Inhibition of Protein−Protein Association by Small Molecules: Approaches and Progress

A novel genetic system to detect protein–protein interactions

1989 • 6,022 citations

Discovering High-Affinity Ligands for Proteins: SAR by NMR

1996 • 1,986 citations

Structure and Mechanism in Protein Science. A guide to Enzyme Catalysis and Protein Folding

2001 • 1,799 citations

Crystal Structure of an Hsp90–Geldanamycin Complex: Targeting of a Protein Chaperone by an Antitumor Agent

1997 • 1,345 citations

Apoptosis Signaling

2000 • 1,290 citations

On the attribution and additivity of binding energies

1981 • 902 citations

Pharmacological Rescue of Mutant p53 Conformation and Function

1999 • 794 citations

A small-molecule, nonpeptide CCR5 antagonist with highly potent and selective anti-HIV-1 activity

1999 • 752 citations

Computational Alanine Scanning To Probe Protein−Protein Interactions: A Novel Approach To Evaluate Binding Free Energies

1999 • 741 citations

Identification of small-molecule inhibitors of interaction between the BH3 domain and Bcl-xL

2001 • 546 citations

High-throughput screening: new technology for the 21st century

2000 • 530 citations

Protein−Protein Interactions: Interface Structure, Binding Thermodynamics, and Mutational Analysis

1997 • 474 citations

Binding in the growth hormone receptor complex.

1996 • 434 citations

Proliferation, But Not Growth, Blocked by Conditional Deletion of 40 S Ribosomal Protein S6

2000 • 366 citations

Regulation of Protein Secretion Through Controlled Aggregation in the Endoplasmic Reticulum

2000 • 345 citations

Antimitotic natural products and their interactions with tubulin

1996 • 327 citations

Toward Proteomimetics: Terphenyl Derivatives as Structural and Functional Mimics of Extended Regions of an α-Helix

2001 • 308 citations

A three-hybrid system for detecting small ligand–protein receptor interactions

1996 • 297 citations

A small molecule designed to bind to the adenine nucleotide pocket of Hsp90 causes Her2 degradation and the growth arrest and differentiation of breast cancer cells

2001 • 282 citations

Controlling protein association and subcellular localization with a synthetic ligand that induces heterodimerization of proteins.

1996 • 275 citations

CAVEAT: A program to facilitate the design of organic molecules

1994 • 263 citations

Dissecting cellular processes using small molecules: identification of colchicine-like, taxol-like and other small molecules that perturb mitosis

2000 • 245 citations

Low-Molecular-Weight Peptidic and Cyclic Antagonists of the Receptor for the Complement Factor C5a

1999 • 245 citations

Discovery of Potent Antagonists of the Interaction between Human Double Minute 2 and Tumor Suppressor p53

2000 • 238 citations

A molecular clamp in the crystal structure of the N-terminal domain of the yeast Hsp90 chaperone

1997 • 229 citations

Designed molecules that fold to mimic protein secondary structures

1999 • 204 citations

Allosteric inhibitors of inducible nitric oxide synthase dimerization discovered via combinatorial chemistry

2000 • 198 citations

A ligand-reversible dimerization system for controlling protein–protein interactions

2000 • 187 citations

The Hsp90 complex—a super-chaperone machine as a novel drug target

1998 • 171 citations

Time-resolved fluorometry: an overview of the labels and core technologies for drug screening applications

1997 • 146 citations

Structure-based design of an osteoclast-selective, nonpeptide Src homology 2 inhibitor with in vivo antiresorptive activity

2000 • 133 citations

Inhibiting the assembly of protein—protein interfaces

1998 • 110 citations

Synthesis and evaluation of geldanamycin-estradiol hybrids

1999 • 106 citations

Potent Blockade of Hepatocyte Growth Factor-stimulated Cell Motility, Matrix Invasion and Branching Morphogenesis by Antagonists of Grb2 Src Homology 2 Domain Interactions

2001 • 97 citations

The chemokine/chemokine-receptor family: potential and progress for therapeutic intervention

2000 • 85 citations

Synthesis and evaluation of geldanamycin–testosterone hybrids

2000 • 83 citations

Structure-Based Design and Synthesis of High Affinity Tripeptide Ligands of the Grb2-SH2 Domain

1998 • 82 citations

A diverse set of oligomeric class II MHC-peptide complexes for probing T-cell receptor interactions

2000 • 64 citations

Structure-based Design of Compounds Inhibiting Grb2-SH2 Mediated Protein-protein Interactions in Signal Transduction Pathways

2000 • 62 citations

Structure-Based Design, Synthesis, and X-ray Crystallography of a High-Affinity Antagonist of the Grb2-SH2 Domain Containing an Asparagine Mimetic

1999 • 62 citations

Inhibition by trifluoperazine of calmodulin-induced activation of ATPase activity of rat erythrocyte

1980 • 61 citations

Affinity modulation of small-molecule ligands by borrowing endogenous protein surfaces

1999 • 60 citations

Structure-Based Design of a Novel Series of Nonpeptide Ligands That Bind to the pp60^src SH2 Domain

1997 • 60 citations

Chemokine Receptor Antagonists

2000 • 59 citations

A Src SH2 selective binding compound inhibits osteoclast-mediated resorption

2000 • 59 citations

UCS15A, a non-kinase inhibitor of Src signal transduction

2001 • 58 citations

On the origins of the DNA sequence selectivity of mitomycin monoalkylation transformations

1992 • 47 citations

LY294002-geldanamycin heterodimers as selective inhibitors of the PI3K and PI3K-related family

2001 • 46 citations

Potent Antagonists of the SH2 Domain of Grb2: Optimization of the X₊₁ Position of 3-Amino-Z-Tyr(PO₃H₂)-X₊₁-Asn-NH₂

1998 • 45 citations

Highly potent inhibitors of the Grb2-SH2 domain

1999 • 44 citations

Trifluoperazine, a calmodulin antagonist, inhibits muscle cell fusion.

1983 • 42 citations

Analysis of the binding surfaces of proteins

1999 • 39 citations

Exploring the Specificity Pockets of Two Homologous SH3 Domains Using Structure-Based, Split-Pool Synthesis and Affinity-Based Selection

1998 • 38 citations

An elF-4A-like protein is a suppressor of an Escherichia coli mutant defective in 5OS ribosomal subunit assembly

1989 • 37 citations

The formation of a covalent complex between a dipeptide ligand and the src SH2 domain

1998 • 19 citations

Nonpeptidic, Monocharged, Cell Permeable Ligands for the p56lck SH2 Domain

2001 • 13 citations