98 articles for thisTarget
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Article Title
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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
Novel inhibitors of alpha 4 beta 1 integrin receptor interactions through library synthesis and screening.
University Of California
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
Synthesis and evaluation of 4,5-dihydro-5-methylisoxazolin-5-carboxamide derivatives as VLA-4 antagonists.
Ranbaxy Research Laboratories
Biselectivity of isoDGR peptides for fibronectin binding integrin subtypesa5ß1 andavß6: conformational control through flanking amino acids.
Technische Universit£T M£Nchen
Identification of N-acyl 4-(5-pyrimidine-2,4-dionyl)phenylalanine derivatives and their orally active prodrug esters as dual-acting alpha4-beta1 and alpha4-beta7 receptor antagonists.
Hoffmann-La Roche
Identification of N-acyl 4-(3-pyridonyl)phenylalanine derivatives and their orally active prodrug esters as dual actinga4ß1 anda4ß7 receptor antagonists.
Hoffmann-La Roche
A novel, potent, and orally active VLA-4 antagonist with good aqueous solubility: trans-4-[1-[[2-(5-Fluoro-2-methylphenylamino)-7-fluoro-6-benzoxazolyl]acetyl]-(5S)-[methoxy(methyl)amino]methyl-(2S)-pyrrolidinylmethoxy]cyclohexanecarboxylic acid.
Daiichi Sankyo
Identification of trans-4-[1-[[7-fluoro-2-(1-methyl-3-indolyl)-6-benzoxazolyl]acetyl]-(4S)-fluoro-(2S)-pyrrolidinylmethoxy]cyclohexanecarboxylic acid as a potent, orally active VLA-4 antagonist.
Daiichi Sankyo
LDV peptidomimetics equipped with biotinylated spacer-arms: synthesis and biological evaluation on CCRF-CEM cell line.
Universit£
Combinatorial chemistry identifies high-affinity peptidomimetics against alpha4beta1 integrin for in vivo tumor imaging.
University Of California
Discovery of N-{N-[(3-cyanobenzene) sulfonyl]-4(R)-(3,3-difluoropiperidin-1-yl)-(l)-prolyl}-4-[(3',5'-dichloro-isonicotinoyl) amino]-(l)-phenylalanine (MK-0617), a highly potent and orally active VLA-4 antagonist.
Merck Research Laboratories
Discovery of trans-4-[1-[[2,5-Dichloro-4-(1-methyl-3-indolylcarboxamido)phenyl]acetyl]-(4S)-methoxy-(2S)-pyrrolidinylmethoxy]cyclohexanecarboxylic acid: an orally active, selective very late antigen-4 antagonist.
Daiichi Sankyo
Influence of acid surrogates toward potency of VLA-4 antagonist.
Merck Research Laboratories
Identified a morpholinyl-4-piperidinylacetic acid derivative as a potent oral active VLA-4 antagonist.
Daiichi Pharmaceutical
Identification of potent and novel alpha4beta1 antagonists using in silico screening.
Biogen
Potent alpha 4 beta 1 peptide antagonists as potential anti-inflammatory agents.
Genentech
N-isonicotinoyl-(L)-4-aminophenylalanine derivatives as tight binding VLA-4 antagonists.
Merck Research Laboratories
N-aryl 2,6-dimethoxybiphenylalanine analogues as VLA-4 antagonists.
Merck Research Laboratories
Identification of unique VLA-4 antagonists from a combinatorial library.
Merck Research Laboratories
N-acyl-L-phenylalanine derivatives as potent VLA-4 antagonists that mimic a cyclic peptide conformation.
Hoffmann-La Roche
N-(pyrimidin-4-yl) and N-(pyridin-2-yl) phenylalanine derivatives as VLA-4 integrin antagonists.
Celltech R&D
Discovery and evaluation of N-(triazin-1,3,5-yl) phenylalanine derivatives as VLA-4 integrin antagonists.
Celltech R&D
N-Tetrahydrofuroyl-(L)-phenylalanine derivatives as potent VLA-4 antagonists.
Merck Research Laboratories
Isoxazolyl, oxazolyl, and thiazolylpropionic acid derivatives as potent alpha(4)beta(1) integrin antagonists.
Pfizer
Imide and lactam derivatives of N-benzylpyroglutamyl-L-phenylalanine as VCAM/VLA-4 antagonists.
Hoffmann-La Roche
Discovery and evaluation of potent, cysteine-based alpha4beta1 integrin antagonists.
Celltech Chiroscience
N-benzylpyroglutamyl-L-phenylalanine derivatives as VCAM/VLA-4 antagonists.
Hoffmann-La Roche
Discovery of a potent, orally bioavailable pyrimidine VLA-4 antagonist effective in a sheep asthma model.
Elan Pharmaceuticals
Non-peptide fibrinogen receptor antagonists. 7. Design and synthesis of a potent, orally active fibrinogen receptor antagonist.
Merck Research Laboratories
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
Selective cell adhesion inhibitors: Barbituric acid based alpha4beta7--MAdCAM inhibitors.
Millennium Pharmaceuticals
Synthesis and SAR of pyridazinone-substituted phenylalanine amide alpha4 integrin antagonists.
Johnson & Johnson Pharmaceutical Research & Development
Discovery of subnanomolar arginine-glycine-aspartate-based alphaVbeta3/alphaVbeta5 integrin binders embedding 4-aminoproline residues.
Universit£
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
Ultrasmall particle of iron oxide--RGD peptidomimetic conjugate: synthesis and characterisation.
Universit£
Multiple N-methylation by a designed approach enhances receptor selectivity.
Technische UniversitäT MüNchen
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
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
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
Rational design and synthesis of novel heparan sulfate mimetic compounds as antiadhesive agents.
Riken Discovery Research Institute
Bioisosteric replacement of anilide with benzoxazole: potent and orally bioavailable antagonists of VLA-4.
Merck Research Laboratories
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
Aza-bicyclic amino acid sulfonamides as alpha(4)beta(1)/alpha(4)beta(7) integrin antagonists.
Johnson & Johnson Pharmaceutical Research & Development
Synthesis and biological evaluation of nonpeptide integrin antagonists containing spirocyclic scaffolds.
Pharmaceutical Research Institute
Synthesis and structure-activity relationship of mannose-based peptidomimetics selectively blocking integrin alpha4beta7 binding to mucosal addressin cell adhesion molecule-1.
Technische UniversitäT MüNchen
Improvement of biological activity and proteolytic stability of peptides by coupling with a cyclic peptide.
Kyowa Hakko Kogyo
Nonpeptide RGD antagonists: a novel class of mimetics, the 5,8-disubstituted 1-azabicyclo[5.2.0]nonan-2-one lactam.
University Of Montpellier
N-(3-phenylsulfonyl-3-piperidinoyl)-phenylalanine derivatives as potent, selective VLA-4 antagonists.
Merck Research Laboratories
Solid-phase synthesis of dual alpha4beta1/alpha4beta7 integrin antagonists: two scaffolds with overlapping pharmacophores.
Genentech
N-Cycloalkanoyl-L-phenylalanine derivatives as VCAM/VLA-4 antagonists.
Roche Research Center
Focused library approach for identification of new N-acylphenylalanines as VCAM/VLA-4 antagonists.
Roche Research Center
Substituted tetrahydrofuroyl-1-phenylalanine derivatives as potent and specific VLA-4 antagonists.
Merck Research Laboratories
Substituted N-(3,5-dichlorobenzenesulfonyl)-L-prolyl-phenylalanine analogues as potent VLA-4 antagonists.
Merck Research Laboratories
The discovery of acylated beta-amino acids as potent and orally bioavailable VLA-4 antagonists.
Merck Research Laboratories
The discovery of small molecule carbamates as potent dual alpha(4)beta(1)/alpha(4)beta(7) integrin antagonists.
Merck Research Laboratories
Specific and dual antagonists of alpha(4)beta(1) and alpha(4)beta(7) integrins.
Merck Research Laboratories
Discovery and evaluation of piperidinyl carboxylic acid derivatives as potent alpha(4)beta(1) integrin antagonists.
Bayer
Design and synthesis of potent and selective inhibitors of integrin VLA-4.
Novartis Institute For Biomedical Research
The discovery of sulfonylated dipeptides as potent VLA-4 antagonists.
Merck Research Laboratories
2-Acylimino-3H-thiazoline derivatives: a novel template for platelet GPIIb/IIIa receptor antagonists.
Taisho Pharmaceutical
Discovery and evaluation of potent, tyrosine-based alpha4beta1 integrin antagonists.
Celltech Chiroscience
N-acyl phenylalanine analogues as potent small molecule VLA-4 antagonists.
Roche Research Center
Orally bioavailable nonpeptide vitronectin receptor antagonists with efficacy in an osteoporosis model.
Smithkline Beecham Pharmaceuticals
Orally active isoxazoline glycoprotein IIb/IIIa antagonists with extended duration of action.
Dupont Pharmaceuticals
Selective, tight-binding inhibitors of integrin alpha4beta1 that inhibit allergic airway responses.
Biogen
Discovery of potent isoxazoline glycoprotein IIb/IIIa receptor antagonists.
Dupont Pharmaceuticals
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