Turning promiscuous kinase inhibitors into safer drugs

Goodman and Gilman's the Pharmacological Basis of Therapeutics

1986 • 6,964 citations

Efficacy and Safety of Imatinib Mesylate in Advanced Gastrointestinal Stromal Tumors

2002 • 4,254 citations

A quantitative analysis of kinase inhibitor selectivity

2008 • 2,334 citations

A small molecule–kinase interaction map for clinical kinase inhibitors

2005 • 1,854 citations

Structural Mechanism for STI-571 Inhibition of Abelson Tyrosine Kinase

2000 • 1,770 citations

Tyrosine Kinase Inhibition: An Approach to Drug Development

1995 • 1,655 citations

Protein Kinase Inhibitors: Insights into Drug Design from Structure

2004 • 1,180 citations

Cardiotoxicity of the cancer therapeutic agent imatinib mesylate

2006 • 1,126 citations

Magic shotguns versus magic bullets: selectively non-selective drugs for mood disorders and schizophrenia

2004 • 1,111 citations

Rational design of inhibitors that bind to inactive kinase conformations

2006 • 1,013 citations

Molecular mechanisms of cardiotoxicity of tyrosine kinase inhibition

2007 • 765 citations

Multicomponent therapeutics for networked systems

2005 • 749 citations

A Specific Mechanism of Nonspecific Inhibition

2003 • 584 citations

Issues and progress with protein kinase inhibitors for cancer treatment

2003 • 529 citations

Combinatorial chemoprevention of intestinal neoplasia

2000 • 492 citations

Can we rationally design promiscuous drugs?

2006 • 461 citations

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

2007 • 346 citations

High-throughput assays for promiscuous inhibitors

2005 • 328 citations

Playing dirty

2005 • 326 citations

Inhibition of the ABL Kinase Activity Blocks the Proliferation of BCR/ABL+Leukemic Cells and Induces Apoptosis

1997 • 325 citations

Identifying off-target effects and hidden phenotypes of drugs in human cells

2006 • 284 citations

Insufficiently dehydrated hydrogen bonds as determinants of protein interactions

2002 • 254 citations

Synthesis and Structure−Activity Relationships of 6,7-Disubstituted 4-Anilinoquinoline-3-carbonitriles. The Design of an Orally Active, Irreversible Inhibitor of the Tyrosine Kinase Activity of the Epidermal Growth Factor Receptor (EGFR) and the Human Epidermal Growth Factor Receptor-2 (HER-2)

2002 • 253 citations

GOODMAN AND GILMAN'S THE PHARMACOLOGICAL BASIS OF THERAPEUTICS

1981 • 211 citations

Promiscuous drugs compared to selective drugs (promiscuity can be a virtue)

2005 • 196 citations

Predicting ADME properties and side effects: the BioPrint approach.

2003 • 176 citations

An anticancer C-Kit kinase inhibitor is reengineered to make it more active and less cardiotoxic

2007 • 161 citations

A new paradigm for protein kinase inhibition: blocking phosphorylation without directly targeting ATP binding

2007 • 158 citations

Phase I Study of EKB-569, an Irreversible Inhibitor of the Epidermal Growth Factor Receptor, in Patients With Advanced Solid Tumors

2006 • 145 citations

Pharmaceutical research in molecular oncology

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TYROSINE KINASE INHIBITORS AND THE DAWN OF MOLECULAR CANCER THERAPEUTICS

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Design of Non-Nucleoside Inhibitors of HIV-1 Reverse Transcriptase with Improved Drug Resistance Properties. 1.

2004 • 89 citations

Keeping dry and crossing membranes

2004 • 69 citations

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

2007 • 57 citations

Molecular dimension explored in evolution to promote proteomic complexity

2004 • 48 citations

Molecular basis for specificity in the druggable kinome: sequence-based analysis

2007 • 47 citations

"Promiscuous" Anticancer Drugs That Hit Multiple Targets May Thwart Resistance

2004 • 46 citations

Dehydration Propensity of Order−Disorder Intermediate Regions in Soluble Proteins

2007 • 43 citations

Failure and Success in Modern Drug Discovery: Guiding Principles in the Establishment of High Probability of Success Drug Discovery Organizations

2005 • 42 citations

Kinase packing defects as drug targets

2007 • 23 citations

Redesigning kinase inhibitors

2008 • 20 citations

Dirty drugs' secrets uncovered

2006 • 7 citations