Design and synthesis of potent and selective α4β7 integrin antagonists

Journal of Medicinal Chemistry

Volumn 44, Issue 16, 2001, Pages 2586-2592

  Boer, J ^a   Gottschling, D ^a   Schuster, A ^b   Semmrich, M ^b   Holzmann, B ^a   Kessler, H ^b  

^a TECHNICAL UNIVERSITY OF MUNICH   (Germany)

^b TECHNICAL UNIVERSITY OF MUNICH   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

ADDRESSIN; ALPHA4 BETA7 INTEGRIN; CELL ADHESION MOLECULE; CYCLO(LEUCYLASPARTYLTHREONYLALANYL DEXTRO PROLYLALANINE); CYCLO(LEUCYLASPARTYLTHREONYLALANYL DEXTRO PROLYLPHENYLALANINE); CYCLO(LEUCYLASPARTYLTHREONYLASPARTYL DEXTRO PROLYLHISTIDINE); CYCLO(LEUCYLASPARTYLTHREONYLASPARTYL DEXTRO PROLYLPHENYLALANINE); CYCLO(LEUCYLASPARTYLTHREONYLASPARTYL DEXTRO PROLYLTYROSINE); CYCLOPEPTIDE; INTEGRIN; MUCOSAL ADDRESSIN CELL ADHESION MOLECULE 1; UNCLASSIFIED DRUG; VASCULAR CELL ADHESION MOLECULE 1;

ANIMAL CELL; ARTICLE; BINDING AFFINITY; CHRONIC INFLAMMATION; CONTROLLED STUDY; DIABETES MELLITUS; DRUG PROTEIN BINDING; ENTERITIS; IMMUNE RESPONSE; LYMPHOID ORGAN; NONHUMAN; SCREENING TEST;

ANIMALS; CELL ADHESION; CHO CELLS; COMBINATORIAL CHEMISTRY TECHNIQUES; CRICETINAE; DRUG DESIGN; HUMANS; IMMUNOGLOBULINS; INTEGRINS; JURKAT CELLS; LAMININ; LIGANDS; LYMPHOCYTES; MAGNETIC RESONANCE SPECTROSCOPY; MODELS, MOLECULAR; MOLECULAR CONFORMATION; MUCOPROTEINS; OLIGOPEPTIDES; PEPTIDE LIBRARY; PEPTIDES, CYCLIC; STRUCTURE-ACTIVITY RELATIONSHIP; TRANSFECTION;

EID: 0035797364     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm0005508     Document Type: Article

References (49)

1. Integrins: Versatility, modulation and signaling in cell adhesion
2. Integrins - A versatile and old family of cell adhesion molecules
3. VLA proteins in the integrin family: Structures, functions, and their role on leukocytes
4. Alpha 4 beta 7 integrin mediates B. cell binding to fibronectin and vascular cell adhesion molecule-1. Expression and function of alpha 4 integrins on human B. lymphocytes
5. Alpha4beta7 integrin mediates lymphocyte binding to the mucosal vascular addressin madcam-1
6. Molecular analysis of the physiological and pathophysiological role of alpha 4-integrins
7. Small peptide inhibitors of alpha4beta7 mediated MAdCAM-1 adhesion to lymphocytes
8. Structural requirements for mucosal vascular addressin binding to its lymphocyte receptor alpha4beta7
9. Mucosal addressin cell adhesion molecule-1
10. Distinct binding specificities of integrins alpha4beta7 (LPAM-1), alpha 4beta (VLA-4), alpha IEL beta7
11. Identification of a murine Peyer's Patch - Specific lymphocyte homing receptor as an integrin molecule with an alpha chain homologous to human VLA-4 alpha
12. Peyer's patch-specific lymphocyte homing receptors consist of a VLA-4 like alpha chain associated with either of two integrin beta chains, one of which is novel
13. Cloning expression of mouse integrin beta p(beta 7): A functional role in Peyer's patch-specific lymphocyte homing
14. Monoclonal antibodies specific for beta 7 integrin and mucosal addressin cell adhesion molecule-1 (MAdCAM-1) reduce inflammation in the colon of scid mice reconstituted with CD45RBhigh CD4+ T. cells
15. Involvement of beta 7 integrin and mucosal addressin cell adhesion molecule-1 (MAdCAM-1) in the development of diabetes in obese diabetic mice
16. Stereoisomeric peptide libraries and peptidomimetics for designing selective inhibitors of the alphavbeta3 integrin for new cancer therapy
17. Conformation and biological activity of cyclic peptides
18. Conformation/activity studies of rational designed anti-adhesive RGD peptides
19. Arg-Gly-Asp constrained within cyclic pentapeptides. Strong and selective inhibitors of cell adhesion to vitronectin and laminin fragment P1
20. Structures, dynamics, and biological activities of 15 cyclic hexpeptide analogues of the alpha-amylase inhibitor Tendamistat (HOE 467) in solution
21. Peptidkonformationen 40. Cyclische hexapeptidanaloge des thymopoietins. Synthese und konformationsstudien
22. Influence of serine in position i on conformation and dynamics of revers turns
23. The anatomy and taxonomy of protein structure
24. Peptide flexibility and caculations of an ensemble of molecules
25. Peptide conformations 47. Alanine containing analogues of cyclo(D-Pro-Phe-Thr-Lys(Z)-Trp-Phe-) - Conformationally controlled structure-activity-relationships
26. The minimal essential sequence for a major cell type-specific adhesion site (CS1) within the alternatively spliced type connecting segment domain of fibronectin is leucineaspartic acid-valine
27. Activation-dependent recognition by hematopoietic cells of the LDV sequence in the V. region of fibronectin
28. Design of superactive selective integrin receptor antagonists containing the RGD sequence
29. The structure of immunoglobulin superfamily domains 1 and 2 of MAdCAM-1 reveals novel features important for integrin recognition
30. Solid-phase peptide synthesis
31. Solid-phase synthesis
32. Solid-phase peptide synthesis utilizing 9-fluorenylmethoxycarbonyl amino acids
33. Peptides '83: Structures and function
34. NMR of peptides
35. 13C assignments from sensitivity-enhanced detection of heteronuclear multiple-bond connectivity by 2D multiple quantum NMR
36. Proton-detected C,H correlation via long-range couplings with soft pulses; determination of coupling constants
37. Improved resolution in proton-detected heteronuclear long-range correlation
38. Structure determination of a tetrasaccharide: Transient nuclear overhauser effects in the rotating frame
39. Separation of cross-relaxation and J cross-peaks in 2D rotating frame NMR spectroscopy
40. A simple alternative to E. COSY
41. Improved molecular dynamics simulations for the determination of peptide structures
42. An evaluation of computational strategies for use in the determination of protein structure from distance constraints obtained by nuclear magnetic resonance
43. The sampling properties of some distance geometry algorithms applied to unconstrained polypeptide chains: A study of 1830 independently computed conformations
44. Consistent force field studies of intermolecular forces in hydrogen-bonded crystals
45. Novel modified tripeptide inhibitors of alpha4beta7 mediated lymphoid cell adhesion to MAdCAM-1