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Targeting host cell furin proprotein convertases as a therapeutic strategy against bacterial toxins and viral pathogens.

Shiryaev SA, Remacle AG, Ratnikov BI, Nelson NA, Savinov AY, Wei G, Bottini M, Rega MF, Parent A, Desjardins R, Fugere M, Day R, Sabet M, Pellecchia M, Liddington RC, Smith JW, Mustelin T, Guiney DG, Lebl M, Strongin AY.

J Biol Chem. 2007 Jul 20;282(29):20847-53. Epub 2007 May 30.


Substrate cleavage analysis of furin and related proprotein convertases. A comparative study.

Remacle AG, Shiryaev SA, Oh ES, Cieplak P, Srinivasan A, Wei G, Liddington RC, Ratnikov BI, Parent A, Desjardins R, Day R, Smith JW, Lebl M, Strongin AY.

J Biol Chem. 2008 Jul 25;283(30):20897-906. doi: 10.1074/jbc.M803762200. Epub 2008 May 27.


The prosegments of furin and PC7 as potent inhibitors of proprotein convertases. In vitro and ex vivo assessment of their efficacy and selectivity.

Zhong M, Munzer JS, Basak A, Benjannet S, Mowla SJ, Decroly E, Chrétien M, Seidah NG.

J Biol Chem. 1999 Nov 26;274(48):33913-20.


Sequence specificity of furin, a proprotein-processing endoprotease, for the hemagglutinin of a virulent avian influenza virus.

Walker JA, Molloy SS, Thomas G, Sakaguchi T, Yoshida T, Chambers TM, Kawaoka Y.

J Virol. 1994 Feb;68(2):1213-8.


Optimization of furin inhibitors to protect against the activation of influenza hemagglutinin H5 and Shiga toxin.

Gagnon H, Beauchemin S, Kwiatkowska A, Couture F, D'Anjou F, Levesque C, Dufour F, Desbiens AR, Vaillancourt R, Bernard S, Desjardins R, Malouin F, Dory YL, Day R.

J Med Chem. 2014 Jan 9;57(1):29-41. doi: 10.1021/jm400633d. Epub 2013 Dec 23.


Selective and potent furin inhibitors protect cells from anthrax without significant toxicity.

Remacle AG, Gawlik K, Golubkov VS, Cadwell GW, Liddington RC, Cieplak P, Millis SZ, Desjardins R, Routhier S, Yuan XW, Neugebauer WA, Day R, Strongin AY.

Int J Biochem Cell Biol. 2010 Jun;42(6):987-95. doi: 10.1016/j.biocel.2010.02.013. Epub 2010 Mar 1.


The secretory proprotein convertases furin, PC5, and PC7 activate VEGF-C to induce tumorigenesis.

Siegfried G, Basak A, Cromlish JA, Benjannet S, Marcinkiewicz J, Chrétien M, Seidah NG, Khatib AM.

J Clin Invest. 2003 Jun;111(11):1723-32.


Processing of alpha4 integrin by the proprotein convertases: histidine at position P6 regulates cleavage.

Bergeron E, Basak A, Decroly E, Seidah NG.

Biochem J. 2003 Jul 15;373(Pt 2):475-84.


Cleavage mechanism of the H5N1 hemagglutinin by trypsin and furin.

Guo XL, Li L, Wei DQ, Zhu YS, Chou KC.

Amino Acids. 2008 Aug;35(2):375-82. doi: 10.1007/s00726-007-0611-3. Epub 2008 Jan 31.


Effects of spontaneous deamidation on the cytotoxic activity of the Bacillus anthracis protective antigen.

Zomber G, Reuveny S, Garti N, Shafferman A, Elhanany E.

J Biol Chem. 2005 Dec 2;280(48):39897-906. Epub 2005 Sep 27.


A role for PACE4 in the proteolytic activation of anthrax toxin protective antigen.

Gordon VM, Rehemtulla A, Leppla SH.

Infect Immun. 1997 Aug;65(8):3370-5.


Polyarginine inhibits gp160 processing by furin and suppresses productive human immunodeficiency virus type 1 infection.

Kibler KV, Miyazato A, Yedavalli VS, Dayton AI, Jacobs BL, Dapolito G, Kim SJ, Jeang KT.

J Biol Chem. 2004 Nov 19;279(47):49055-63. Epub 2004 Sep 14.


Furin targeted drug delivery for treatment of rhabdomyosarcoma in a mouse model.

Hajdin K, D'Alessandro V, Niggli FK, Schäfer BW, Bernasconi M.

PLoS One. 2010 May 3;5(5):e10445. doi: 10.1371/journal.pone.0010445.


Heterosubtypic neutralizing monoclonal antibodies cross-protective against H5N1 and H1N1 recovered from human IgM+ memory B cells.

Throsby M, van den Brink E, Jongeneelen M, Poon LL, Alard P, Cornelissen L, Bakker A, Cox F, van Deventer E, Guan Y, Cinatl J, ter Meulen J, Lasters I, Carsetti R, Peiris M, de Kruif J, Goudsmit J.

PLoS One. 2008;3(12):e3942. doi: 10.1371/journal.pone.0003942. Epub 2008 Dec 16.


Heparin enhances the furin cleavage of HIV-1 gp160 peptides.

Pasquato A, Dettin M, Basak A, Gambaretto R, Tonin L, Seidah NG, Di Bello C.

FEBS Lett. 2007 Dec 22;581(30):5807-13. Epub 2007 Nov 26.

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