Publications

PTG-100

Model Based Predictions of the PTG-100 Pharmacodynamic Responses in Ulcerative Colitis Patients

Mattheakis, L., Fosser, C., Saralaya, R., Horsch, K., Rao, N., Bai, L., Zhao, L., Annamalai, T., Liu, D., 12th Congress of ECCO, February 17, 2017, Barcelona, Spain.

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Safety, Pharmacokinetics and Pharmacodynamics of the Novel Oral Peptide Therapeutic PTG-100 (α4β7 Integrin Antagonist) in Normal Healthy Volunteers

Shames, R., Tozzi, L., Mattheakis, L., Annamalai, T., Bhandari, A., and Liu, D., 24th United European Gastroenterology Week, October 15-19, 2016, Vienna, Austria.

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Pharmacokinetics and Pharmacodynamics Following Oral Administration Of PTG-100, a Peptide Antagonist of Integrin α4β7

Annamalai, T., Mattheakis, L., Bhandari, A., Liu, D., Zemede, G., Hadley, S., Zhao, L., Rao, N., 24th United European Gastroenterology Week, October 15-19, 2016, Vienna, Austria.

Establishing the Human Equivalent Dose for PTG-100, an Oral Peptide Antagonist of Integrin α4β7

Mattheakis, L., Zemede, G., Bai, L., Tran, V., Celino, H., Frederick, B., Zhao, L., Dogra, M., Tovera, J., Shah, S., Rao, N., Hadley, S., Bhandari, A., Annamalai, T., Patel, D., Liu, D., Digestive Disease Week, May 21-24, 2016, San Diego, United States.

Preclinical Characterization of PTG-100, an Oral α4β7 Integrin Peptide Antagonist for Treatment of Ulcerative Colitis

Mattheakis, L., Bhandari, A., Bai, L., Zemede, G., Tran, V., Spencer, N., Celino, H., Frederick, B., Dias, J., Zhao, L., Annamalai, T., Patel, D., Liu, D., ICMI 2015 July 14-18, 2015, Berlin, Germany.

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PTG-100, an Oral Peptide Antagonist of Integrin α4β7 that Alters Trafficking of Gut Homing T Cells in Preclinical Animal Models

Mattheakis, L., Bhandari, A., Bai, L., Zemede, G., Tran, V., Celino, H., Frederick, B., Zhao, L., Dogra, M., Lister, H., Tovera, J., Shah, S., Annamalai, T., Patel , D., Liu, D., 2015 Advances in IBD – Crohn’s & Colitis Foundation’s Clinical & Research Conference, December 2015.

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Integrin α4β7: Discovery of Gut-Restrictive Oral Peptide Antagonists that are Active in Murine Models of Inflammatory Bowel Disease

Mattheakis, L., Bhandari, A., Bai, L., Zemede, G., Tran, V., Spencer, N., Celino, H., Frederick, B., Xu, C., Dias, J., Annamalai, T., Habtezion, A., Patel, D., Liu, D., 2014 Advances in IBD – Crohn’s & Colitis Foundation’s Clinical & Research Conference, December 2014.

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PTG-200

The Biomarker Profile of PTG-200, an Oral Peptide Antagonist of IL-23 Receptor, Tracks with Efficacy in Preclinical Model of IBD

Cheng, X., Taranath, R., Mattheakis, L., Bhandari, A., Liu, D., 12th Congress of ECCO, February 17, 2017, Barcelona, Spain, The Biomarker Profile of PTG-200, an Oral Peptide Antagonist of IL-23 Receptor, Correlates with Efficacy in Preclinical Models of IBD, Cheng, X., Taranath, R., Zhao, L., Yuan, L., Shah, S., Foulke, M., Annamalai, T., Mattheakis, L., Bhandari, A., Patel, D., Liu, D., 2016 Advances in Inflammatory Bowel Diseases, Crohn’s & Colitis Foundation of America’s Clinical & Research Conference, December 9, 2016, Orlando, FL.

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Discovery and Characterization of Novel Oral Peptide Antagonists of Human IL-23 Receptor that are Efficacious in a Rat Model of IBD

Cheng, X., Bhandari, A., Bourne, G., Frederick, B., Zhang, J., McMahon, J., Scott, S., Celino, H., Zemede, G., Spencer, N., Tran, V., Dogra, M., Dias, J., Bai, L., Annamalai, T., Smythe, M., Mattheakis, L., Patel, D., Liu, D., ICMI 2015 July 14-18, 2015, Berlin, Germany.

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Discovery of Novel Oral Peptide Antagonists of IL-23 Receptor that are Efficacious in Rat Model of IBD

Bhandari, A., Cheng, X., Bourne, G., Frederick, B., Zhang, J., McMahon, J., Celino, H., Zemede, G., Tran, V., Tovera, J., Dogra, M., Bai, L., Chen, L., Shaw, S., Annamalai, T., Mattheakis, L., Patel, D., Liu, D., 2015 Advances in IBD – Crohn’s & Colitis Foundation’s Clinical & Research Conference, December 2015.

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PTG-300

Hepcidin Mimetic PTG-300 for Treatment of Ineffective Erythropoiesis and Iron Overload

Gregory Bourne, Li Zhao, Ashok Bhandari, Brian Frederick, Jaimee McMahon, Vinh Tran, Jenny Zhang, Adam Stephenson, James Tovera, Lu Bai, Thamil Annamalai, Dinesh Patel, Mark Smythe, David Liu, Seventh Congress of the International Bioiron Society, May 7-11, 2017, Los Angeles, CA.

Hepcidin Mimetic PTG-300 for Treatment of Ineffective Erythropoiesis and Iron Overload Diseases

Greg Bourne, Li Zhao, Ashok Bhandari, Brian Frederick, Jaimee McMahon, Jenny Zhang, Adam Stephenson, Thamil Annamalai, Larry Mattheakis, Dinesh Patel, Mark Smythe, David Liu, 6th Modern Solid Phase Peptide Synthesis & Its Applications Symposium 2017, October 14, 2017, Fraser Island, Qld Australia.

Technology Platform

Oral peptides with dual mu/delta opioid receptor agonist activities are superior to eluxadoline in preclinical models of IBS-D,

Larry Mattheakis, Li Zhao, Noa Zerangue, Heather Hsu, Jenny Zhang, Greg Bourne, Adam Stephenson, Ashok Bhandari, David Liu, Sampath-Kumar Anandan, 3rd Meeting of the Federation of Neurogastroenterology and Motility, August 29-September 1, 2018, Amsterdam, Netherlands.

Orally Delivered Peptides for Treatment of Inflammatory Bowel Disease

Smythe, M. L, In: Samuel Chackalamannil, David P Rotella and Simon E Ward, (eds.), (2017), Comprehensive Medicinal Chemistry III vol. 6, pp. 157–170. Oxford: Elsevier. http://dx.doi.org/10.1016/B978-0-12-409547-2.12417-5.

Clustering of disulfide-rich peptides provides scaffolds for hit discovery by phage display: application to interleukin-23

Barkan, D.T., Cheng,X-L., Celino, H., Tran, T.T., Bhandari, A., Craik, C.S., Sali, A., and Smythe, M.L., BMC Bioinformatics, (2016), 17, 481. https://doi.org/10.1186/s12859-016-1350-9.

Discovery and Characterization of a Potent Interleukin-6 Binding Peptide with Neutralizing Activity In Vivo

Ranganath, S., Bhandari, A., Avitahl-Curtis, N., McMahon, J., Wachtel, D., Zhang J., Leitheiser C., Bernier, S.G., Liu, G., Tran, T.T., Celino, H., Tobin J., Jung, J., Zhao, H., Gle, K.E., Graul, C., Griffin, A., Schairer, W.C., Higgins, C., Reza, T.L., Mowe, E., Rivers, S., Scott, S., Monreal, A., Shea, C., Bourne, G., Coons, C., Smith, A., Tang, K., Mandyam, R.A., Masferer, J., Liu, D., Patel, D.V., Fretzen, A., Murphy, C.A., Milne, G.T., Smythe, M.L., Carlson, K.E., PLOS ONE (2015), 10(11), 1-19. (journals.plos.org/plosone/article?id=10.1371/journal.pone.0141330).

Conformational searching using a population-based incremental learning algorithm

Long, S.M., Tran, T.T., Adams, P., Darwen, P., Smythe, M.L., Journal of Computational Chemistry (2011) 32:1541-1549.

Defining scaffold geometries for interacting with proteins: geometrical classification of secondary structure linking regions

Tran, T.T., Kulis, C., Long, S.M., Bryant, D., Adams, P., Smythe, M.L., Journal Computer Aided Molecular Design (2010) Vol 24, 917-934.

Library of biphenyl privileged substructures using a safety- catch linker approach

Severinsen, R., Bourne, G.T., Tran, T.T., Ankersen, M., Begtrup, M., Smythe, M.L., Journal of Combinatorial Chemistry (2008) Vol 10, Issue 4, 557-566.

Cyclic tetrapeptides via the ring contraction strategy: chemical techniques useful for their identification

Horton, D.A., Bourne, G.T., Coughlan, J., Kaiser, S.M., Jacobs, C,M., Jones, A., Ruhmann, A., Turner, J.Y., Smythe, M.L., Organic & Biomolecular Chemistry (2008), Vol 6, Issue 8, 1386-1395.