About: One novel quinoxaline derivative as a potent human cyclophilin A inhibitor shows highly inhibitory activity against mouse spleen cell proliferation

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About: One novel quinoxaline derivative as a potent human cyclophilin A inhibitor shows highly inhibitory activity against mouse spleen cell proliferation Goto Sponge NotDistinct Permalink

An Entity of Type : schema:ScholarlyArticle, within Data Space : covidontheweb.inria.fr associated with source document(s)

Attributes	Values
type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
has title	One novel quinoxaline derivative as a potent human cyclophilin A inhibitor shows highly inhibitory activity against mouse spleen cell proliferation
Creator	Jiang, Hualiang Liu, Hong Chen, Jing Chen, Kaixian Shen, Xu Zhang, Li Xu, Qiang Li, Jian Wang, Feng Gui, Chunshan Qin, Yu Bai, Donglu Nan, Fajun Shen, Jingkang
Source	Elsevier; Medline; PMC
abstract	Abstract Cyclophilin A (CypA) is a ubiquitous cellular enzyme playing critical roles in many biological processes, and its inhibitor has been reported to have potential immunosuppressive activity. In this work, we reported a novel quinoxaline derivative, 2,3-di(furan-2-yl)-6-(3-N,N-diethylcarbamoyl-piperidino)carbonylamino quinoxaline (DC838, 3), which was confirmed to be a potent inhibitor against human CypA. By using the surface plasmon resonance (SPR) and fluorescence titration techniques, the kinetic analysis of CypA/DC838 interaction was quantitatively performed. CypA peptidyl prolyl cis–trans isomerase (PPIase) activity inhibition assay showed that DC838 demonstrated highly CypA PPIase inhibitory activity. In vivo assay results showed that DC838 could inhibit mouse spleen cell proliferation induced by concanavalin A (Con A). Molecular docking simulation further elucidated the specific DC838 binding to CypA at the atomic level. The current work should provide useful information in the discovery of immunosuppressor based on CypA inhibitor.
has issue date	2006-08-15(xsd:dateTime)
bibo:doi	10.1016/j.bmc.2006.04.026
bibo:pmid	16682211
has license	els-covid
sha1sum (hex)	5ff71dfaa81b4bd709454cdddf399b8a76d5eb41
schema:url	https://doi.org/10.1016/j.bmc.2006.04.026
resource representing a document's title	One novel quinoxaline derivative as a potent human cyclophilin A inhibitor shows highly inhibitory activity against mouse spleen cell proliferation
has PubMed Central identifier	PMC7126670
has PubMed identifier	16682211
schema:publication	Bioorganic & Medicinal Chemistry
resource representing a document's body	covid:5ff71dfaa81b4bd709454cdddf399b8a76d5eb41#body_text
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