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Targeted Therapy for Breast Cancer - MedStar Health Cancer Network

No notes for slide. Veterinary Pathophysiology [PDF] 1. Med Chem Comm. Lamba V, Ghosh I. New directions in targeting protein kinases: focusing upon true allosteric and bivalent inhibitors. Curr Pharm Des. Liu Y, Gray NS.

Report of the Chemoprevention Working Group to the American Association for Cancer Research

Rational design of inhibitors that bind to inactive kinase conformations. Nat Chem Biol. Targeting cancer with small molecule kinase inhibitors.

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Comprehensive analysis of kinase inhibitor selectivity. Force T, Kolaja KL. Cardiotoxicity of kinase inhibitors: the prediction and translation of preclinical models to clinical outcomes.

Prevention of Cancer in the Next Millennium

Hasinoff BB. The cardiotoxicity and myocyte damage caused by small molecule anticancer tyrosine kinase inhibitors is correlated with lack of target specificity. Toxicol Appl Pharmacol. Kufareva I, Abagyan R. Type-II kinase inhibitor docking, screening, and profiling using modified structures of active kinase states. Glutamine addiction: a new therapeutic target in cancer.

Advances of small molecule targeting of kinases.

Edited by Jim Cassidy, Donald Bissett, Roy Spence, and Miranda Payne

Curr Opin Chem Biol. Eglen R, Reisine T. Drug discovery and the human kinome: recent trends. Pharmacol Ther. In Seminars in oncology. Amsterdam: Elsevier; The target landscape of clinical kinase drugs. Allosteric inhibitors of Bcr-abl—dependent cell proliferation. Bioorg Med Chem Lett. Allosteric activators of glucokinase: potential role in diabetes therapy. Guertin KR, Grimsby J. Small molecule glucokinase activators as glucose lowering agents: a new paradigm for diabetes therapy. Curr Med Chem. Type II kinase inhibitors: an opportunity in cancer for rational design.

The Bcr-Abl tyrosine kinase inhibitor imatinib and promising new agents against Philadelphia chromosome-positive leukemias. Int J Clin Oncol. Structural bioinformatics-based design of selective, irreversible kinase inhibitors. Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib.

Oral Microbiome and Cancer Therapy-Induced Oral Mucositis | JNCI Monographs | Oxford Academic

Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors. Developing irreversible inhibitors of the protein kinase cysteinome. Chem Biol. The resurgence of covalent drugs. Barf T, Kaptein A. Irreversible protein kinase inhibitors: balancing the benefits and risks. Determining cysteines available for covalent inhibition across the human kinome. Second and third-generation epidermal growth factor receptor tyrosine kinase inhibitors in advanced nonsmall cell lung cancer.

Curr Opin Oncol. Ibrutinib targets mutant-EGFR kinase with a distinct binding conformation.

Protein kinase biochemistry and drug discovery. Bioorg Chem. An alternative inhibitor overcomes resistance caused by a mutation of the epidermal growth factor receptor.

Moebitz H. The ABC of protein kinase conformations. Cohen P. Protein kinases—the major drug targets of the twenty-first century? Kinomics: characterizing the therapeutically validated kinase space. Drug Discov Today. A molecular brake in the kinase hinge region regulates the activity of receptor tyrosine kinases. Structural biology of protein tyrosine kinases. In: Protein Tyrosine Kinases.

New York: Springer; Regulation of protein kinases: controlling activity through activation segment conformation. Active and inactive protein kinases: structural basis for regulation. Scapin G. Protein kinase inhibition: different approaches to selective inhibitor design. Curr Drug Targets. Structural characterization of proline-rich tyrosine kinase 2 PYK2 reveals a unique DFG-out conformation and enables inhibitor design. Tyrosine kinase inhibitors: from rational design to clinical trials.