Crystallographic analysis of Anticalin® targeting CTLA-4 confirms the excellent suitability of Pieris' lipocalin scaffold to develop superior biotherapeutics
Freising-Weihenstephan/Germany (ots) - Crystallographic analysis of Anticalin® targeting CTLA-4 confirms the excellent suitability of Pieris' lipocalin scaffold to develop superior biotherapeutics
Pieris AG, a biopharmaceutical company developing therapeutic products comprising Anticalins®, a novel proprietary class of human binding proteins, announced today that it has reached key technological milestones for its proprietary lead projects PRS-010 and PRS-050, targeting CTLA-4 and VEGF, respectively. Analysis of the three-dimensional crystal structure of a target-specific Anticalin® in complex with its ligand confirms the previously predicted plasticity and the superior potential of the human lipocalin scaffold for the generation of targeted therapeutics.
PRS-010 acts as an antagonist to the T-cell specific 'immune brake' receptor CTLA-4 by tight complex formation with its extracellular region. By blocking the function of this immunological co-receptor in a directed manner, T-cell activation may ultimately be harnessed as an effective mechanism for the treatment of a wide range of tumors. PRS-050 inhibits the biological activity of VEGF due to its sub-nanomolar affinity for this soluble key angiogenic factor in conjunction with its effective epitope specificity. Several Anticalin(r)-specific advantages will be capitalized in this program to develop a superior biotherapeutic inhibiting tumor angiogenesis as well as retinal neovascularization.
"Our structural findings clearly confirm Pieris' concept of employing lipocalins with their hypervariable loop region as a human protein scaffold for developing Anticalins® that tightly bind to prescribed targets", says Prof. Arne Skerra from the Technical University of Munich, Germany, and co-founder of Pieris.
"The high level of structural complementarity of the Anticalin® with functionally important regions of the therapeutic target explains the observed antagonistic mode of action on the structural level and confirms our project development efforts", comments Dr Andreas Hohlbaum, Director of Science and Preclinical Development of Pieris.
Notes to editors
About Pieris AG
Pieris is a biopharmaceutical company engaged in the discovery and development of Anticalins® for the diagnosis and treatment of life-threatening human disorders. Exploiting extensive know-how in protein engineering as part of a broad intellectual property portfolio, the Company applies a balanced risk business model to the development of its Anticalin® candidates. Recognizing the enormous market potential of protein-based drugs, Pieris is committed to becoming an integrated drug discovery and development company.
About the Anticalin® technology
Anticalins® as engineered human proteins with prescribed binding properties are derived from the lipocalin scaffold and exhibit fundamental similarities with fully human antibodies e.g. picomolar potency and expected low immunogenicity. Anticalins(r) have several additional advantages over conventional antibodies due to their small size, robust tertiary structure and straight composition that confers high solubility, predictable stability and beneficial economy of production. Fast pharmacokinetics and favourable tissue penetration of Anticalins® can be balanced with adjustable modulation of serum half-life by established methodologies.
By developing Anticalin® based products, Pieris and its collaborators are not only able to develop superior biotherapeutics, but they will also have the ability to overcome the encumbering patent landscape as currently present for developing conventional antibodies. To date, Pieris has reached all development milestones under the agreements with its industry partners on time.
Further information is available at http://www.pieris-ag.com
VEGF: Vascular Endothelial Growth Factor
Anticalin®, Anticalins® are registered trademarks of Pieris AG.
ots Originaltext: Pieris AG
Dr Andreas Hohlbaum
Dir. of Science & Preclin. Dev.
Phone +49/8161-1411- 400