Literature DB >> 11294392

Synthesis and biological evaluation of a sialyl Lewis X mimic with significantly improved E-selectin inhibition.

G Thoma1, J L Magnani, J T Patton.   

Abstract

The synthesis of the highly potent E-selectin inhibitor 5 is described. Sialyl Lewis X mimic 5 was rationally designed by combining two previously disclosed beneficial sLe(x) modifications in a single molecule. The compound was found to be 30-fold more potent than sLe(x) in a static, cell-free equilibrium assay. Furthermore, compound 5 was highly active (IC50 = 10 microM) in a dynamic non-equilibrium assay in which sLe(x) did not inhibit neutrophil rolling at up to 1000 microM.

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Year:  2001        PMID： 11294392     DOI： 10.1016/s0960-894x(01)00092-0

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  3 in total

1.  P-selectin glycoprotein ligand regulates the interaction of multiple myeloma cells with the bone marrow microenvironment.

Authors:  Abdel Kareem Azab; Phong Quang; Feda Azab; Costas Pitsillides; Brian Thompson; Triona Chonghaile; John T Patton; Patricia Maiso; Val Monrose; Antonio Sacco; Hai T Ngo; Ludmila M Flores; Charles P Lin; John L Magnani; Andrew L Kung; Anthony Letai; Ruben Carrasco; Aldo M Roccaro; Irene M Ghobrial
Journal:  Blood       Date:  2011-11-16       Impact factor: 22.113

2.  Convergent Synthesis of Sialyl LewisX- O-Core-1 Threonine.

Authors:  Mohammed Y R Sardar; Appi Reddy Mandhapati; Simon Park; Walter J Wever; Richard D Cummings; Elliot L Chaikof
Journal:  J Org Chem       Date:  2018-04-23       Impact factor: 4.354

Review 3.  Selectins-The Two Dr. Jekyll and Mr. Hyde Faces of Adhesion Molecules-A Review.

Authors:  Igor Tvaroška; Chandrabose Selvaraj; Jaroslav Koča
Journal:  Molecules       Date:  2020-06-19       Impact factor: 4.411
  3 in total

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