Doing more than just the structure—structural genomics in kinase drug discovery

The Protein Kinase Complement of the Human Genome

2002 • 7,708 citations

How many drug targets are there?

2006 • 3,319 citations

Mechanism of Activation of the RAF-ERK Signaling Pathway by Oncogenic Mutations of B-RAF

2004 • 2,674 citations

The selectivity of protein kinase inhibitors: a further update

2007 • 2,451 citations

Protein kinases — the major drug targets of the twenty-first century?

2002 • 2,101 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

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

2006 • 1,693 citations

ICM—A new method for protein modeling and design: Applications to docking and structure prediction from the distorted native conformation

1994 • 1,630 citations

Halogen bonds in biological molecules

2004 • 1,545 citations

Protein Kinase Inhibitors: Insights into Drug Design from Structure

2004 • 1,180 citations

Rational design of inhibitors that bind to inactive kinase conformations

2006 • 1,013 citations

Inhibition of p38 MAP kinase by utilizing a novel allosteric binding site

2002 • 818 citations

Drugs, their targets and the nature and number of drug targets

2006 • 796 citations

Features of Selective Kinase Inhibitors

2005 • 625 citations

Chemical screening methods to identify ligands that promote protein stability, protein crystallization, and structure determination

2006 • 577 citations

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

2007 • 346 citations

The Crystal Structure of a c-Src Complex in an Active Conformation Suggests Possible Steps in c-Src Activation

2005 • 330 citations

Pathophysiological Roles of ASK1-MAP Kinase Signaling Pathways

2007 • 239 citations

Ruthenium Half-Sandwich Complexes Bound to Protein Kinase Pim-1

2006 • 227 citations

c-Src Binds to the Cancer Drug Imatinib with an Inactive Abl/c-Kit Conformation and a Distributed Thermodynamic Penalty

2007 • 215 citations

Frequent Alterations in the Expression of Serine/Threonine Kinases in Human Cancers

2006 • 188 citations

A Novel Mode of Gleevec Binding Is Revealed by the Structure of Spleen Tyrosine Kinase

2004 • 186 citations

Structural Analysis Identifies Imidazo[1,2-b]Pyridazines as PIM Kinase Inhibitors with In vitro Antileukemic Activity

2007 • 186 citations

Identification of Novel p38α MAP Kinase Inhibitors Using Fragment-Based Lead Generation

2004 • 178 citations

Kinomics—structural biology and chemogenomics of kinase inhibitors and targets

2003 • 175 citations

Nek2 kinase in chromosome instability and cancer

2005 • 170 citations

Kinomics: characterizing the therapeutically validated kinase space

2005 • 158 citations

Structural Basis of Inhibitor Specificity of the Human Protooncogene Proviral Insertion Site in Moloney Murine Leukemia Virus (PIM-1) Kinase

2005 • 149 citations

Advances in the structural biology, design and clinical development of VEGF-R kinase inhibitors for the treatment of angiogenesis

2003 • 133 citations

SAR and inhibitor complex structure determination of a novel class of potent and specific Aurora kinase inhibitors

2005 • 126 citations

Structural and Functional Characterization of the Human Protein Kinase ASK1

2007 • 103 citations

Structure and Regulation of the Human Nek2 Centrosomal Kinase

2007 • 100 citations

Synthesis, Structure and Function of Avian Sarcoma Virus-specific DNA in Permissive and Nonpermissive Cells

1974 • 96 citations

Nek2 as an Effective Target for Inhibition of Tumorigenic Growth and Peritoneal Dissemination of Cholangiocarcinoma

2007 • 94 citations

Alternative binding modes of an inhibitor to two different kinases

2003 • 74 citations

Ruthenium Complexes as Protein Kinase Inhibitors

2004 • 67 citations

The scientific impact of the Structural Genomics Consortium: a protein family and ligand-centered approach to medically-relevant human proteins

2007 • 63 citations

ASK1 (MAP3K5) as a potential therapeutic target in malignant fibrous histiocytomas with 12q14–q15 and 6q23 amplifications

2004 • 60 citations

Molecular Design and Clinical Development of VEGFR Kinase Inhibitors

2007 • 59 citations

The second wave in kinase cancer drugs

2006 • 58 citations

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

2007 • 57 citations

Novel, potent and selective anilinoquinazoline and anilinopyrimidine inhibitors of p38 MAP kinase

2004 • 55 citations

Structural genomics and drug discovery: all in the family

2008 • 42 citations

Detection and Characterization of RNA Tumor Virus-specific DNA in Cells

2015 • 13 citations

Deleted Work

1955 • 0 citations