Publications & Posters

Drug Discovery

Publications & Posters

SSAO Inhibitors

Title: Inhibition of semicarbazide-sensitive amine oxidase/vascular adhesion protein-1 reduces lipopolysaccharide-induced neuroinflammation

Authors: Becchi, S., Buson, A., Foot, J., Jarolimek, W. and Balleine, B. W.

Reference: Br J Pharmacol. 2017 Jul;174(14):2302-2317. doi: 10.1111/bph.13832. Epub 2017 Jun 10.

Title: The inhibitor of semicarbazide-sensitive amine oxidase, PXS-4728A, ameliorates key features of chronic obstructive pulmonary disease in a mouse model

Authors: Jarnicki, A. G., Schilter, H., Liu, G., Wheeldon, K., Essilfie, A. T., Foot, J. S., Yow, T. T., Jarolimek, W. and Hansbro, P. M.

Reference: Br J Pharmacol. 2016 Nov;173(22):3161-3175. doi: 10.1111/bph.13573. Epub 2016 Oct 12.

Title: Effects of an anti-inflammatory VAP-1/SSAO inhibitor, PXS-4728A, on pulmonary neutrophil migration

Authors: Schilter, H. C., Collison, A., Russo, R. C., Foot, J. S., Yow, T. T., Vieira, A. T., Tavares, L. D., Mattes, J., Teixeira, M. M. and Jarolimek, W.

Reference: Respir Res. 2015 Mar 20;16:42. doi: 10.1186/s12931-015-0200-z.

Title: Semicarbazide-sensitive amine oxidase (SSAO) inhibition ameliorates kidney fibrosis in a unilateral ureteral obstruction murine model

Authors: Wong, M., Saad, S., Zhang, J., Gross, S., Jarolimek, W., Schilter, H., Chen, J. A., Gill, A. J., Pollock, C. A. and Wong, M. G.

Reference: Am J Physiol Renal Physiol. 2014 Oct 15;307(8):F908-16. doi: 10.1152/ajprenal.00698.2013. Epub 2014 Aug 20.

Title: PXS-4681A, a potent and selective mechanism-based inhibitor of SSAO/VAP-1 with anti-inflammatory effects in vivo

Authors: Foot, J. S., Yow, T. T., Schilter, H., Buson, A., Deodhar, M., Findlay, A. D., Guo, L., McDonald, I. A., Turner, C. I., Zhou, W. and Jarolimek, W.

Reference: J Pharmacol Exp Ther. 2013 Nov;347(2):365-74. doi: 10.1124/jpet.113.207613. Epub 2013 Aug 13.

Title: The discovery and development of selective 3-fluoro-4-aryloxyallylamine inhibitors of the amine oxidase activity of semicarbazide-sensitive amine oxidase/vascular adhesion protein-1 (SSAO/VAP-1)

Authors: Foot, J. S., Deodhar, M., Turner, C. I., Yin, P., van Dam, E. M., Silva, D. G., Olivieri, A., Holt, A. and McDonald, I. A.

Reference: Bioorg Med Chem Lett. 2012 Jun 15;22(12):3935-40. doi: 10.1016/j.bmcl.2012.04.111. Epub 2012 Apr 30.

LOXL2 Inhibitors

Title: The lysyl oxidase like 2/3 enzymatic inhibitor, PXS‐5153A, reduces crosslinks and ameliorates fibrosis

Authors: Heidi Schilter, Alison D. Findlay, Lara Perryman, Tin T. Yow, Joshua Moses, Amna Zahoor, Craig I. Turner, Mandar Deodhar, Jonathan S. Foot, Wenbin Zhou, Angelique Greco, Amar Joshi, Benjamin Rayner, Sarah Townsend, Alberto Buson, Wolfgang Jarolimek.

Reference: J Cell Mol Med. 2018;1–12.

Title: Nanoscale dysregulation of collagen structure-function disrupts mechano-homeostasis and mediates pulmonary fibrosis

Authors: M.G. Jones, O.G. Andriotis, J.J.W. Roberts, K. Lunn, V.J. Tear, L. Cao, K. Ask, D.E. Smart, A. Bonfanti, P. Johnson, A. Alzetani, F. Conforti, R. Doherty, C.Y. Lai, B. Johnson, K.N. Bourdakos, S.V. Fletcher, B.G. Marshall, S. Joga⁹, C. Brereton, S.J. Chee, C. Ottensmeier, P. Sime, J. Gauldie, M. Kolb, S. Mahajan, A. Fabre, A. Bhaskar, W. Jarolimek, L. Richeldi, K.M.A. O’Reilly, P.D. Monk, P.J. Thurner, D.E. Davies

Reference: eLife

Title: Lysyl oxidase-like 2 inhibition ameliorates glomerulosclerosis and albuminuria in diabetic nephropathy

Authors: Stangenberg, S., Saad, S., Schilter, H., Zaky, A., Gill,A. Pollock, C., and Wong, M.G.

Reference: Scientific reports in press

Title: Multiple Functions of Lysyl Oxidase Like-2 in Oral Fibroproliferative Processes

Authors: Saxena, D., Mahjour, F., Findlay, A. D., Mously, E. A., Kantarci, A. and Trackman, P. C.

Reference: J Dent Res. 2018 May 1:22034518775971. doi: 10.1177/0022034518775971.

Title: Inhibition Of LOXL2: Pharmaxis' Small Molecule Approach To Treat Fibrosis

Authors: Buson, A., Cock, T.A., Deodhar, M., Findlay, A.D., Foot, J. S., Jarnicki, A., Moses, J., Turner, C. I., Yow, T. T., Zhou, W., Hansbro, P. M. and Jarolimek, W.

Reference: DOI: 10.1164/ajrccm-conference.2014.189.1_MeetingAbstracts.A6669

Title: Inhibition of Collagen cross-links by novel LOXL2 selective inhibitors in an in-vitro model of fibroblastic foci of IPF

Authors: Roberts J., Lunn K., Tear V., Jones M., Davies D., Jarolimek W., Cao L., Montfort T., Mahajan S., Andriotis O., Thurner P., Monk P.

Link: read poster from ERS 2016

Title: Inhibition of Lysyl Oxidase Like-2 (LOXL2) reduces cardiac interstitial fibrosis in mice

Authors: Buson A., Cao L., Deodhar M., Findlay A.D., Foot J.S., Greco A., Jarolimek W., Moses J., Perryman L., Rayner B., Schilter H.C., Tan X., Turner., Yow T.T., Zahoor A., Zhou W.

Link: read poster

Title: Inhibition of Lysyl Oxidase Like-2 reduces accumulation and collagen cross-links in CCL4-induced liver fibrosis

Authors: Jarolimek W., Buson A., Cao L., Deodhar M., Findlay A.D., Foot J.S., Greco A., Moses J., Schilter H.C., Tan X., Turner., Yow T.T., Zhou W.

Link: read poster

LOX Inhibitors

Title: Pre-clinical evaluation of small molecule LOXL2 inhibitors in breast cancer

Authors: Chang, J., Lucas, M. C., Leonte, L. E., Garcia-Montolio, M., Singh, L. B., Findlay, A. D., Deodhar, M., Foot, J. S., Jarolimek, W., Timpson, P., Erler, J. T. and Cox, T. R.

Reference: Oncotarget. 2017 Apr 18;8(16):26066-26078. doi: 10.18632/oncotarget.15257

Title: A Novel Lysyl Oxidase Inhibitor Attenuates Bone Marrow Fibrosis and Decreases Spleen Size in a Mouse Model of Primary Myelofibrosis

Authors: Leiva, O., Matsuura, S., Findlay,A., Turner, C., Jarolimek, W. and Ravid, K.

Reference: Blood 2017 130:4214;

Other

Title: Synthetic Studies on the Natural Product Myrsinoic Acid F Reveal Biologically Active Analogues

Authors: Mikusek, J., Nugent, J., Ward, J. S., Schwartz, B. D., Findlay, A. D., Foot, J. S. and Banwell, M. G.

Reference: Org Lett. 2018 Jun 11. doi: 10.1021/acs.orglett.8b01558.

Title: The effect of non-specific tight junction modulators on the transepithelial transport of poorly permeable drugs across airway epithelial cells

Authors: Ghadiri, M., Young, P. M., Jarolimek, W., Grau, G. E., Oliver, B. G. and Traini, D.

Product Pipeline

Drug Discovery