Peptides and Peptiomimetics in Drug Discovery
In this research area, we are interested in the process of using bioactive peptides as starting points in drug discovery. We have been focusing on the design and synthesis of protease inhibitors for viral diseases, as well as of peptidomimetics of neuropeptides for treatment of neuropathic pain. In parallel to our efforts to rationally transform peptides into orally bioavailable and drug-like molecules we aim at the development of novel methods for synthesis of modified peptides, radiolabeled peptides, peptidomimetic scaffolds, and carboxylic acid bioisosteres; useful within organic synthesis and solid-phase peptide synthesis (SPPS).
Publications
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Ultralarge Virtual Screening Identifies SARS-CoV-2 Main Protease Inhibitors with Broad-Spectrum Activity against Coronaviruses.
(2022). Journal of the American Chemical Society, . vol. 144, ss. 2905-2920 DOI -
Targeting the NS2B-NS3 protease of tick-borne encephalitis virus with pan-flaviviral protease inhibitors.
(2021). Antiviral Research, . vol. 190 DOI -
Antibacterial sulfonimidamide-based oligopeptides as type I signal peptidase inhibitors: Synthesis and biological evaluation.
(2021). European Journal of Medicinal Chemistry, . vol. 224 DOI -
The amino-terminal heptapeptide of the algesic substance P provides analgesic effect in relieving chronic neuropathic pain.
(2021). European Journal of Pharmacology, . vol. 892 DOI -
Identification of a C2-symmetric diol based human immunodeficiency virus protease inhibitor targeting Zika virus NS2B-NS3 protease.
(2020). Journal of Biomolecular Structure and Dynamics, vol. 38, ss. 5526-5536 DOI -
Solid Phase Synthesis of Sulfonimidamide Pseudopeptides and Library Generation.
(2020). European Journal of Organic Chemistry, . vol. 2020, ss. 3796-3807 DOI -
Macrocyclic Peptidomimetics as Inhibitors of Insulin-Regulated Aminopeptidase (IRAP).
(2020). RSC Medicinal chemistry, vol. 11, ss. 234-244 DOI -
Synthesis of Sulfonimidamide-Based Amino Acid Building Blocks with Orthogonal Protecting Groups.
(2019). European Journal of Organic Chemistry, . ss. 1045-1057 DOI -
From the Anti-Nociceptive Substance P Metabolite Substance P (1-7) to Small Peptidomimetics.
(2018). Current protein and peptide science, vol. 19, ss. 1038-1048 DOI -
An imidazole based H-Phe-Phe-NH2 peptidomimetic with anti-allodynic effect in spared nerve injury mice.
(2018). Bioorganic & Medicinal Chemistry Letters, vol. 28, ss. 2446-2450 DOI