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February 26-28, 2013
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TIDES: Oligonucleotide and Peptide® Therapeutics from Research through Commercialization
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Peptide Discovery and Development
- Agenda summary: Go to the agenda summary to view the detailed agenda for each track, course, keynote or plenary session.
- To view the complete agenda: Please download the PDF brochure.
Peptide Discovery and Development
Courses: Sunday | Plenary Sessions: Monday | Main Conference: Tuesday | Wednesday
Monday keynote and plenary sessions are shared across all tracks. Please click on the respective links below for the full Monday agenda.
7:30
Registration and Coffee
12:50
Lunch on your own
5:30
Networking, Wine and Cheese Reception in Poster and Exhibit Hall
Courses: Sunday | Plenary Sessions: Monday | Main Conference: Tuesday | Wednesday
7:15
Registration and Coffee
8:15
Chairman's Remarks
Tomi K. Sawyer, Ph.D., Chief Scientific Officer and Senior Vice President, Aileron Therapeutics Inc.
Tomi K. Sawyer, Ph.D., Chief Scientific Officer and Senior Vice President, Aileron Therapeutics Inc.
Novel Synthetic Approaches to Modify Peptides and Improve Drug-like Properties
8:30
Chemoselective Approaches for Protein Synthesis and Bioconjugation
Chemical ligation approaches have become essential tools for the engineering of complex molecules including proteins, nucleic acids and nanoparticles. What makes these reactions so useful is their compatibility with the biological "solvent" water and a high level of chemoselectivity that enables their application in complex molecular environments. Examples of how these reactions are used to synthesize proteins and peptide-bioconjugates in order to tune their structural and functional properties are presented.
Philip Dawson, Ph.D., Associate Professor, Department of Chemistry and Associate Dean of Graduate Studies, The Scripps Research Institute
Chemical ligation approaches have become essential tools for the engineering of complex molecules including proteins, nucleic acids and nanoparticles. What makes these reactions so useful is their compatibility with the biological "solvent" water and a high level of chemoselectivity that enables their application in complex molecular environments. Examples of how these reactions are used to synthesize proteins and peptide-bioconjugates in order to tune their structural and functional properties are presented.
Philip Dawson, Ph.D., Associate Professor, Department of Chemistry and Associate Dean of Graduate Studies, The Scripps Research Institute
9:00
Clicking into Peptide Staples via a Chemoselective Cysteine Arylation
Here we report a novel and robust method to staple unprotected peptides using a cysteine click reaction. Importantly, this chemistry allowed for peptide modifications that imparted favorable cell penetration and proteolytic stability. This approach expands the biomolecular toolkit for the facile modification cysteine contained within peptides.
Brad L. Pentelute, Ph.D., Assistant Professor of Chemistry, Massachusetts Institute of Technology
Here we report a novel and robust method to staple unprotected peptides using a cysteine click reaction. Importantly, this chemistry allowed for peptide modifications that imparted favorable cell penetration and proteolytic stability. This approach expands the biomolecular toolkit for the facile modification cysteine contained within peptides.
Brad L. Pentelute, Ph.D., Assistant Professor of Chemistry, Massachusetts Institute of Technology
Structure-based Design of Novel Peptides
9:30
Interfering Peptides Targeting Protein-protein Interactions
Protein-protein interaction surfaces are attractive yet challenging targets for disease intervention. We use rational design in combination with in-vivo and in-vitro selection systems to generate interfering peptides (iPEP) specifically targeting intracellular protein interaction domains. Different selection strategies, the generation of iPEPs against Jun, Fos, AF10 and Mitf as well as photoswitchable iPEPs are discussed.
Katja Arndt, Ph.D., Professor of Molecular Biotechnology, Institute for Biochemistry and Biology, University of Potsdam, Germany
Protein-protein interaction surfaces are attractive yet challenging targets for disease intervention. We use rational design in combination with in-vivo and in-vitro selection systems to generate interfering peptides (iPEP) specifically targeting intracellular protein interaction domains. Different selection strategies, the generation of iPEPs against Jun, Fos, AF10 and Mitf as well as photoswitchable iPEPs are discussed.
Katja Arndt, Ph.D., Professor of Molecular Biotechnology, Institute for Biochemistry and Biology, University of Potsdam, Germany
10:00
The Design of Cell-penetrating Peptides with Intrinsic Biological Activity
Using computational models, we found key predictors of cellular uptake from the peptide sequence. This talk illustrates examples in which a grafting approach was used to engineer a CPP sequence to also carry a function (eIF4E) and, vice versa, where a functional peptide was engineered to also be a CPP (IRF5).
Francesca Milletti, Ph.D., Head, Cheminformatics and Statistics, Hoffmann-La Roche
Using computational models, we found key predictors of cellular uptake from the peptide sequence. This talk illustrates examples in which a grafting approach was used to engineer a CPP sequence to also carry a function (eIF4E) and, vice versa, where a functional peptide was engineered to also be a CPP (IRF5).
Francesca Milletti, Ph.D., Head, Cheminformatics and Statistics, Hoffmann-La Roche
10:30
Networking Refreshment Break in Poster and Exhibit Hall
11:15
Structure-based Discovery of ATSP-7041, a Dual MDM2 and MDMX Targeting Stapled α-Helical Peptide Exhibiting Potency In Vitro and In Vivo Efficacy in Xenograft Models of Human Cancer
The structure-based discovery of ATSP-7041 shows the first example of a negatively charged, amphipathic stapled α−helical peptide having potent and selective cellular activities. ATSP-7041 is a novel dual MDM2/MDMX inhibitor exhibiting a proof-of-concept for the treatment of cancers with wild-type p53 and overexpression of MDM2/MDMX. ATSP-7041 binds both MDM2 and MDMX with nanomolar affinities, achieves sub-micromolar in vitro activity in cancer cell lines and demonstrates robust in vivo tumor growth suppression in an MDM2/MDMX-overexpressing xenograft cancer models with clear correlation to on-target PK/PD activity.
Vincent Guerlavais, Ph.D., Senior Principal Scientist, Aileron Therapeutics, Inc.
The structure-based discovery of ATSP-7041 shows the first example of a negatively charged, amphipathic stapled α−helical peptide having potent and selective cellular activities. ATSP-7041 is a novel dual MDM2/MDMX inhibitor exhibiting a proof-of-concept for the treatment of cancers with wild-type p53 and overexpression of MDM2/MDMX. ATSP-7041 binds both MDM2 and MDMX with nanomolar affinities, achieves sub-micromolar in vitro activity in cancer cell lines and demonstrates robust in vivo tumor growth suppression in an MDM2/MDMX-overexpressing xenograft cancer models with clear correlation to on-target PK/PD activity.
Vincent Guerlavais, Ph.D., Senior Principal Scientist, Aileron Therapeutics, Inc.
11:45
Identification of Cell-permeable Peptides Targeting the Wnt-pathway - Functional Characterization and Activity In Vivo
Nexigen develops peptide drugs aiming at non-enzymatic, "un-druggable" proteins. We identified cell-permeable peptides which target the Wnt signaling pathway. This pathway plays an important role in oncology (e.g. colon cancer). The talk highlights Nexigen's approach to screen for and further develop cell-permeable peptide modulators. We provide experimental evidence for the successful identification and characterization of such modulators which show activity in various cellular systems as well as in vivo.
Hanjo Hennemann, Ph.D., Chief Scientific Officer, Nexigen GmbH, Germany
Nexigen develops peptide drugs aiming at non-enzymatic, "un-druggable" proteins. We identified cell-permeable peptides which target the Wnt signaling pathway. This pathway plays an important role in oncology (e.g. colon cancer). The talk highlights Nexigen's approach to screen for and further develop cell-permeable peptide modulators. We provide experimental evidence for the successful identification and characterization of such modulators which show activity in various cellular systems as well as in vivo.
Hanjo Hennemann, Ph.D., Chief Scientific Officer, Nexigen GmbH, Germany
12:15
The Alphabody: At the Crossroads of Constrained Peptides and Small Proteins
Alphabodies can materialize in two formats. The peptidic format comprises a bundle of alpha-helically constrained peptides, organized in a triple-stranded coiled coil, which are connected by linkers in the protein format. As illustrated for the IL-23 target, binders obtained in one format can be converted into the other format. Both formats are amenable to library screening for the discovery of helically constrained peptides, including D-peptides, which, depending on the application requirements can be developed as protein or as peptidic therapeutics.
Ignace Lasters, Ph.D., Chief Scientific Officer, Complix NV, Belgium
Alphabodies can materialize in two formats. The peptidic format comprises a bundle of alpha-helically constrained peptides, organized in a triple-stranded coiled coil, which are connected by linkers in the protein format. As illustrated for the IL-23 target, binders obtained in one format can be converted into the other format. Both formats are amenable to library screening for the discovery of helically constrained peptides, including D-peptides, which, depending on the application requirements can be developed as protein or as peptidic therapeutics.
Ignace Lasters, Ph.D., Chief Scientific Officer, Complix NV, Belgium
12:45
Networking Luncheon in Poster and Exhibit Hall
1:55
Chairman's Remarks
Tomi K. Sawyer, Ph.D., Chief Scientific Officer and Senior Vice President, Aileron Therapeutics Inc.
Tomi K. Sawyer, Ph.D., Chief Scientific Officer and Senior Vice President, Aileron Therapeutics Inc.
Molecular Diversity and Novel Peptide Macrocycles
2:00
Plant-based Production of Orally Active Macrocyclic Peptides
Plants produce ultra-stable macrocyclic peptides for defense purposes. We adapt these cyclotides as scaffolds for drug design by en-grafting them with bioactive peptide sequences targeting cancer, cardiovascular disease, pain and metabolic disease. With recent discoveries of cyclotide genes in legumes, the opportunity exists to manufacture pharmaceutical cyclotides efficiently and inexpensively in transgenic plants.
David Craik, Ph.D., Professor of Biomolecular Structure, Institute for Molecular Bioscience, University of Queensland, Australia
Plants produce ultra-stable macrocyclic peptides for defense purposes. We adapt these cyclotides as scaffolds for drug design by en-grafting them with bioactive peptide sequences targeting cancer, cardiovascular disease, pain and metabolic disease. With recent discoveries of cyclotide genes in legumes, the opportunity exists to manufacture pharmaceutical cyclotides efficiently and inexpensively in transgenic plants.
David Craik, Ph.D., Professor of Biomolecular Structure, Institute for Molecular Bioscience, University of Queensland, Australia
2:30
New Strategies for Peptide Macrocyclization
Peptide macrocycles are having a prominent footprint in contemporary drug discovery programs. Our novel technology offers a means to rapidly produce peptide macrocycles equipped with structural markers that enable optimization of both cell permeability and production of diverse compounds that are differentiated on the basis of their three-dimensional shapes. This platform is based on aziridine aldehydes, reagents with an uncanny ability to tie up the loose ends of linear peptides into circular shapes.
Andrei Yudin, Ph.D., Founder, Encycle Therapeutics and Professor of Chemistry, University of Toronto, Canada
Peptide macrocycles are having a prominent footprint in contemporary drug discovery programs. Our novel technology offers a means to rapidly produce peptide macrocycles equipped with structural markers that enable optimization of both cell permeability and production of diverse compounds that are differentiated on the basis of their three-dimensional shapes. This platform is based on aziridine aldehydes, reagents with an uncanny ability to tie up the loose ends of linear peptides into circular shapes.
Andrei Yudin, Ph.D., Founder, Encycle Therapeutics and Professor of Chemistry, University of Toronto, Canada
3:00
Macrocycles for Drug Discovery - Identification of Small Molecule Synthetic Macrocycle Antagonists of Human IL17A
Ensemble Therapeutics has developed a DNA-programmed chemistry platform for the rapid synthesis and screening of macrocycles (Ensemblins™). Using this platform, small molecule macrocyclic compounds have been discovered that are nanomolar inhibitors of the interaction of the IL17A cytokine with its receptor. These compounds are anti-inflammatory in IL17-dependent animal inflammatory models and optimized for oral bioavailability.
Nick Terrett, PhD., Chief Scientific Officer, Ensemble Therapeutics Corp.
Ensemble Therapeutics has developed a DNA-programmed chemistry platform for the rapid synthesis and screening of macrocycles (Ensemblins™). Using this platform, small molecule macrocyclic compounds have been discovered that are nanomolar inhibitors of the interaction of the IL17A cytokine with its receptor. These compounds are anti-inflammatory in IL17-dependent animal inflammatory models and optimized for oral bioavailability.
Nick Terrett, PhD., Chief Scientific Officer, Ensemble Therapeutics Corp.
3:30
Networking Refreshment Break in Poster and Exhibit Hall
4:15
Bi-cyclic Peptides to Target Protein-protein Interactions
The Bicycle technology is based on repertoires of peptides displayed on the surface of bacteriophages which can be modified with an organochemical scaffold to create a diverse array of constrained peptides. These repertoires have been extensively used for iterative selections to identify high affinity binding peptides for a wide array of protein-protein interactions, including cytokine-cytokine receptors and proteases. Results will be presented that exemplify the potential of the technology and its application to animal models of diseases.
Christophe Bonny, Ph.D., Chief Scientific Officer, Bicycle Therapeutics, United Kingdom
The Bicycle technology is based on repertoires of peptides displayed on the surface of bacteriophages which can be modified with an organochemical scaffold to create a diverse array of constrained peptides. These repertoires have been extensively used for iterative selections to identify high affinity binding peptides for a wide array of protein-protein interactions, including cytokine-cytokine receptors and proteases. Results will be presented that exemplify the potential of the technology and its application to animal models of diseases.
Christophe Bonny, Ph.D., Chief Scientific Officer, Bicycle Therapeutics, United Kingdom
Panel Discussion
4:45
Emerging Strategies for Novel Peptide Drug Discovery
Tomi K. Sawyer, Ph.D., Chief Scientific Officer and Senior Vice President, Aileron Therapeutics Inc.
Panelists:
David Craik, Ph.D., Professor of Biomolecular Structure, Institute for Molecular Bioscience, University of Queensland, Australia
Hanjo Hennemann, Ph.D., Chief Scientific Officer, Nexigen GmbH, Germany
Francesca Milletti, Ph.D., Head, Cheminformatics and Statistics, Hoffmann-La Roche
Nick Terrett, Ph.D., Chief Scientific Officer, Ensemble Therapeutics Corp.
- Predictive tools and structure-based, computational approaches
- New frontiers in peptide design and engineering
- Novel peptide-like scaffolds and structures
- Peptides as protein-protein interaction modulators
Tomi K. Sawyer, Ph.D., Chief Scientific Officer and Senior Vice President, Aileron Therapeutics Inc.
Panelists:
David Craik, Ph.D., Professor of Biomolecular Structure, Institute for Molecular Bioscience, University of Queensland, Australia
Hanjo Hennemann, Ph.D., Chief Scientific Officer, Nexigen GmbH, Germany
Francesca Milletti, Ph.D., Head, Cheminformatics and Statistics, Hoffmann-La Roche
Nick Terrett, Ph.D., Chief Scientific Officer, Ensemble Therapeutics Corp.
5:15
Networking, Wine and Cheese Reception in Poster and Exhibit Hall
Dedicated Poster Viewing - Poster presenters will be at their posters to discuss results with you. Sponsored by
Dedicated Poster Viewing - Poster presenters will be at their posters to discuss results with you. Sponsored by
Courses: Sunday | Plenary Sessions: Monday | Main Conference: Tuesday | Wednesday
7:30
Coffee
Featured Presentation
Unpublished Data
8:00
Tackling RNAi Delivery with Bioreversible PhosphoTriester siRNN ProdrugsIn the world of RNAi therapeutics, siRNA delivery remains the technological problem to solve. We pioneered a RNAi delivery technology that radically shrinks the size to the smallest possible, self-delivering monomeric RNAi molecule by synthesis of neutral bioreversible phosphotriester siRNN prodrugs that are converted by intracellular restricted enzymes into charged phosphodiester siRNAs.
Steven F. Dowdy, Ph.D., Professor, Cellular and Molecular Medicine, UCSD School of Medicine
8:25
Chairman's Remarks
Jesse Z. Dong, Ph.D., Vice President, Compound Discovery, IPSEN
Jesse Z. Dong, Ph.D., Vice President, Compound Discovery, IPSEN
Intracellular Delivery of Peptides
8:30
Biologically Active Cell Penetrating Peptides as Potential Therapeutics-Opening up the "Undruggable Target Space"
Intracellular protein-protein interactions represent a very large target space, which have thus far been viewed as mostly undruggable with small molecules. Cell penetrating peptides are emerging as the potential key to unlock this large target space. This presentation describes the different strategies to generate cell penetrating peptides as therapeutics and discusses their potential and challenges.
Nader Fotouhi, Ph.D., Vice President, Global Head Discovery Technologies, Hoffmann-La Roche
Intracellular protein-protein interactions represent a very large target space, which have thus far been viewed as mostly undruggable with small molecules. Cell penetrating peptides are emerging as the potential key to unlock this large target space. This presentation describes the different strategies to generate cell penetrating peptides as therapeutics and discusses their potential and challenges.
Nader Fotouhi, Ph.D., Vice President, Global Head Discovery Technologies, Hoffmann-La Roche
9:00
Intracellular Delivery of Peptides - An Overview from the Perspectives of Pharma
This lecture provides an overview about current methodologies and technologies important for the understanding of intracellular transport for peptides. Some conformational aspects are highlighted and the value of in-silico prediction is discussed. The identification of cell-permeable peptides to address intracellular targets further encourages peptide therapeutics in the biotech/pharma environment.
Thomas Vorherr Ph.D., Director Peptide Discovery, Novartis Pharma AG, Switzerland
This lecture provides an overview about current methodologies and technologies important for the understanding of intracellular transport for peptides. Some conformational aspects are highlighted and the value of in-silico prediction is discussed. The identification of cell-permeable peptides to address intracellular targets further encourages peptide therapeutics in the biotech/pharma environment.
Thomas Vorherr Ph.D., Director Peptide Discovery, Novartis Pharma AG, Switzerland
9:30
Cellular Peptide Delivery - Exploration of Structure Space
Strategies to address intracellular protein-protein-interactions are critically depend on efficient strategies for cellular delivery. Next to conjugation with cell-penetrating peptides, structural modifications within the protein scaffold can also confer cell-penetrating capacity. The effective implementation of cell-entry capacity requires the understanding of the structure-activity relationships of molecular events involved in uptake. This presentation discusses analyses for the cellular delivery of linear, cyclic and bicyclic peptide scaffolds that create a basis for a rational design of peptide-based drugs for intracellular applications. Our results have immediate implications for the development of conformational constrained inhibitors of protein-protein interactions from synthetic scaffolds and from scaffolds provided by nature such as cyclic toxins.
Roland Brock, Ph.D., Head, Department of Biochemstry, Nijmegen Centre for Molecular Life Sciences, Radboud University Nijmegen Medical Centre, The Netherlands
Strategies to address intracellular protein-protein-interactions are critically depend on efficient strategies for cellular delivery. Next to conjugation with cell-penetrating peptides, structural modifications within the protein scaffold can also confer cell-penetrating capacity. The effective implementation of cell-entry capacity requires the understanding of the structure-activity relationships of molecular events involved in uptake. This presentation discusses analyses for the cellular delivery of linear, cyclic and bicyclic peptide scaffolds that create a basis for a rational design of peptide-based drugs for intracellular applications. Our results have immediate implications for the development of conformational constrained inhibitors of protein-protein interactions from synthetic scaffolds and from scaffolds provided by nature such as cyclic toxins.
Roland Brock, Ph.D., Head, Department of Biochemstry, Nijmegen Centre for Molecular Life Sciences, Radboud University Nijmegen Medical Centre, The Netherlands
Preclinical Strategies to Exploit Novel Targets and Optimize Properties of Peptides
10:00
Exploiting Disulfide-rich Peptides in Drug Discovery
Disulfide-rich peptides (DRPs) are ideal scaffolds for drug development and have favorable features for diverse clinical applications. They possess a disulfide-strained core that imparts extraordinary chemical and biological stability characteristics, but also sequence flexibility, allowing the introduction of novel functionalities. We have developed robust and validated design, synthesis and display methods to exploit this scaffold class. This presentation describes an innovative combination of small molecule drug discovery approaches and protein-based molecular evolution strategies guided by structure based drug design to exploit this scaffold class in a diversity, target-class or structure-based context. The versatility of the platform is illustrated by its application to various drug target classes.
Mark Smythe, Ph.D., Founder, Protagonist Therapeutics
Disulfide-rich peptides (DRPs) are ideal scaffolds for drug development and have favorable features for diverse clinical applications. They possess a disulfide-strained core that imparts extraordinary chemical and biological stability characteristics, but also sequence flexibility, allowing the introduction of novel functionalities. We have developed robust and validated design, synthesis and display methods to exploit this scaffold class. This presentation describes an innovative combination of small molecule drug discovery approaches and protein-based molecular evolution strategies guided by structure based drug design to exploit this scaffold class in a diversity, target-class or structure-based context. The versatility of the platform is illustrated by its application to various drug target classes.
Mark Smythe, Ph.D., Founder, Protagonist Therapeutics
10:30
Networking Refreshment Break in Poster and Exhibit Hall
11:15
Phenotypic Screening of Phylomer Libraries to Discover and Validate Targets Using "Protein Interference"
Phylomers are a new class of peptide, derived from genomic fragments of biodiverse microbial species, which encode structural motifs which have evolved within thermostable proteins. Phylomers have been identified with potent activity against diverse classes of intracellular targets and extracellular targets. The enormous structural diversity allows for direct phenotypic screening in mammalian or bacterial cells. The high affinity of Phylomer hits then allows for the identification of targets using pull-down mass spectroscopy approaches. The Phylomer hits can then be used as probes to validate those targets. Unlike the complementary technique of siRNA interference, such 'protein interference' with Phylomers operates at the protein level and therefore can be used to map vulnerable interfaces on potential target proteins which could provide opportunities for therapeutic intervention with peptides or other molecules. The application of Phylomers for target discovery and validation is being pursued by Phylogica's new spin-off with Cambridge University, "Phenomica".
Paul Watt, Ph.D., Non-Executive Director, Phenomica; CEO, Phylogica, Australia
Phylomers are a new class of peptide, derived from genomic fragments of biodiverse microbial species, which encode structural motifs which have evolved within thermostable proteins. Phylomers have been identified with potent activity against diverse classes of intracellular targets and extracellular targets. The enormous structural diversity allows for direct phenotypic screening in mammalian or bacterial cells. The high affinity of Phylomer hits then allows for the identification of targets using pull-down mass spectroscopy approaches. The Phylomer hits can then be used as probes to validate those targets. Unlike the complementary technique of siRNA interference, such 'protein interference' with Phylomers operates at the protein level and therefore can be used to map vulnerable interfaces on potential target proteins which could provide opportunities for therapeutic intervention with peptides or other molecules. The application of Phylomers for target discovery and validation is being pursued by Phylogica's new spin-off with Cambridge University, "Phenomica".
Paul Watt, Ph.D., Non-Executive Director, Phenomica; CEO, Phylogica, Australia
11:45
Peptide Lead Optimization using Solid-phase Peptide Arrays
This lecture highlights a number of key examples of successful lead optimization of peptide drug candidates using surface-immobilized peptide arrays. The technology allows for systematic screening of 10,000 - 100,000 of different AA-variants of lead peptide sequences that resulted in up to a 100~fold activity enhancements.
Peter Timmerman, Ph.D., Chief Technology Officer, Pepscan Therapeutics, The Netherlands
This lecture highlights a number of key examples of successful lead optimization of peptide drug candidates using surface-immobilized peptide arrays. The technology allows for systematic screening of 10,000 - 100,000 of different AA-variants of lead peptide sequences that resulted in up to a 100~fold activity enhancements.
Peter Timmerman, Ph.D., Chief Technology Officer, Pepscan Therapeutics, The Netherlands
12:15
Design of Novel Multivalent Ligands for the Treatment of Neuropathic Pain Which Cross the BBB and are Non-toxic and Non-addictive
Current methods for treating prolonged and neuropathic pain using opioids, NSAIDs and other modalities are generally unsuccessful due to problems of efficacy and toxicity. Utilizing insights obtained from changes in the expressed genomes that accompany these diseases, we have designed multivalent peptide and peptidomimetic ligands that interact with two or more receptors/acceptors and ameliorate these pain states without the problems and toxicities of current drugs such as tolerance, cardiovascular effects, development of dependency, addiction and inhibition of gut motility.
Victor J. Hruby, Ph.D., Regents Professor, Department of Chemistry and Biochemistry, University of Arizona
Current methods for treating prolonged and neuropathic pain using opioids, NSAIDs and other modalities are generally unsuccessful due to problems of efficacy and toxicity. Utilizing insights obtained from changes in the expressed genomes that accompany these diseases, we have designed multivalent peptide and peptidomimetic ligands that interact with two or more receptors/acceptors and ameliorate these pain states without the problems and toxicities of current drugs such as tolerance, cardiovascular effects, development of dependency, addiction and inhibition of gut motility.
Victor J. Hruby, Ph.D., Regents Professor, Department of Chemistry and Biochemistry, University of Arizona
12:45
Networking Luncheon in Poster and Exhibit Hall
1:55
Chairman's Remarks
Thomas Vorherr Ph.D., Director Peptide Discovery, Novartis Pharma AG, Switzerland
Thomas Vorherr Ph.D., Director Peptide Discovery, Novartis Pharma AG, Switzerland
Peptides in Early Development and New Frontiers in Peptide R&D
2:15
First Non-hormonal Therapeutic Candidate for Endometriosis
Endometriosis is estimated to affect 5-10% of women of reproductive age and causes infertility in about 50% of afflicted women. Our target is found to be upregulated in endometriotic lesions and is known to increase the transcription of Estrogen Receptor-α, Matrix Metalloproteinases and cell growth. We have discovered and developed a peptide which specifically targets protein affecting endometriosis proliferation. Presented cellular and animal data demonstrates inhibition of lesion growth of endometriosis by targeting angiogenesis.
Vinay K. Singh, Ph.D., Assistant Professor, Department of Biomedical and Molecular Sciences, Queen's University, Canada
Endometriosis is estimated to affect 5-10% of women of reproductive age and causes infertility in about 50% of afflicted women. Our target is found to be upregulated in endometriotic lesions and is known to increase the transcription of Estrogen Receptor-α, Matrix Metalloproteinases and cell growth. We have discovered and developed a peptide which specifically targets protein affecting endometriosis proliferation. Presented cellular and animal data demonstrates inhibition of lesion growth of endometriosis by targeting angiogenesis.
Vinay K. Singh, Ph.D., Assistant Professor, Department of Biomedical and Molecular Sciences, Queen's University, Canada
2:45
ShK-186 from Discovery to Clinical Development
The potassium channel Kv1.3 has been evolving as a viable drug target since its discovery in the mid-1980's. The unique Kv1.3 high phenotype which characterizes patients with autoimmune diseases makes this channel a novel therapeutic target for treating these disorders. Peptides isolated from scorpion venom and sea anemone nematocysts have potent Kv1.3 blocking activities which make them attractive candidates for clinical development. In particular, ShK, a peptide blocker isolated from the anemone Stichodactyla heliantus, has been extensively studied and a clinical candidate has emerged and recently started Phase Ia trials earlier this year. This lecture describes our research program which has resulted in the first in-class drug, ShK-186, targeting Kv1.3 for treatment of multiple sclerosis.
Michael Pennington, Ph.D., President and COO, Peptides International
The potassium channel Kv1.3 has been evolving as a viable drug target since its discovery in the mid-1980's. The unique Kv1.3 high phenotype which characterizes patients with autoimmune diseases makes this channel a novel therapeutic target for treating these disorders. Peptides isolated from scorpion venom and sea anemone nematocysts have potent Kv1.3 blocking activities which make them attractive candidates for clinical development. In particular, ShK, a peptide blocker isolated from the anemone Stichodactyla heliantus, has been extensively studied and a clinical candidate has emerged and recently started Phase Ia trials earlier this year. This lecture describes our research program which has resulted in the first in-class drug, ShK-186, targeting Kv1.3 for treatment of multiple sclerosis.
Michael Pennington, Ph.D., President and COO, Peptides International
3:15
Networking Refreshment Break
3:45
From Discovery to the Clinic: Applications of Protein Epitope Mimetics
Protein Epitope Mimetics (PEM) Technology has emerged as a powerful approach to identify potent and selective modulators of protein-protein interactions (PPIs). This presentation describes successful case studies of applying the PEM approach from discovery to the clinic. POL7080 is a first in class novel anti-pseudomonal antibiotic with a novel mode of action which has successfully completed Phase I. POL6326, a novel potent and selective CXCR4 antagonist, is the most advanced PEM molecule and is currently in Phase II clinical trials for stem cell transplantation.
Daniel Obrecht, Ph.D., Chief Scientific Officer, Polyphor, Switzerland
Protein Epitope Mimetics (PEM) Technology has emerged as a powerful approach to identify potent and selective modulators of protein-protein interactions (PPIs). This presentation describes successful case studies of applying the PEM approach from discovery to the clinic. POL7080 is a first in class novel anti-pseudomonal antibiotic with a novel mode of action which has successfully completed Phase I. POL6326, a novel potent and selective CXCR4 antagonist, is the most advanced PEM molecule and is currently in Phase II clinical trials for stem cell transplantation.
Daniel Obrecht, Ph.D., Chief Scientific Officer, Polyphor, Switzerland
4:15
Accurate In Vivo Cancer Identification Using Protease-triggered Fluorescent Peptides
Identifying cancerous tissue during surgery is critical for making real-time decisions such as determining which tissue to remove and assessing the spread of cancer. We have generated in vivo optimized fluorescent peptides that utilize pathological protease activity to identify cancerous tissue. In combination with fluorescence imaging instrumentation, these peptide agents visualize cancer with high diagnostic performance and have the potential to aid the oncologic surgeon.
Jesus "Tito" Gonzalez, Ph.D., Chief Scientific Officer, Avelas Biosciences
Identifying cancerous tissue during surgery is critical for making real-time decisions such as determining which tissue to remove and assessing the spread of cancer. We have generated in vivo optimized fluorescent peptides that utilize pathological protease activity to identify cancerous tissue. In combination with fluorescence imaging instrumentation, these peptide agents visualize cancer with high diagnostic performance and have the potential to aid the oncologic surgeon.
Jesus "Tito" Gonzalez, Ph.D., Chief Scientific Officer, Avelas Biosciences
4:45
Peptides for Diagnostic Imaging and Targeted Radionuclide Therapy: A Theranostic Approach
Theranostic radio-tracers for cancer diagnosis and therapy combine a therapeutic agent with a diagnostic test to allow truly individualised tumour treatment. 3B Pharmaceuticals specialises in the development of proprietary innovative peptide-based and peptidomimetic cancer theranostics, exemplified by its neurotensin receptor-specific tracers for the diagnosis and treatment of highly aggressive pancreatic adenocarcinoma.
Ulrich Reineke, Ph.D., CEO and Co-Founder, 3B Pharmaceuticals, Germany
Theranostic radio-tracers for cancer diagnosis and therapy combine a therapeutic agent with a diagnostic test to allow truly individualised tumour treatment. 3B Pharmaceuticals specialises in the development of proprietary innovative peptide-based and peptidomimetic cancer theranostics, exemplified by its neurotensin receptor-specific tracers for the diagnosis and treatment of highly aggressive pancreatic adenocarcinoma.
Ulrich Reineke, Ph.D., CEO and Co-Founder, 3B Pharmaceuticals, Germany
5:45
Close of TIDES
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