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

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

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)