Medicinal Chemistry

JPT’s Medicinal Chemistry unit has long standing experience from discovery to preclinical development projects. The team members have been critically involved in several peptide and small molecule hit-to-lead qualification and peptide optimization projects.
Medicinal Chemistry at JPT is supported by an extraordinarily high capacity in peptide chemistry, automated synthesis, analytics and purification. By using solid as well as solution phase chemistry, JPT is able to synthesize as many as 50 000 crude and several hundred purified peptides per week.
JPT is in possession of an extensive collection of building blocks and routinely does many types of peptide modifications and conjugations. Besides that, JPT has collected a significant know-how in conformational stabilization and size reduction of peptides, which is used to optimize compounds to finally meet the predefined target product profile.

Applications

Applications

  • Peptide drug discovery
  • Peptide optimization (activity, PhysChem, size)
  • Peptide substrate qualification
  • Optimization of mimotopes for therapeutic protein purification

References

References

  • Detection of Neurodegenerative Diseases
    Saliha et al. US 2019/0094246
  • Peptide Mimotopes of the Cd3 T-Cell Co-Receptor Epsilon Chain and Uses Thereof
    Sahin et al. WO 2017/008844
  • Peptide Mimotopes of Claudin 18.2 and Uses Thereof
    Sahin et al.  WO 2015/113576
  • Peptide microarrays enable rapid mimotope optimization for pharmacokinetic analysis of the novel therapeutic antibody IMAB362
    Schnatbaum et al. Biotechnol. J. (2014)
  • An Acetylome Peptide Microarray Reveals Specificities and Deacetylation Substrates for all Human Sirtuin Isoforms
    Rauh et al. Nat Commun. (2013)
  • Novel Small Molecule Bradykinin B1 Receptor Antagonists. Part 3: Hydroxyurea Derivatives
    Schnatbaum et al., Bioorg. Med. Chem. Lett. (2010) - PMID: 20036120
  • Novel Small Molecule Bradykinin B1 Receptor Antagonists. Part 2: 5-Membered Diaminoheterocycles
    Zischinsky, Schnatbaum et al., Bioorg. Med. Chem. Lett. (2010) - PMID: 20015651
  • Novel Small Molecule Bradykinin B1 Receptor Antagonists. Part 1: Benzamides and Semicarbazides
    Schaudt, Schnatbaum et al., Bioorg. Med. Chem. Lett. (2010) - PMID: 20015645
  • Small Molecule Bradykinin B2 Receptor Modulators
    Gibson, Schnatbaum et al., WO 2010/031589 (2010)
  • TFPI Inhibitors and Methods of Use
    Dockal, Reimer et al., WO 2010/071894 (2010)
  • Small Molecule Antagonists of the Bradykinin B1 Receptor
    Locardi, Reimer et al., WO002009036996 (2009)
  • Peptide Arrays for Enzyme Profiling
    Thiele, Zerweck et al., Methods Mol. Biol. (2009) - PMID: 19649588
  • Design and Synthesis of a New Class of Selective Integrin Alpha5beta1 Antagonists
    Stragies, Reimer et al. J. Med. Chem. 50 (2007) - PMID: 17616113
  • Novel Small Molecule Bradykinin B2 Receptor Antagonists
    Gibson, Schnatbaum et al., J. Med. Chem. (2009) - PMID: 19552431
  • Peptidomimetic C5a Receptor Antagonists with Hydrophobic Substitutions at the C-terminus: Increased Receptor Specificity and in vivo Activity
    Schnatbaum et al., Bioorg. Med. Chem. Lett. (2006) - PMID: 16876401
  • 8-Oxy-Quinoline Derivatives as Bradykinin B2 Receptor Modulators
    Gibson, Schnatbaum et al., WO08116620 (2008)
  • C5A Receptor Antagonists
    Schnatbaum et al., WO06074964 (2006)
  • C5A Receptor Antagonists
    Schnatbaum et al., WO05010030 (2005)
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