165 articles for thisTarget
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Synthesis of Novel c(AmpRGD)-Sunitinib Dual Conjugates as Molecular Tools Targeting thea
University of Parma
Cyclic RGD peptidomimetics containing 4- and 5-amino-cyclopropane pipecolic acid (CPA) templates as dualaVß3 anda5ß1 integrin ligands.
University of Florence
Rational improvement of the affinity and selectivity of integrin binding of grafted lasso peptides.
Philipps-Universit£T Marburg
Pharmacophoric modifications lead to superpotentavß3 integrin ligands with suppresseda5ß1 activity.
Technische Universit£T M£Nchen
Synthesis and in vitro evaluation of a novel radioligand foravß3 integrin receptor imaging: [18F]FPPA-c(RGDfK).
University Hospital of Geneva
Modulation ofavß3- anda5ß1-integrin-mediated adhesion by dehydro-ß-amino acids containing peptidomimetics.
University of Bologna
Towards dual antithrombotic compounds - balancing thrombin inhibitory and fibrinogen GPIIb/IIIa binding inhibitory activities of 2,3-dihydro-1,4-benzodioxine derivatives through regio- and stereoisomerism.
University of Ljubljana
Biselectivity of isoDGR peptides for fibronectin binding integrin subtypesa5ß1 andavß6: conformational control through flanking amino acids.
Technische Universit£T M£Nchen
One step radiosynthesis of 6-[(18)F]fluoronicotinic acid 2,3,5,6-tetrafluorophenyl ester ([(18)F]F-Py-TFP): a new prosthetic group for efficient labeling of biomolecules with fluorine-18.
University of Troms£
Tetrazine-trans-cyclooctene ligation for the rapid construction of integrinavß3 targeted PET tracer based on a cyclic RGD peptide.
University of Delaware
Exploring new near-infrared fluorescent disulfide-based cyclic RGD peptide analogs for potential integrin-targeted optical imaging.
Washington University
Synthesis and evaluation of bivalent, peptidomimetic antagonists of theavß3 integrins.
The Methodist Hospital Research Institute
Inhibition of cancer cell adhesion by heterochiral Pro-containing RGD mimetics.
University of Bologna
Discovery of small molecule inhibitors of integrin alphavbeta3 through structure-based virtual screening.
Chinese Academy of Medical Sciences and Peking Union Medical College
Discovery of small molecule integrin alphavbeta3 antagonists as novel anticancer agents.
University of Southern California
Novel and selective alpha(v)beta3 receptor peptide antagonist: design, synthesis, and biological behavior.
University of Naples Federico Ii
Design, synthesis, and evaluation of near infrared fluorescent multimeric RGD peptides for targeting tumors.
Washington University
Synthesis and biological evaluation of dimeric RGD peptide-paclitaxel conjugate as a model for integrin-targeted drug delivery.
University of Southern California
Nonpeptide alphavbeta3 antagonists. Part 11: discovery and preclinical evaluation of potent alphavbeta3 antagonists for the prevention and treatment of osteoporosis.
Merck Research Laboratories
Non-peptidic alpha(v)beta3 antagonists containing indol-1-yl propionic acids.
Johnson & Johnson Pharmaceutical Research and Development
Nonpeptide alpha V beta 3 antagonists. Part 9: Improved pharmacokinetic profile through the use of an aliphatic, des-amide backbone.
Merck Research Laboratories
Docking studies on alphavbeta3 integrin ligands: pharmacophore refinement and implications for drug design.
Technische Universit£T M£Nchen
Nonpeptide alpha(v)beta(3) antagonists. 1. Transformation of a potent, integrin-selective alpha(IIb)beta(3) antagonist into a potent alpha(v)beta(3) antagonist.
Merck Research Laboratories
Synthesis and solution conformation of cyclo[RGDRGD]: a cyclic peptide with selectivity for the alpha V beta 3 receptor.
Texas A&M University
Non-peptide fibrinogen receptor antagonists. 7. Design and synthesis of a potent, orally active fibrinogen receptor antagonist.
Merck Research Laboratories
Non-peptide alpha v beta 3 antagonists. Part 7: 3-Substituted tetrahydro-naphthyridine derivatives.
Merck Research Laboratories
Biphenyls as potent vitronectin receptor antagonists. Part 2: biphenylalanine ureas.
Bayer
Non-peptide alpha(v)beta(3) antagonists: identification of potent, chain-shortened RGD mimetics that incorporate a central pyrrolidinone constraint.
Merck Research Laboratories
Non-peptide alpha(v)beta(3) antagonists. Part 5: identification of potent RGD mimetics incorporating 2-aryl beta-amino acids as aspartic acid replacements.
Merck Research Laboratories
Non-peptide alpha(v)beta(3) antagonists. Part 4: potent and orally bioavailable chain-shortened RGD mimetics.
Merck Research Laboratories
Synthesis of highly potent and selective hetaryl ureas as integrin alpha(V)beta3-receptor antagonists.
Basf
Non-peptide alpha(v)beta(3) antagonists. Part 3: identification of potent RGD mimetics incorporating novel beta-amino acids as aspartic acid replacements.
Merck Research Laboratories
Nonpeptide alpha(v)beta(3) antagonists. Part 2: constrained glycyl amides derived from the RGD tripeptide.
Merck Research Laboratories
Discovery of an imidazopyridine-containing 1,4-benzodiazepine nonpeptide vitronectin receptor (alpha v beta 3) antagonist with efficacy in a restenosis model.
Smithkline Beecham Pharmaceuticals
Synthesis and biological evaluation (in vitro and in vivo) of cyclic arginine-glycine-aspartate (RGD) peptidomimetic-paclitaxel conjugates targeting integrinaVß3.
University of Milan
Camptothecins in tumor homing via an RGD sequence mimetic.
Sigma-Tau Industrie Farmaceutiche Riunite
Near-infrared fluorescent divalent RGD ligand for integrinavß3-targeted optical imaging.
Washington University
¹²5I-radiolabeled morpholine-containing arginine-glycine-aspartate (RGD) ligand ofavß3 integrin as a molecular imaging probe for angiogenesis.
University of Florence
Structure-activity relationship of a series of non peptidic RGD integrin antagonists targetinga5ß1: part 1.
Astrazeneca
Structure-activity relationship of a series of non peptidic RGD integrin antagonists targetinga5ß1: part 2.
Astrazeneca
Antiangiogenic effect of dual/selective alpha(5)beta(1)/alpha(v)beta(3) integrin antagonists designed on partially modified retro-inverso cyclotetrapeptide mimetics.
Universita Degli Studi Di Bologna
alphavbeta3 Integrin-targeting Arg-Gly-Asp (RGD) peptidomimetics containing oligoethylene glycol (OEG) spacers.
Universite Catholique De Louvain
Synthesis, SAR and in vitro evaluation of new cyclic Arg-Gly-Asp pseudopentapeptides containing a s-cis peptide bond as integrin alphavbeta3 and alphavbeta5 ligands.
Department of Organic Chemistry Ugo Schiff University of Firenze Via Della Lastruccia 13
Discovery of subnanomolar arginine-glycine-aspartate-based alphaVbeta3/alphaVbeta5 integrin binders embedding 4-aminoproline residues.
University of Parma
Design and synthesis of novel potent and selective integrin alphanubeta3 antagonists--novel synthetic routes to isoquinolinone, benzoxazinone, and quinazolinone acetates.
Basf
Identification of novel short chain 4-substituted indoles as potent alphavbeta3 antagonist using structure-based drug design.
Johnson & Johnson Pharmaceutical Research and Development
Grafting aminocyclopentane carboxylic acids onto the RGD tripeptide sequence generates low nanomolar alphaVbeta3/alphaVbeta5 integrin dual binders.
University of Parma
Design, synthesis, and biochemical evaluation of novel alpha V beta 3 integrin ligands.
3-Dimensional Pharmaceuticals
Selective alpha4beta7 integrin antagonists and their potential as antiinflammatory agents.
Genentech
Non-peptide glycoprotein IIb/IIIa inhibitors. 17. Design and synthesis of orally active, long-acting non-peptide fibrinogen receptor antagonists.
Merck Research Laboratories
RGD mimetics containing a central hydantoin scaffold: alpkha(v)beta3 vs alpha(IIb)beta3 selectivity requirements.
Hoechst Marion Roussel
Fluorinated dual antithrombotic compounds based on 1,4-benzoxazine scaffold.
University of Ljubljana
Improvement in aqueous solubility in small molecule drug discovery programs by disruption of molecular planarity and symmetry.
The University of Tokyo
Small molecule inhibitors of hantavirus infection.
University of New Mexico School of Medicine
Click-chemistry-derived triazole ligands of arginine-glycine-aspartate (RGD) integrins with a broad capacity to inhibit adhesion of melanoma cells and both in vitro and in vivo angiogenesis.
University of Florence
Novel tumor-targeted RGD peptide-camptothecin conjugates: synthesis and biological evaluation.
Istituto Di Ricerche Chimiche E Biochimiche G. Ronzoni
Morpholine-based RGD-cyclopentapeptides as alphavbeta3/alphavbeta5 integrin ligands: role of configuration towards receptor binding affinity.
Università
Dual integrin and gastrin-releasing peptide receptor targeted tumor imaging using 18F-labeled PEGylated RGD-bombesin heterodimer 18F-FB-PEG3-Glu-RGD-BBN.
Stanford University School of Medicine
Synthesis and initial evaluation of novel, non-peptidic antagonists of the alpha(v)-integrins alpha(v)beta(3) and alpha(v)beta(5).
Pharmacopeia
Structure-function analysis of Arg-Gly-Asp helix motifs in alpha v beta 6 integrin ligands.
Cancer Research Uk Clinical Centre
Multiple N-methylation by a designed approach enhances receptor selectivity.
Technische UniversitäT MüNchen
Biphenyls as potent vitronectin receptor antagonists. Part 3: Squaric acid amides.
Bayer Healthcare
Synthesis and biological evaluation of non-peptide alpha(v)beta(3)/alpha(5)beta(1) integrin dual antagonists containing 5,6-dihydropyridin-2-one scaffolds.
Università
Design and synthesis of a new class of selective integrin alpha5beta1 antagonists.
Jerini
Discovery of +(2-{4-[2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethoxy]phenyl}-cyclopropyl)acetic acid as potent and selective alphavbeta3 inhibitor: design, synthesis, and optimization.
Pfizer
Halting the Spread of Herpes Simplex Virus-1: The Discovery of an Effective Dual ?v?6/?v?8 Integrin Ligand.
University of Naples Federico II
Synthesis of pyrazoles and isoxazoles as potent alpha(v)beta3 receptor antagonists.
Pfizer
Incorporation of the unusual C(alpha)-fluoroalkylamino acids into cyclopeptides: synthesis of arginine-glycine-aspartate (RGD) analogues and study of their conformational and biological behavior.
Istituto Di Ricerche Chimiche E Biochimiche G. Ronzoni
Synthesis of 2,5-thiazole butanoic acids as potent and selective alpha(v)beta3 integrin receptor antagonists with improved oral pharmacokinetic properties.
Pfizer
Convergent, parallel synthesis of a series of beta-substituted 1,2,4-oxadiazole butanoic acids as potent and selective alpha(v)beta3 receptor antagonists.
Pfizer
Ligand binding analysis for human alpha5beta1 integrin: strategies for designing new alpha5beta1 integrin antagonists.
Università
Nonpeptide alpha(v)beta3 antagonists: identification of potent, chain-shortened 7-oxo RGD mimetics.
Merck Research Laboratories
Design, synthesis, and biological evaluation of novel potent and selective alphavbeta3/alphavbeta5 integrin dual inhibitors with improved bioavailability. Selection of the molecular core.
Johnson and Johnson Pharmaceutical Research & Development
Sortase A-mediated cyclization of novel polycyclic RGD peptides for ?
Hefei Normal University
1,2,3,4-Tetrahydroquinoline-containing alphaVbeta3 integrin antagonists with enhanced oral bioavailability.
Johnson & Johnson Pharmaceutical Research & Development
Integrin-Mediated Targeted Cancer Therapy Using c(RGDyK)-Based Conjugates of Gemcitabine.
Aristotle University of Thessaloniki
Piperidine-containing beta-arylpropionic acids as potent antagonists of alphavbeta3/alphavbeta5 integrins.
Johnson & Johnson Pharmaceutical Research and Development
Discovery of a potent and selective alpha v beta 3 integrin antagonist with strong inhibitory activity against neointima formation in rat balloon injury model.
Dainippon Pharmaceutical
Discovery of novel 2,8-diazaspiro[4.5]decanes as orally active glycoprotein IIb-IIIa antagonists.
Millennium Pharmaceuticals
Synthesis of cinnamic acids and related isosteres as potent and selective alpha v beta 3 receptor antagonists.
Pfizer
Solid-phase synthesis of a small library of 3-phenylthio-3-nicotinyl propionic acid derivatives acting as antagonists of the integrin alphaVbeta3.
Nerviano
Synthesis and biological evaluation of nonpeptide integrin antagonists containing spirocyclic scaffolds.
Pharmaceutical Research Institute
Nonpeptide alphavbeta3 antagonists. 8. In vitro and in vivo evaluation of a potent alphavbeta3 antagonist for the prevention and treatment of osteoporosis.
Merck Research Laboratories
Design, synthesis, and biological evaluation of novel bifunctional thyrointegrin antagonists for neuroblastoma.
Pharmaceutical Research Institute
Tuning the Biological Activity of RGD Peptides with Halotryptophans?.
Bielefeld University
Non-peptide alphavbeta3 antagonists. Part 6: design and synthesis of alphavbeta3 antagonists containing a pyridone or pyrazinone central scaffold.
Merck Research Laboratories
Phenylbutyrates as potent, orally bioavailable vitronectin receptor (integrin alphavbeta3) antagonists.
Glaxosmithkline
Solid-phase synthesis of cyclic RGD-furanoid sugar amino acid peptides as integrin inhibitors.
Leiden University
Highly potent and selective alphaVbeta3-receptor antagonists: solid-phase synthesis and SAR of 1-substituted 4-amino-1H-pyrimidin-2-ones.
Basf
Binding model for nonpeptide antagonists of alpha(v)beta(3) integrin.
Merck Research Laboratories
Substituted benzocyloheptenes as potent and selective alpha(v) integrin antagonists.
Institut De Recherches Servier
Dual antagonists of ?5?1/?v?1 integrin for airway hyperresponsiveness.
University of California San Francisco
Nanomolar small molecule inhibitors for alphav(beta)6, alphav(beta)5, and alphav(beta)3 integrins.
Merck
New ?-Lactam Derivatives Modulate Cell Adhesion and Signaling Mediated by RGD-Binding and Leukocyte Integrins.
University of Bologna
Synthesis and SAR of N-substituted dibenzazepinone derivatives as novel potent and selective alpha(V)beta(3) antagonists.
Knoll
Discovery and evaluation of piperidinyl carboxylic acid derivatives as potent alpha(4)beta(1) integrin antagonists.
Bayer
Novel cilengitide-based cyclic RGD peptides as ?v?
Division of Organic Chemistry Csir-National Chemical Laboratory (Ncl)
alpha(v)beta(3) Antagonists based on a central thiophene scaffold.
Aventis Pharma Deutschland
Spirocyclic nonpeptide glycoprotein IIb-IIIa antagonists. Part 1: design of potent and specific 3,9-diazaspiro[5.5]undecanes.
Cor Therapeutics
Solid-phase synthesis of a nonpeptide RGD mimetic library: new selective alphavbeta3 integrin antagonists.
Technische UniversitäT MüNchen
2-Acylimino-3H-thiazoline derivatives: a novel template for platelet GPIIb/IIIa receptor antagonists.
Taisho Pharmaceutical
Dual Targeting of Norepinephrine Transporter (NET) Function and Thyrointegrin ?v?3 Receptors in the Treatment of Neuroblastoma.
Albany College of Pharmacy and Health Sciences
Insights into Protein-Ligand Interactions in Integrin Complexes: Advances in Structure Determinations.
Pliant Therapeutics
Discovery and evaluation of potent, tyrosine-based alpha4beta1 integrin antagonists.
Celltech Chiroscience
Selective Targeting of Integrin ?v?8 by a Highly Active Cyclic Peptide.
Technische Universit£T M£Nchen
Disubstituted indazoles as potent antagonists of the integrin alpha(v)beta(3).
Dupont Pharmaceuticals
Isoxazolines as potent antagonists of the integrin alpha(v)beta(3).
Dupont Pharmaceuticals
Discovery of orally active nonpeptide vitronectin receptor antagonists based on a 2-benzazepine Gly-Asp mimetic.
Smithkline Beecham Pharmaceuticals
N-Methylated cyclic RGD peptides as highly active and selective alpha(V)beta(3) integrin antagonists.
Technische UniversitäT MüNchen
Orally bioavailable nonpeptide vitronectin receptor antagonists with efficacy in an osteoporosis model.
Smithkline Beecham Pharmaceuticals
Orally bioavailable nonpeptide vitronectin receptor antagonists containing 2-aminopyridine arginine mimetics.
Smithkline Beecham Pharmaceuticals
Rapid synthesis of RGD mimetics with isoxazoline scaffolds on solid phase: identification of alphavbeta3 antagonists lead compounds.
Dupont Pharmaceuticals
Orally active isoxazoline glycoprotein IIb/IIIa antagonists with extended duration of action.
Dupont Pharmaceuticals
Profile of a Highly Selective Quaternized Pyrrolidine Betaine ?
Glaxosmithkline Medicines Research Centre
Benzimidazole derivatives as arginine mimetics in 1,4-benzodiazepine nonpeptide vitronectin receptor (alpha v beta 3) antagonists.
Smithkline Beecham Pharmaceuticals
Discovery of an Orally Bioavailable Pan ?v Integrin Inhibitor for Idiopathic Pulmonary Fibrosis.
Glaxosmithkline Medicines Research Centre
Fibrinogen receptor (GPIIb-IIIa) antagonists derived from 5,6-bicyclic templates. Amidinoindoles, amidinoindazoles, and amidinobenzofurans containing the N-alpha-sulfonamide carboxylic acid function as potent platelet aggregation inhibitors.
Cor Therapeutics
Use of conformationally restricted benzamidines as arginine surrogates in the design of platelet GPIIb-IIIa receptor antagonists.
Eli Lilly
Discovery of potent nonpeptide vitronectin receptor (alpha v beta 3) antagonists.
Smithkline Beecham Pharmaceuticals
Could Dissecting the Molecular Framework of ?-Lactam Integrin Ligands Enhance Selectivity?
University of Bologna
Insight to the binding mode of triazole RGD-peptidomimetics to integrin-rich cancer cells by NMR and molecular modeling.
University of Milano
Dehydro-?-proline Containing ?4?1 Integrin Antagonists: Stereochemical Recognition in Ligand-Receptor Interplay.
University of Bologna
In silico studies, synthesis and binding evaluation of substituted 2-pyrrolidinones as peptidomimetics of RGD tripeptide sequence.
Paris Descartes University
Strategies to inhibit tumor associated integrin receptors: rationale for dual and multi-antagonists.
University of Bradford
Structure Activity Relationships of ?v Integrin Antagonists for Pulmonary Fibrosis by Variation in Aryl Substituents.
University of Nottingham
Non-peptide fibrinogen receptor antagonists. 2. Optimization of a tyrosine template as a mimic for Arg-Gly-Asp.
Merck Research Laboratories
Design and synthesis of novel cyclic RGD-containing peptides as highly potent and selective integrin alpha IIb beta 3 antagonists.
Telios Pharmaceuticals
Natural inhibitors targeting osteoclast-mediated bone resorption.
Chinese Academy of Sciences
Discovery of ( S)-3-(3-(3,5-Dimethyl-1 H-pyrazol-1-yl)phenyl)-4-(( R)-3-(2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl)pyrrolidin-1-yl)butanoic Acid, a Nonpeptidic ?
University of Strathclyde
Succinimide-Based Conjugates Improve IsoDGR Cyclopeptide Affinity to ?
Irccs Ospedale San Raffaele
Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme.
University of Naples Federico II
Synthesis of a Chloroalkene Dipeptide Isostere-Containing Peptidomimetic and Its Biological Application.
Tokyo Medical and Dental University
Non-peptide fibrinogen receptor antagonists. 1. Discovery and design of exosite inhibitors.
Merck Research Laboratories
METHOD FOR TREATING GRAFT VERSUS HOST DISEASE CAUSED BY HEMATOPOIETIC STEM CELL TRANSPLANTATION
Beijing Tide Pharmaceutical
Matrix metalloproteinase (MMP) inhibitors and methods of use thereof
Foresee Pharmaceuticals
Heterocycle compounds as Tyro3, Axl and MerTK (TAM) family of receptor tyrosine kinase inhibitors
Development Center For Biotechnology
Heterocyclic compounds useful as aurora a selective inhibitors
Jacobio Pharmaceuticals
Pyrazolo[1,5-A][1,3,5]triazine and pyrazolo[1,5-A]pyrimidine derivatives as CDK inhibitors
Aurigene Discovery Technologies
Substituted-3H-imidazo [4,5-c] pyridine and 1H-pyrrolo[2,3-c]pyridine series of novel ectonucleotide pyrophosphatase/phosphodiesterase-1 (ENPP1) and stimulator for interferon genes (STING) modulators as cancer immunotherapeutics
Stingray Therapeutics