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
INTEGRIN α4β7 ANTAGONISTS
PTG-100, an Oral α4β7 Antagonist Peptide: Preclinical Development and Phase 1 and 2a Studies in Ulcerative Colitis
William Sandborn, Larry C. Mattheakis, Nishit B. Modi, David Pugatch, Brian Bressler, Scott Lee, Raj Bhandari, Bittoo Kanwar, Richard Shames, Geert D’Haens, Stefan Schreiber, Silvio Danese, Brian Feagan, Rish K. Pai, David Y. Liu, Suneel Gupta, Gastroenterology, August 29, 2021. View Page
Single- and Multiple-Dose Pharmacokinetics and Pharmacodynamics of PN-943, a Gastrointestinal-Restricted Oral Peptide Antagonist of α4β7, in Healthy Volunteers
Nishit B. Modi, Xiaoli Cheng, Larry Mattheakis, Ching-Chang Hwang, Roya Nawabi, David Liu, and Suneel Gupta, Clinical Pharmacology in Drug Development, May 4, 2021. View Page
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.
View PosterThe 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.
View PosterPTG-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.
View PosterModel 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.
View PosterSafety, 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.
View PosterPharmacokinetics 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.
View PosterPreclinical 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.
View PosterIntegrin 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.
View PosterINTERLEUKIN-23 RECEPTOR 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.
View PosterDiscovery 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.
View PosterDiscovery 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.
View PosterTECHNOLOGY 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.