Halofuginone inhibits the development of T helper 17 cells, immune cells that play an important role in autoimmune disease, but it does not affect other kinds of T cells which are involved in normal immune function.[3] Halofuginone therefore has potential for the treatment of autoimmune disorders.[4]
Halofuginone is also an inhibitor of collagen type I gene expression and as a consequence it may inhibit tumor cell growth.[1] Halofuginone exerts its effects by acting as a high affinity inhibitor of the enzyme glutamyl-prolyl tRNA synthetase. Inhibition of prolyl tRNA charging leads to the accumulation of uncharged prolyl tRNAs, which serve as a signal to initiate the amino acid starvation response, which in turn exerts anti-inflammatory and anti-fibrotic effects.[5]
Referencesedit
^ ab"Halofuginone hydrobromide". NCI Drug Dictionary. National Cancer Institute, National Institutes of Health, U.S. Department of Health and Human Services.
^. WebCite. 10 March 2000. Archived from the original on 4 March 2012.
^Sundrud MS, Koralov SB, Feuerer M, Calado DP, Kozhaya AE, Rhule-Smith A, et al. (June 2009). "Halofuginone inhibits TH17 cell differentiation by activating the amino acid starvation response". Science. 324 (5932): 1334–8. Bibcode:2009Sci...324.1334S. doi:10.1126/science.1172638. PMC2803727. PMID 19498172.
^Sundrud MS, Koralov SB, Feuerer M, Calado DP, Kozhaya AE, Rhule-Smith A, Lefebvre RE, Unutmaz D, Mazitschek R, Waldner H, Whitman M, Keller T, Rao A (June 2009). "Halofuginone inhibits TH17 cell differentiation by activating the amino acid starvation response". Science. 324 (5932): 1334–8. Bibcode:2009Sci...324.1334S. doi:10.1126/science.1172638. PMC2803727. PMID 19498172.
"A new lead for autoimmune disease". EurekAlert! (Press release). 4 June 2009.
^Keller TL, Zocco D, Sundrud MS, Hendrick M, Edenius M, Yum J, et al. (February 2012). "Halofuginone and other febrifugine derivatives inhibit prolyl-tRNA synthetase". Nature Chemical Biology. 8 (3): 311–7. doi:10.1038/nchembio.790. PMC3281520. PMID 22327401.
April 12, 2024
halofuginone, sold, under, brand, name, halocur, coccidiostat, used, veterinary, medicine, synthetic, halogenated, derivative, febrifugine, natural, quinazolinone, alkaloid, which, found, chinese, herb, dichroa, febrifuga, chang, shan, collgard, biopharmaceuti. Halofuginone sold under the brand name Halocur is a coccidiostat used in veterinary medicine It is a synthetic halogenated derivative of febrifugine a natural quinazolinone alkaloid which can be found in the Chinese herb Dichroa febrifuga Chang Shan 1 Collgard Biopharmaceuticals is developing halofuginone for the treatment of scleroderma and it has received orphan drug designation from the U S Food and Drug Administration 2 HalofuginoneClinical dataTrade namesHalocurAHFS Drugs comInternational Drug NamesATCvet codeQP51BX01 WHO Legal statusLegal statusEU Rx onlyIdentifiersIUPAC name 7 Bromo 6 chloro 3 3 2S 3R 3 hydroxy 2 piperidinyl 2 oxopropyl 4 quinazolinoneCAS Number55837 20 2 YPubChem CID400772ChemSpider355164 NUNIIL31MM1385EChEMBLChEMBL1199540 NCompTox Dashboard EPA DTXSID0048260Chemical and physical dataFormulaC 16H 17Br Cl N 3O 3Molar mass414 68 g mol 13D model JSmol Interactive imageSMILES O C CN3C NC2 CC Br C Cl C C2C3 O C C H 1NCCC C H 1OInChI InChI 1S C16H17BrClN3O3 c17 11 6 13 10 5 12 11 18 16 24 21 8 20 13 7 9 22 4 14 15 23 2 1 3 19 14 h5 6 8 14 15 19 23H 1 4 7H2 t14 15 m0 s1 NKey LVASCWIMLIKXLA LSDHHAIUSA N N N Y what is this verify Halofuginone inhibits the development of T helper 17 cells immune cells that play an important role in autoimmune disease but it does not affect other kinds of T cells which are involved in normal immune function 3 Halofuginone therefore has potential for the treatment of autoimmune disorders 4 Halofuginone is also an inhibitor of collagen type I gene expression and as a consequence it may inhibit tumor cell growth 1 Halofuginone exerts its effects by acting as a high affinity inhibitor of the enzyme glutamyl prolyl tRNA synthetase Inhibition of prolyl tRNA charging leads to the accumulation of uncharged prolyl tRNAs which serve as a signal to initiate the amino acid starvation response which in turn exerts anti inflammatory and anti fibrotic effects 5 References edit a b Halofuginone hydrobromide NCI Drug Dictionary National Cancer Institute National Institutes of Health U S Department of Health and Human Services Halofuginone Receives FDA Orphan Drug Status For Scleroderma WebCite 10 March 2000 Archived from the original on 4 March 2012 Sundrud MS Koralov SB Feuerer M Calado DP Kozhaya AE Rhule Smith A et al June 2009 Halofuginone inhibits TH17 cell differentiation by activating the amino acid starvation response Science 324 5932 1334 8 Bibcode 2009Sci 324 1334S doi 10 1126 science 1172638 PMC 2803727 PMID 19498172 Sundrud MS Koralov SB Feuerer M Calado DP Kozhaya AE Rhule Smith A Lefebvre RE Unutmaz D Mazitschek R Waldner H Whitman M Keller T Rao A June 2009 Halofuginone inhibits TH17 cell differentiation by activating the amino acid starvation response Science 324 5932 1334 8 Bibcode 2009Sci 324 1334S doi 10 1126 science 1172638 PMC 2803727 PMID 19498172 A new lead for autoimmune disease EurekAlert Press release 4 June 2009 Keller TL Zocco D Sundrud MS Hendrick M Edenius M Yum J et al February 2012 Halofuginone and other febrifugine derivatives inhibit prolyl tRNA synthetase Nature Chemical Biology 8 3 311 7 doi 10 1038 nchembio 790 PMC 3281520 PMID 22327401 Retrieved from https en wikipedia org w index php title Halofuginone amp oldid 1179574459, wikipedia, wiki, book, books, library,
