5443-31-2Relevant articles and documents
FLUORESCENT PROBES FOR DRUG PERMEABILITY IN GRAM NEGATIVE BACTERIA
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, (2020/02/05)
Described are compounds and methods useful in measuring membrane permeability and efflux transporter activity in bacteria, including multidrug resistance Gram negative bacteria.
A method for inhibiting PRMT7 compound and its preparation method and application (by machine translation)
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, (2018/10/04)
The invention belongs to the field of chemical medicine, and in particular relates to a method for inhibiting PRMT7 compound, its formula is as follows: In some embodiments of the compounds proved that, this compound can to PRMT7 produce better inhibitio
Small molecule antagonists of cell-surface heparan sulfate and heparin-protein interactions
Weiss, Ryan J.,Gordts, Philip L. S. M.,Le, Dzung,Xu, Ding,Esko, Jeffrey D.,Tor, Yitzhak
, p. 5984 - 5993 (2015/09/28)
Surfen, bis-2-methyl-4-amino-quinolyl-6-carbamide, was previously reported as a small molecule antagonist of heparan sulfate (HS), a key cell-surface glycosaminoglycan found on all mammalian cells. To generate structure-activity relationships, a series of rationally designed surfen analogs was synthesized, where its dimeric structure, exocyclic amines, and urea linker region were modified to probe the role of each moiety in recognizing HS. An in vitro assay monitoring inhibition of fibroblast growth factor 2 binding to wild-type CHO cells was utilized to quantify interactions with cell surface HS. The dimeric molecular structure of surfen and its aminoquinoline ring systems was essential for its interaction with HS, and certain dimeric analogs displayed higher inhibitory potency than surfen and were also shown to block downstream FGF signaling in mouse embryonic fibroblast cells. These molecules were also able to antagonize other HS-protein interactions including the binding of soluble RAGE to HS. Importantly, selected molecules were shown to neutralize heparin and other heparinoids, including the synthetic pentasaccharide fondaparinux, in a factor Xa chromogenic assay and in vivo in mice. These results suggest that small molecule antagonists of heparan sulfate and heparin can be of therapeutic potential for the treatment of disorders involving glycosaminoglycan-protein interactions.