned from Targeting BCL-2 Family Members , 2007, Clinical Cancer Research.
[96] P. Leeson,et al. The influence of drug-like concepts on decision-making in medicinal chemistry , 2007, Nature Reviews Drug Discovery.
[97] H. Aburatani,et al. Identification of the transforming EML4–ALK fusion gene in non-small-cell lung cancer , 2007, Nature.
[98] Michael Peyton,et al. Synthetic lethal screen identification of chemosensitizer loci in cancer cells , 2007, Nature.
[99] L. Pearl,et al. Inhibition of the heat shock protein 90 molecular chaperone in vitro and in vivo by novel, synthetic, potent resorcinylic pyrazole/isoxazole amide analogues , 2007, Molecular Cancer Therapeutics.
[100] P. Hajduk,et al. A decade of fragment-based drug design: strategic advances and lessons learned , 2007, Nature Reviews Drug Discovery.
[101] R. Copeland,et al. Drug–target residence time and its implications for lead optimization , 2007, Nature Reviews Drug Discovery.
[102] Joseph A DiMasi,et al. Economics of new oncology drug development. , 2007, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.
[103] Francisco Cervantes,et al. Five-year follow-up of patients receiving imatinib for chronic myeloid leukemia. , 2006, The New England journal of medicine.
[104] Ian Collins,et al. New approaches to molecular cancer therapeutics , 2006, Nature chemical biology.
[105] Brian K Shoichet,et al. Interpreting steep dose-response curves in early inhibitor discovery. , 2006, Journal of medicinal chemistry.
[106] R. Copeland,et al. Drug–target residence time and its implications for lead optimization , 2006, Nature Reviews Drug Discovery.
[107] Sunkyu Kim,et al. Validating cancer drug targets , 2006, Nature.
[108] P. Hajduk,et al. Discovery of a potent inhibitor of the antiapoptotic protein Bcl-xL from NMR and parallel synthesis. , 2006, Journal of medicinal chemistry.
[109] S. Lampel,et al. The druggable genome: an update. , 2005, Drug discovery today.
[110] Paul Workman,et al. The identification, synthesis, protein crystal structure and in vitro biochemical evaluation of a new 3,4-diarylpyrazole class of Hsp90 inhibitors. , 2005, Bioorganic & medicinal chemistry letters.
[111] S. Korsmeyer,et al. An inhibitor of Bcl-2 family proteins induces regression of solid tumours , 2005, Nature.
[112] J. T. Metz,et al. Ligand efficiency indices as guideposts for drug discovery. , 2005, Drug discovery today.
[113] P. Hajduk,et al. Druggability indices for protein targets derived from NMR-based screening data. , 2005, Journal of medicinal chemistry.
[114] Zhijian Zhao,et al. Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors. , 2005, Bioorganic & medicinal chemistry letters.
[115] Phillip Gribbon,et al. High-throughput drug discovery: what can we expect from HTS? , 2005, Drug discovery today.
[116] Krystal J Alligood,et al. A Unique Structure for Epidermal Growth Factor Receptor Bound to GW572016 (Lapatinib) , 2004, Cancer Research.
[117] I. Kola,et al. Can the pharmaceutical industry reduce attrition rates? , 2004, Nature Reviews Drug Discovery.
[118] Tudor I. Oprea,et al. Pursuing the leadlikeness concept in pharmaceutical research. , 2004, Current opinion in chemical biology.
[119] A. Hopkins,et al. Ligand efficiency: a useful metric for lead selection. , 2004, Drug discovery today.
[120] A. Marx,et al. Efficacy and safety of imatinib in adult patients with c-kit-positive acute myeloid leukemia. , 2004, Blood.
[121] D. Matei,et al. Imatinib Mesylate (Gleevec) Inhibits Ovarian Cancer Cell Growth through a Mechanism Dependent on Platelet-Derived Growth Factor Receptor α and Akt Inactivation , 2004, Clinical Cancer Research.
[122] Hiroaki Kitano,et al. Cancer robustness: Tumour tactics , 2003, Nature.
[123] P. Workman. How much gets there and what does it do?: The need for better pharmacokinetic and pharmacodynamic endpoints in contemporary drug discovery and development. , 2003, Current pharmaceutical design.
[124] Francisco Cervantes,et al. Imatinib compared with interferon and low-dose cytarabine for newly diagnosed chronic-phase chronic myeloid leukemia. , 2003, The New England journal of medicine.
[125] P. Workman. Auditing the pharmacological accounts for Hsp90 molecular chaperone inhibitors: unfolding the relationship between pharmacokinetics and pharmacodynamics. , 2003, Molecular cancer therapeutics.
[126] A. Hopkins,et al. The druggable genome , 2002, Nature Reviews Drug Discovery.
[127] I. Weinstein. Addiction to Oncogenes--the Achilles Heal of Cancer , 2002, Science.
[128] A. Nicholson,et al. Mutations of the BRAF gene in human cancer , 2002, Nature.
[129] T. Fleming,et al. Use of chemotherapy plus a monoclonal antibody against HER2 for metastatic breast cancer that overexpresses HER2. , 2001, The New England journal of medicine.
[130] Ennis,et al. Use of chemotherapy plus a monoclonal antibody against HER2 for metastatic breast cancer that overexpresses HER2. , 2001, The New England journal of medicine.
[131] F. Lombardo,et al. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings. , 2001, Advanced drug delivery reviews.
[132] D. Hanahan,et al. The Hallmarks of Cancer , 2000, Cell.
[133] W Godolphin,et al. Studies of the HER-2/neu proto-oncogene in human breast and ovarian cancer. , 1989, Science.
[134] Zhen-yi Wang,et al. Use of all-trans retinoic acid in the treatment of acute promyelocytic leukemia. , 1988, Haematology and blood transfusion.