In conversation with Peter Macheroux

Review Biochemistry & Molecular Biology

The emerging role of dipeptidyl peptidase 3 in pathophysiology

Grazia Malovan et al.

Summary: This review focuses on recent advances in understanding the structure, catalytic activity, and physiological relevance of Dipeptidyl peptidase 3 (DPP3). The article highlights the broader role of DPP3 as a valuable biomarker in cardiovascular and renal pathologies, as well as its potential as a promising drug target.

FEBS JOURNAL (2023)

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Article Biochemistry & Molecular Biology

Design and synthesis of efficient fluororethylene-peptidomimetic inhibitors of dipeptidyl peptidase III (DPP3)

Harald Podversnik et al.

Summary: DPP3 is a widely expressed enzyme involved in various physiological processes. We have designed peptide-based inhibitors to effectively inhibit the activity of DPP3.

BIOORGANIC & MEDICINAL CHEMISTRY (2022)

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Article Chemistry, Multidisciplinary

Efficient Entropy-Driven Inhibition of Dipeptidyl Peptidase III by Hydroxyethylene Transition-State Peptidomimetics

Jakov Ivkovic et al.

Summary: This study reports on the design, synthesis, and characterization of peptidomimetic inhibitors targeting DPP3 using a hydroxyethylene transition-state mimetic. The inhibitors mimic the VVYPW-motif of tynorphin and show efficient inhibition of DPP3 in low mu M range. Biophysical characterization confirms the unusual entropy-driven mode of binding.

CHEMISTRY-A EUROPEAN JOURNAL (2021)

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Article Microbiology