Publications

HEPCIDIN MIMETICS

PTG-300 Eliminates the Need for Therapeutic Phlebotomy in Both Low and High-Risk Polycythemia Vera Patients

Kremyanskaya M, Ginzburg Y, Kuykendall AT, et al., The 62nd ASH Annual Meeting and Exposition, December 5-8, 2020, virtual meeting (originally scheduled for San Diego, California, USA). View Page

PTG-300 Eliminates the Need for Therapeutic Phlebotomy in Both Low and High-Risk Polycythemia Vera Patients

Marina Kremyanskaya, Yelena Ginzburg, Andrew Kuykendall, Abdulraheem Yacoub, Jay Yang, Suneel Gupta, Frank Valone, Sarita Khanna, Srdan Verstovsek, and Ronald Hoffman, The 62nd ASH Annual Meeting and Exposition, December 5-8, 2020, virtual meeting (originally scheduled for San Diego, California, USA). View Page

Mechanism of Systemic Iron Regulation and Hematocrit Control By Hepcidin Peptidomimetics in Pre-Clinical Models

Roopa Taranath, Larry Mattheakis, Li Zhao, Larry Lee, James Tovera, Jingsong Zhao, Xiaoli Cheng, David Liu, The 62nd ASH Annual Meeting and Exposition, December 5-8, 2020, virtual meeting (originally scheduled for San Diego, California, USA). View Page

Hepcidin Peptidomimetics – Oral Efficacy in Pre-Clinical Disease Models of Iron Overload and Erythrocytosis

Roopa Taranath, Gregory Bourne, Jie Zhang, Brian Frederick, Tran T Tran, Ashok Bhandari, Jayanthi Vengalam, Jaimee McMahon, Keith Huie, Grace A Ledet, Li Zhao, James Tovera, Larry Lee, Bo Yang, Celino Dion, Lucy Yuan, Genet Zemede, Michelle Nguyen, Mohammad Masjedizadeh, Xiaoli Cheng, Larry Mattheakis, David Liu, Mark L Smythe, The 62nd ASH Annual Meeting and Exposition, December 5-8, 2020, virtual meeting (originally scheduled for San Diego, California, USA). View Page

Regulation of Iron Homeostasis By PTG-300 Improves Disease Parameters in Mouse Models for Beta-Thalassemia and Hereditary Hemochromatosis

Roopa Taranath, Gregory Bourne, Li Zhao, Brian Frederick, Chelsea King, David Liu, The 61st ASH Annual Meeting and Exposition, December 7-19, 2019, Orlando, Florida, USA. View Page

Hepcidin Mimetic PTG-300 for Treatment of Ineffective Erythropoiesis and Chronic Anemia in Hemoglobinopathy Diseases

Greg Bourne, Li Zhao, Ashok Bhandari, Brian Frederick, Vinh Tran, Jenny Zhang, Adam Stephenson, Roopa Taranath, James Tovera, Thamil Annamalai, Larry Mattheakis, Mark Smythe, David Liu, 23rd Eurpopean Haematology Congress, June 14-17, 2018, Stockholm, Sweden. View Page

Hepcidin Mimetic PTG-300 Induces Dose-Related and Sustained Reductions in Serum Iron and Transferrin Saturation in Healthy Subjects

Andrew Nicholls, Jason Lickliter, Lucio Tozzi, David Liu, Richard Shames, 23rd Eurpopean Haematology Congress, June 14-17, 2018, Stockholm, Sweden. View Page

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 12-14, 2017, Fraser Island, Australia. View Page

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, and David Liu, Seventh Congress of the International BioIron Society (IBIS), May 7-11, 2017, Los Angeles, California, USA. View Page

IL-23R ANTAGONISTS

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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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. View Page

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. View Page

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. View Page

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.

α4β7 INTEGRIN ANTAGONISTS

PN-943, an Oral α4β7 Integrin Antagonist, Inhibits MAdCAM1-Mediated Proliferation and Cytokine Release from CD4+ T-Cells Independent of Trafficking

Lili Cheng, Sarayu Venkataraman, Li Zhao, Larry Lee, Tenny Tang, David Liu, Larry Mattheakis, 15th Congress of ECCO on February 12-15, 2020, Vienna, Austria.

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The Oral α4β7 Integrin Specific Antagonist PN-10943 is More Effective than PTG-100 in Multiple Preclinical Studies

Larry Mattheakis, PhD, 50th Anniversary of Digestive Disease Week, May 18-21, 2019, San Diego, California, United States.

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PTG-100, an Oral Gut-Restricted Peptide α4β7 Antagonist, Induces Clinical and Histologic Remission in Patients with Moderate to Severely Active Ulcerative Colitis

 William J. Sandborn, Brian Bressler, Scott Lee, Raj Bhandari, Bittoo Kanwar, Lucio Tozzi, Richard Shames, Geert D’Haens, Jean-Frederic Colombel, Stefan Schreiber, Silvio Danese, Rish K. Pai, Brian Feagan, UEG Week Vienna 2018, October 20 – 24, 2018, Vienna, Austria.

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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.

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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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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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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