Identification and in vivo efficacy of small-molecule antagonists of integrin αvβ3 (the vitronectin receptor)

Integrins: Versatility, modulation, and signaling in cell adhesion

1992 • 9,986 citations

Principles of Bone Biology

2019 • 1,699 citations

Principles of Bone Biology

1997 • 1,367 citations

Integrins and anoikis

1997 • 1,145 citations

The role of αv integrins during angiogenesis: insights into potential mechanisms of action and clinical development

1999 • 651 citations

Selective recognition of cyclic RGD peptides of NMR defined conformation by alpha IIb beta 3, alpha V beta 3, and alpha 5 beta 1 integrins.

1994 • 527 citations

The αvβ3 integrin “vitronectin receptor”

1997 • 343 citations

Decreased angiogenesis and arthritic disease in rabbits treated with an αvβ3 antagonist

1999 • 306 citations

Integrins and Angiogenesis

2004 • 290 citations

A peptidomimetic antagonist of the alpha(v)beta3 integrin inhibits bone resorption in vitro and prevents osteoporosis in vivo.

1997 • 287 citations

Role of αvβ3 integrin in osteoclast migration and formation of the sealing zone

1999 • 192 citations

Inhibition of neointimal hyperplasia by blocking αvβ3 integrin with a small peptide antagonist GpenGRGDSPCA*

1994 • 190 citations

Bi-directional signal transduction by integrin receptors

2000 • 159 citations

Selective αvβ3 integrin blockade potently limits neointimal hyperplasia and lumen stenosis following deep coronary arterial stent injury1:

1997 • 159 citations

The Integrin Ligand Echistatin Prevents Bone Loss in Ovariectomized Mice and Rats

1998 • 122 citations

Discovery of Orally Active Nonpeptide Vitronectin Receptor Antagonists Based on a 2-Benzazepine Gly-Asp Mimetic

1999 • 115 citations

Discovery of Potent Nonpeptide Vitronectin Receptor (α_Vβ₃) Antagonists

1997 • 114 citations

A peptidomimetic antagonist of the integrin alpha(v)beta3 inhibits Leydig cell tumor growth and the development of hypercalcemia of malignancy.

1998 • 106 citations

Emerging Therapies for the Prevention or Treatment of Postmenopausal Osteoporosis

1998 • 106 citations

Novel small molecule alpha v integrin antagonists: comparative anti-cancer efficacy with known angiogenesis inhibitors.

1999 • 100 citations

Vascular expression of the α_vβ₃-integrin in lung and other organs

2000 • 98 citations

Type II‘ to Type I β-Turn Swap Changes Specificity for Integrins

1996 • 96 citations

Binding of Abciximab to αVβ3 and Activated αMβ2 Receptors: With a Review of Platelet-Leukocyte Interactions

1999 • 96 citations

Potential non-glycoprotein IIb/IIIa effects of abciximab

1999 • 94 citations

Integrin antagonists

1999 • 86 citations

Isoxazolines as Potent Antagonists of the Integrin α_vβ₃

1999 • 85 citations

Novel Solid-Phase Synthesis of Azapeptides and Azapeptoides via Fmoc-Strategy and Its Application in the Synthesis of RGD-Mimetics

1999 • 85 citations

Antibody to beta3 integrin inhibits osteoclast-mediated bone resorption in the thyroparathyroidectomized rat.

1996 • 80 citations

Reduction in Atherosclerotic Lesion Size in Pigs by αVβ3 Inhibitors Is Associated With Inhibition of Insulin-Like Growth Factor-I–Mediated Signaling

1999 • 78 citations

Potent, Selective, Orally Active 3-Oxo-1,4-benzodiazepine GPIIb/IIIa Integrin Antagonists

1996 • 71 citations

Disubstituted Indazoles as Potent Antagonists of the Integrin α_vβ₃

1999 • 71 citations

Design, synthesis and biological evaluation of carbohydrate-based mimetics of cRGDFV

1997 • 70 citations

Solid-phase synthesis of a selective αvβ3 integrin antagonist library

1997 • 69 citations

Vitaxin, a Humanized Monoclonal Antibody to the Vitronectin Receptor (α _v β ₃ ), Reduces Neointimal Hyperplasia and Total Vessel Area After Balloon Injury in Hypercholesterolemic Rabbits

1999 • 68 citations

Design, synthesis and biological evaluation of nonpeptide integrin antagonists

1998 • 62 citations

Integrin cell adhesion receptors and the concept of agonism

2000 • 58 citations

Clinical management of rheumatoid arthritis

1993 • 58 citations

Antagonism of the Osteoclast Vitronectin Receptor with an Orally Active Nonpeptide Inhibitor Prevents Cancellous Bone Loss in the Ovariectomized Rat

2001 • 55 citations

Synthetic αVβ3 Antagonists Inhibit Insulin-Like Growth Factor-I-Stimulated Smooth Muscle Cell Migration and Replication1

1999 • 52 citations

Design and characterization of orally active Arg-Gly-Asp peptidomimetic vitronectin receptor antagonist SB 265123 for prevention of bone loss in osteoporosis.

1999 • 47 citations

Structure-Activity Relationships of Amino Acid-Containing lntegrin Antagonists

1999 • 46 citations

?v?3, ?v?5, and osteopontin are coordinately upregulated at early time points in a rabbit model of neointima formation

1999 • 46 citations

Synthesis and Solution Conformation of Cyclo[RGDRGD]: A Cyclic Peptide with Selectivity for the αVβ3 Receptor

1996 • 40 citations

Preclinical pharmacokinetics and interspecies scaling of a novel vitronectin receptor antagonist.

1999 • 39 citations

Structure-activity relationships of beta-amino acid-containing integrin antagonists.

1999 • 36 citations

Reduced Intimal Thickening Following αvβ 3 Blockade is Associated with Smooth Muscle Cell Apoptosis

1998 • 36 citations

RGD Mimetics containing a central hydantoin scaffold: α V β 3 vs α IIb β 3 selectivity requirements

2000 • 35 citations

Vascular Indications for Integrin αv Antagonists

1997 • 34 citations

Orally bioavailable nonpeptide vitronectin receptor antagonists with efficacy in an osteoporosis model

1999 • 34 citations

A role for angiogenesis in rheumatoid arthritis

1999 • 33 citations

The Integrin Ligand Echistatin Prevents Bone Loss in Ovariectomized Mice and Rats

1998 • 33 citations

Orally bioavailable nonpeptide vitronectin receptor antagonists containing 2-aminopyridine arginine mimetics

1999 • 30 citations

Rapid synthesis of RGD mimetics with isoxazoline scaffolds on solid phase: Identification of αvβ3 antagonists lead compounds

1999 • 27 citations

Combinatorial Chemistry Techniques Applied to Nonpeptide lntegrin Antagonists

1998 • 27 citations

Synthesis and Biological Evaluation of Integrin Antagonists Containingtrans- andcis-2,5-Disubstituted THF Rings

2000 • 27 citations

Combinatorial chemistry techniques applied to nonpeptide integrin antagonists.

1998 • 27 citations

αvβ3 Integrin Binding Affinity and Specificity of SM256 in Various Species

1999 • 25 citations

Antibody to beta3 integrin inhibits osteoclast-mediated bone resorption in the thyroparathyroidectomized rat

1996 • 25 citations

Chapter 10. GPIIb/IIIa Antagonists

1996 • 25 citations

Arterial Wall Neovascularization

1997 • 24 citations

Benzimidazole derivatives as arginine mimetics in 1,4-benzodiazepine nonpeptide vitronectin receptor (αvβ3) antagonists

1998 • 24 citations

Construction of a family of biphenyl combinatorial libraries: Structure-activity studies utilizing libraries of mixtures

1998 • 23 citations

Discovery of an imidazopyridine-containing 1,4-benzodiazepine nonpeptide vitronectin receptor (αvβ3) antagonist with efficacy in a restenosis model

1998 • 21 citations

Sugar amino acids and carbohydrates as scaffolds and peptidomimetics

1999 • 21 citations

Synthesis and biological evaluation of dianhydrohexitol integrin antagonists

1999 • 17 citations

Integrins as novel drug discovery targets: potential therapeutic and diagnostic implications

2000 • 14 citations

Section Review: Cardiovascular & Renal: Glycoprotein IIb/IIIa antagonists

1996 • 11 citations

Anti-integrins as a potential therapeutic target in angiogenesis

1999 • 11 citations

Liquid phase parallel synthesis of iminodiacetic acid derivatives

1999 • 8 citations

Synthetic V 3 Antagonists Inhibit Insulin-Like Growth Factor-I-Stimulated Smooth Muscle Cell Migration and Replication

1999 • 5 citations

Integrins and Angiogenesis

1999 • 2 citations

Inhibition of neointima formation by a nonpeptide ?v?3 integrin receptor antagonist in a rabbit cuff model

2000 • 2 citations

ChemInform Abstract: Sugar Amino Acids and Carbohydrates as Scaffolds and Peptidomimetics

2000 • 2 citations