Publications & Posters

pan-LOX Inhibitors

Title: Topical application of an irreversible small molecule inhibitor of lysyl oxidases ameliorates skin scarring and fibrosis

Authors: Chaudhari, N., Findlay, AD.,  Stevenson, AW., Clemons, TD., Yao, Y., Joshi, A., Sayar, S., Wallace, G., Rea, S., Toshniwal, P., Deng, Z., Melton, PE., Hortin, N., Iyer, KS., Jarolimek, W., Wood, FM., Fear, MW.

Reference: Nature Communications 2022,

Title: Novel lysyl oxidase inhibitors attenuate hallmarks of primary myelofibrosis in mice

Authors: Leiva, O., Ng, S. K., Matsuura, S., Chitalia, V., Lucero, H., Findlay, A., Turner, C., Jarolimek, W. and Ravid, K.

Reference: International Journal of Hematology 2019, 110(6), 699. 

Title: Pan-Lysyl Oxidase Inhibitor PXS-5505 Ameliorates Multiple-Organ Fibrosis by Inhibiting Collagen Crosslinks in Rodent Models of Systemic Sclerosis

Authors: Yao, Y., Findlay, A., Stolp, J., Rayner, B., Ask, K. and Jarolimek, W.

Reference: International Journal of Molecular Sciences 2022 May 16; 23(10), 5533.
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;

SSAO Inhibitors

Title: Semicarbazide sensitive amine oxidase and vascular adhesion protein-1: one protein being validated as a therapeutic target for inflammatory diseases

Authors: McDonald, I. A., Foot, J., Yin, P., Flening, E. and van Dam, E. M.

Reference:  Annual Reports in Medicinal Chemistry 2007, 42, 229.  

Title: Combining monoamine oxidase B and semicarbazide-sensitive amine oxidase enzyme inhibition to address inflammatory disease

Authors: Foot, J. S., Buson, A., Deodhar, M., Findlay, A. D., Robertson, A. D., Turner, C. I., Yow, T., Zhou, W. and Jarolimek, W.

Reference: Bioorg Med Chem Lett. 2022, 74: 128942. Epub 2022 Aug 11.

Title: Inhibition of vascular adhesion protein 1 protects dopamine neurons from the effects of acute inflammation and restores habit learning in the striatum.

Authors: Becchi, S., Buson, A. & Balleine, B.W.

Reference: J Neuroinflammation 18, 233 (2021).

Title: Semicarbazide-Sensitive Amine Oxidase Inhibition Ameliorates Albuminuria and Glomerulosclerosis but Does Not Improve Tubulointerstitial Fibrosis in Diabetic Nephropathy

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

Reference: PLoS One 15, no. 6 (2020): e0234617.


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: An activity-based bioprobe differentiates a novel small molecule inhibitor from a LOXL2 antibody and provides renewed promise for anti-fibrotic therapeutic strategies


Authors: Findlay, A., Turner, C., Schilter, H., Deodhar, M., Zhou, W., Perryman, L., Foot, J., Zahoor, A., Yao, Y., Hamilton, R., Brock, M., Raso, C., Stolp, J., Galati, M., Hamprecht, D., Charlton, B. and Jarolimek, W.

Reference: Clinical and Translational Medicine 2021) 11(11), e572. 


Title: Inhibition of LOXL2 and other lysyl oxidase (like) enzymes: intervention at the core of fibrotic pathology


Authors: Findlay, A., Turner, C. and Hamprecht, D.

Reference: RSC Drug Discovery Series 2020, 73, 145. 

Title: Lysyl oxidase inhibitors attenuate cyclosporin A-induced nephropathy in mouse

Authors: Nguyen LT, Saad S, Shi Y, Wang R, Chou ASY, Gill A, Yao Y, Jarolimek W, Pollock CA

Reference:. Sci Rep (2021) 11, 12437

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: Identification and Optimization of Mechanism-Based Fluoroallylamine Inhibitors of Lysyl Oxidase-Like 2/3.

Authors: Findlay, A. D., J. S. Foot, A. Buson, M. Deodhar, A. G. Jarnicki, P. M. Hansbro, G. Liu, et al.

Reference: J Med Chem 62, no. 21 (Nov 14 2019): 9874-89.

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 Sci Rep 8, no. 1 (Jun 21 2018): 9423.
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 



Title: Measurement of collagen cross-links from tissue samples by mass spectrometry


Authors: Joshi, A., Zahoor, A. and Buson, A.

Reference: Methods in Molecular Biology (New York, NY, United States) 2019, 1944, 79. 

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.

Reference: J Drug Target. 2017 Apr;25(4):342-349. doi: 10.1080/1061186X.2016.1258703. Epub 2016 Nov 24.

Title: Effect of polyunsaturated fatty acids (PUFAs) on airway epithelial cells' tight junction

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

Reference: Pulm Pharmacol Ther. 2016 Oct;40:30-8. doi: 10.1016/j.pupt.2016.07.004. Epub 2016 Jul 22.

Title: The mannose-6-phosphate analogue, PXS64, inhibits fibrosis via TGF-beta1 pathway in human lung fibroblasts

Authors: Schilter, H., Cantemir-Stone, C. Z., Leksa, V., Ohradanova-Repic, A., Findlay, A. D., Deodhar, M., Stockinger, H., Song, X., Molloy, M., Marsh, C. B. and Jarolimek, W.

Reference: Immunol Lett. 2015 Jun;165(2):90-101. doi: 10.1016/j.imlet.2015.04.003. Epub 2015 Apr 27.

Title: Mannitol enhances antibiotic sensitivity of persister bacteria in Pseudomonas aeruginosa biofilms

Authors: Barraud, N., Buson, A., Jarolimek, W. and Rice, S. A.

Reference: PLoS One. 2013 Dec 13;8(12):e84220. doi: 10.1371/journal.pone.0084220. eCollection 2013.