The following articles (labelled with PubMed ID or TBD) are for your review
| PMID | Data | Article Title | Organization |
|---|
| 27997164 |
18 |
Synthesis of Novel c(AmpRGD)-Sunitinib Dual Conjugates as Molecular Tools Targeting thea |
Universit£ |
| 27774126 |
95 |
Exploring |
University of California San Francisco |
| 26753814 |
7 |
Cyclic RGD peptidomimetics containing 4- and 5-amino-cyclopropane pipecolic acid (CPA) templates as dualaVß3 anda5ß1 integrin ligands. |
University of Florence |
| 24949551 |
22 |
Rational improvement of the affinity and selectivity of integrin binding of grafted lasso peptides. |
Philipps-Universit£T Marburg |
| 24973662 |
8 |
Targeting integrinsavß3 anda5ß1 with newß-lactam derivatives. |
University of Bologna |
| 24654918 |
19 |
Pharmacophoric modifications lead to superpotentavß3 integrin ligands with suppresseda5ß1 activity. |
Technische Universit£T M£Nchen |
| 9873531 |
3 |
Novel inhibitors of alpha 4 beta 1 integrin receptor interactions through library synthesis and screening. |
University of California |
| 24412498 |
15 |
Synthesis and assay of retro-a4ß1 integrin-targeting motifs. |
University of Bologna |
| 24900800 |
46 |
Small Macrocycles As Highly Active Integrin?2?1 Antagonists. |
Sanofi R & D |
| 24095096 |
3 |
Synthesis and in vitro evaluation of a novel radioligand foravß3 integrin receptor imaging: [18F]FPPA-c(RGDfK). |
University Hospital of Geneva |
| 23811088 |
26 |
Modulation ofavß3- anda5ß1-integrin-mediated adhesion by dehydro-ß-amino acids containing peptidomimetics. |
University of Bologna |
| 23777782 |
107 |
Orally available and efficaciousa4ß1/a4ß7 integrin inhibitors. |
Elan Pharmaceuticals |
| 23312947 |
22 |
Synthesis and evaluation of 4,5-dihydro-5-methylisoxazolin-5-carboxamide derivatives as VLA-4 antagonists. |
Ranbaxy Research Laboratories |
| 23562062 |
4 |
Arylsulfonamide pyrimidines as VLA-4 antagonists. |
Elan Pharmaceuticals |
| 23362923 |
59 |
Biselectivity of isoDGR peptides for fibronectin binding integrin subtypesa5ß1 andavß6: conformational control through flanking amino acids. |
Technische Universit£T M£Nchen |
| 23312474 |
36 |
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 |
| 23312471 |
31 |
Identification of N-acyl 4-(3-pyridonyl)phenylalanine derivatives and their orally active prodrug esters as dual actinga4ß1 anda4ß7 receptor antagonists. |
Hoffmann-La Roche |
| 23218775 |
38 |
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 |
| 22261021 |
33 |
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 |
| 22101134 |
9 |
LDV peptidomimetics equipped with biotinylated spacer-arms: synthesis and biological evaluation on CCRF-CEM cell line. |
Universit£ |
| 21889349 |
20 |
Modeling the molecular basis fora4ß1 integrin antagonism. |
Ian Wark Laboratories |
| 16767086 |
2 |
Combinatorial chemistry identifies high-affinity peptidomimetics against alpha4beta1 integrin for in vivo tumor imaging. |
University of California |
| 19959360 |
50 |
SAR of N-phenyl piperidine based oral integrin alpha5beta1 antagonists. |
Jerini |
| 19910191 |
46 |
Discovery of orally available integrin alpha5beta1 antagonists. |
Jerini |
| 19713111 |
31 |
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 |
| 19891440 |
57 |
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 |
| 16039122 |
9 |
Influence of acid surrogates toward potency of VLA-4 antagonist. |
Merck Research Laboratories |
| 15582407 |
20 |
Identified a morpholinyl-4-piperidinylacetic acid derivative as a potent oral active VLA-4 antagonist. |
Daiichi Pharmaceutical |
| 15582442 |
36 |
2,3-Diphenylpropionic acids as potent VLA-4 antagonists. |
Kaken Pharmaceutical |
| 12086484 |
13 |
Identification of potent and novel alpha4beta1 antagonists using in silico screening. |
Biogen |
| 9341911 |
133 |
Potent alpha 4 beta 1 peptide antagonists as potential anti-inflammatory agents. |
Genentech |
| 12617895 |
30 |
Dehydrophenylalanine derivatives as VLA-4 integrin antagonists. |
Celltech R&D |
| 14552799 |
14 |
Sulphonamide-based small molecule VLA-4 antagonists. |
Molecumetics |
| 12749892 |
42 |
N-isonicotinoyl-(L)-4-aminophenylalanine derivatives as tight binding VLA-4 antagonists. |
Merck Research Laboratories |
| 11858990 |
20 |
N-aryl 2,6-dimethoxybiphenylalanine analogues as VLA-4 antagonists. |
Merck Research Laboratories |
| 11844701 |
5 |
Identification of unique VLA-4 antagonists from a combinatorial library. |
Merck Research Laboratories |
| 11755339 |
33 |
N-acyl-L-phenylalanine derivatives as potent VLA-4 antagonists that mimic a cyclic peptide conformation. |
Hoffmann-La Roche |
| 12161162 |
69 |
N-Aroyl-L-phenylalanine derivatives as VCAM/VLA-4 antagonists. |
Hoffmann-La Roche |
| 12039570 |
51 |
N-(pyrimidin-4-yl) and N-(pyridin-2-yl) phenylalanine derivatives as VLA-4 integrin antagonists. |
Celltech R&D |
| 12039569 |
36 |
Discovery and evaluation of N-(triazin-1,3,5-yl) phenylalanine derivatives as VLA-4 integrin antagonists. |
Celltech R&D |
| 12031328 |
21 |
N-Tetrahydrofuroyl-(L)-phenylalanine derivatives as potent VLA-4 antagonists. |
Merck Research Laboratories |
| 11551757 |
29 |
Isoxazolyl, oxazolyl, and thiazolylpropionic acid derivatives as potent alpha(4)beta(1) integrin antagonists. |
Pfizer |
| 11140722 |
24 |
Imide and lactam derivatives of N-benzylpyroglutamyl-L-phenylalanine as VCAM/VLA-4 antagonists. |
Hoffmann-La Roche |
| 10853676 |
13 |
Discovery and evaluation of potent, cysteine-based alpha4beta1 integrin antagonists. |
Celltech Chiroscience |
| 10782674 |
50 |
N-benzylpyroglutamyl-L-phenylalanine derivatives as VCAM/VLA-4 antagonists. |
Hoffmann-La Roche |
| 21316228 |
28 |
Discovery of a potent, orally bioavailable pyrimidine VLA-4 antagonist effective in a sheep asthma model. |
Elan Pharmaceuticals |
| 7650686 |
3 |
Non-peptide fibrinogen receptor antagonists. 7. Design and synthesis of a potent, orally active fibrinogen receptor antagonist. |
Merck Research Laboratories |
| 22575869 |
61 |
Structure-activity relationship of a series of non peptidic RGD integrin antagonists targetinga5ß1: part 1. |
Astrazeneca |
| 22572578 |
124 |
Structure-activity relationship of a series of non peptidic RGD integrin antagonists targetinga5ß1: part 2. |
Astrazeneca |
| 20055426 |
30 |
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 |
| 18331794 |
20 |
Selective cell adhesion inhibitors: Barbituric acid based alpha4beta7--MAdCAM inhibitors. |
Millennium Pharmaceuticals |
| 18226905 |
60 |
Synthesis and SAR of pyridazinone-substituted phenylalanine amide alpha4 integrin antagonists. |
Johnson & Johnson Pharmaceutical Research & Development |
| 18303826 |
48 |
Discovery of subnanomolar arginine-glycine-aspartate-based alphaVbeta3/alphaVbeta5 integrin binders embedding 4-aminoproline residues. |
Universit£ |
| 15357991 |
20 |
Design, synthesis, and biochemical evaluation of novel alpha V beta 3 integrin ligands. |
3-Dimensional Pharmaceuticals |
| 12139455 |
78 |
Selective alpha4beta7 integrin antagonists and their potential as antiinflammatory agents. |
Genentech |
| 9191954 |
9 |
Non-peptide glycoprotein IIb/IIIa inhibitors. 17. Design and synthesis of orally active, long-acting non-peptide fibrinogen receptor antagonists. |
Merck Research Laboratories |
| 20172716 |
3 |
Ultrasmall particle of iron oxide--RGD peptidomimetic conjugate: synthesis and characterisation. |
Universit£ |
| 17973471 |
24 |
Multiple N-methylation by a designed approach enhances receptor selectivity. |
Technische UniversitäT MüNchen |
| 17869121 |
32 |
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 |
| 17616113 |
63 |
Design and synthesis of a new class of selective integrin alpha5beta1 antagonists. |
Jerini |
| 17387018 |
74 |
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 |
| 17118652 |
15 |
Highly constrained bicyclic VLA-4 antagonists. |
Merck Research Laboratories |
| 16298127 |
80 |
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 |
| 15974570 |
30 |
Ligand binding analysis for human alpha5beta1 integrin: strategies for designing new alpha5beta1 integrin antagonists. |
Università |
| 15715463 |
16 |
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 |
| 15109641 |
4 |
Rational design and synthesis of novel heparan sulfate mimetic compounds as antiadhesive agents. |
Riken Discovery Research Institute |
| 15081035 |
24 |
Bioisosteric replacement of anilide with benzoxazole: potent and orally bioavailable antagonists of VLA-4. |
Merck Research Laboratories |
| 15006384 |
179 |
Synthesis of cinnamic acids and related isosteres as potent and selective alpha v beta 3 receptor antagonists. |
Pfizer |
| 14741263 |
67 |
Solid-phase synthesis of a small library of 3-phenylthio-3-nicotinyl propionic acid derivatives acting as antagonists of the integrin alphaVbeta3. |
Nerviano |
| 14741249 |
21 |
Aza-bicyclic amino acid sulfonamides as alpha(4)beta(1)/alpha(4)beta(7) integrin antagonists. |
Johnson & Johnson Pharmaceutical Research & Development |
| 14698164 |
39 |
Synthesis and biological evaluation of nonpeptide integrin antagonists containing spirocyclic scaffolds. |
Pharmaceutical Research Institute |
| 14667228 |
3 |
Synthesis and structure-activity relationship of mannose-based peptidomimetics selectively blocking integrin alpha4beta7 binding to mucosal addressin cell adhesion molecule-1. |
Technische UniversitäT MüNchen |
| 12852971 |
8 |
Improvement of biological activity and proteolytic stability of peptides by coupling with a cyclic peptide. |
Kyowa Hakko Kogyo |
| 12699755 |
4 |
Nonpeptide RGD antagonists: a novel class of mimetics, the 5,8-disubstituted 1-azabicyclo[5.2.0]nonan-2-one lactam. |
University of Montpellier |
| 12617914 |
116 |
N-(3-phenylsulfonyl-3-piperidinoyl)-phenylalanine derivatives as potent, selective VLA-4 antagonists. |
Merck Research Laboratories |
| 12565960 |
33 |
Thiophene-based vitronectin receptor antagonists. |
Shire Biochem |
| 12270174 |
34 |
Solid-phase synthesis of dual alpha4beta1/alpha4beta7 integrin antagonists: two scaffolds with overlapping pharmacophores. |
Genentech |
| 12161161 |
94 |
N-Cycloalkanoyl-L-phenylalanine derivatives as VCAM/VLA-4 antagonists. |
Roche Research Center |
| 12127538 |
26 |
N-aryl-prolyl-dipeptides as potent antagonists of VLA-4. |
Merck Research Laboratories |
| 12039589 |
6 |
Focused library approach for identification of new N-acylphenylalanines as VCAM/VLA-4 antagonists. |
Roche Research Center |
| 12031329 |
110 |
Substituted tetrahydrofuroyl-1-phenylalanine derivatives as potent and specific VLA-4 antagonists. |
Merck Research Laboratories |
| 11909715 |
73 |
Squaric acid derivatives as VLA-4 integrin antagonists. |
Celltech R&D |
| 11844689 |
51 |
Substituted N-(3,5-dichlorobenzenesulfonyl)-L-prolyl-phenylalanine analogues as potent VLA-4 antagonists. |
Merck Research Laboratories |
| 11844683 |
31 |
The discovery of acylated beta-amino acids as potent and orally bioavailable VLA-4 antagonists. |
Merck Research Laboratories |
| 11755344 |
47 |
The discovery of small molecule carbamates as potent dual alpha(4)beta(1)/alpha(4)beta(7) integrin antagonists. |
Merck Research Laboratories |
| 11755338 |
24 |
Specific and dual antagonists of alpha(4)beta(1) and alpha(4)beta(7) integrins. |
Merck Research Laboratories |
| 11714601 |
9 |
Discovery and evaluation of piperidinyl carboxylic acid derivatives as potent alpha(4)beta(1) integrin antagonists. |
Bayer |
| 11677134 |
42 |
Design and synthesis of potent and selective inhibitors of integrin VLA-4. |
Novartis Institute For Biomedical Research |
| 11591507 |
79 |
The discovery of sulfonylated dipeptides as potent VLA-4 antagonists. |
Merck Research Laboratories |
| 32094009 |
36 |
Novel cilengitide-based cyclic RGD peptides as ?v? |
Division of Organic Chemistry Csir-National Chemical Laboratory (Ncl) |
| 11327582 |
23 |
2-Acylimino-3H-thiazoline derivatives: a novel template for platelet GPIIb/IIIa receptor antagonists. |
Taisho Pharmaceutical |
| 31999923 |
16 |
Insights into Protein-Ligand Interactions in Integrin Complexes: Advances in Structure Determinations. |
Pliant Therapeutics |
| 31266686 |
7 |
Small-molecule agents for the treatment of inflammatory bowel disease. |
Gilead Sciences |
| 10853677 |
34 |
Discovery and evaluation of potent, tyrosine-based alpha4beta1 integrin antagonists. |
Celltech Chiroscience |
| 10782673 |
6 |
N-acyl phenylalanine analogues as potent small molecule VLA-4 antagonists. |
Roche Research Center |
| 30657681 |
262 |
Selective Targeting of Integrin ?v?8 by a Highly Active Cyclic Peptide. |
Technische Universit£T M£Nchen |
| 10406646 |
15 |
Orally bioavailable nonpeptide vitronectin receptor antagonists with efficacy in an osteoporosis model. |
Smithkline Beecham Pharmaceuticals |
| 10197962 |
13 |
Orally active isoxazoline glycoprotein IIb/IIIa antagonists with extended duration of action. |
Dupont Pharmaceuticals |
| 10072689 |
39 |
Selective, tight-binding inhibitors of integrin alpha4beta1 that inhibit allergic airway responses. |
Biogen |
| 31381331 |
70 |
Profile of a Highly Selective Quaternized Pyrrolidine Betaine ? |
Glaxosmithkline Medicines Research Centre |
| 31306009 |
64 |
Cyclization of RGD Peptides by Suzuki-Miyaura Cross-Coupling. |
Bielefeld University |
| 31670514 |
45 |
Could Dissecting the Molecular Framework of ?-Lactam Integrin Ligands Enhance Selectivity? |
University of Bologna |
| 9016328 |
19 |
Discovery of potent isoxazoline glycoprotein IIb/IIIa receptor antagonists. |
Dupont Pharmaceuticals |
| 26101577 |
15 |
Dehydro-?-proline Containing ?4?1 Integrin Antagonists: Stereochemical Recognition in Ligand-Receptor Interplay. |
University of Bologna |
| 24568695 |
76 |
Strategies to inhibit tumor associated integrin receptors: rationale for dual and multi-antagonists. |
University of Bradford |
| 8057299 |
66 |
Non-peptide fibrinogen receptor antagonists. 2. Optimization of a tyrosine template as a mimic for Arg-Gly-Asp. |
Merck Research Laboratories |
| 7507165 |
139 |
Design and synthesis of novel cyclic RGD-containing peptides as highly potent and selective integrin alpha IIb beta 3 antagonists. |
Telios Pharmaceuticals |
| 30215258 |
228 |
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 |
| 29775303 |
60 |
Simultaneous Targeting of RGD-Integrins and Dual Murine Double Minute Proteins in Glioblastoma Multiforme. |
Universit£ |
| 28135089 |
9 |
Emergence of Small-Molecule Non-RGD-Mimetic Inhibitors for RGD Integrins. |
University of Strathclyde |
| 1469694 |
22 |
Non-peptide fibrinogen receptor antagonists. 1. Discovery and design of exosite inhibitors. |
Merck Research Laboratories |
| 17948981 |
10 |
Highly Potent, Water Soluble Benzimidazole Antagonist for Activated alpha(4)beta(1) Integrin. |
University of California Davis |
| 17915848 |
48 |
Small molecule inhibitors of integrin alpha2beta1. |
University of Pennsylvania |
| 16377201 |
24 |
Synthesis, biological evaluation, and pharmacokinetic study of prolyl-1-piperazinylacetic acid and prolyl-4-piperidinylacetic acid derivatives as VLA-4 antagonists. |
Daiichi Pharmaceutical |
| 17194595 |
18 |
Synthesis and biological evaluation of benzoic acid derivatives as potent, orally active VLA-4 antagonists. |
Daiichi Pharmaceutical |
| 16495061 |
8 |
Selection of a 2-azabicyclo[2.2.2]octane-based alpha4beta1 integrin antagonist as an inhaled anti-asthmatic agent. |
Johnson & Johnson Pharmaceutical |
| 17035017 |
25 |
2,6-Quinolinyl derivatives as potent VLA-4 antagonists. |
Ucb Pharma |
| 16455247 |
15 |
Pyridone derivatives as potent and selective VLA-4 integrin antagonists. |
Glaxosmithkline |
| 16931004 |
29 |
Pyridone derivatives as potent, orally bioavailable VLA-4 integrin antagonists. |
Glaxosmithkline |
| 17041919 |
51 |
Structure-activity relationship studies of a series of peptidomimetic ligands for alpha(4) beta(1) integrin on Jurkat T-leukemia cells. |
University of California Davis |
| 16112583 |
74 |
Aza-bicyclic amino acid carboxamides as alpha4beta1/alpha4beta7 integrin receptor antagonists. |
Johnson & Johnson Pharmaceutical |
| 16722660 |
60 |
Synthesis and biological evaluation of novel pyridazinone-based alpha4 integrin receptor antagonists. |
Johnson & Johnson Pharmaceutical |
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