{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Previti S"],"funding":["University of Messina"],"pagination":["3765"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC9229991"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["27(12)"],"pubmed_abstract":["Human African Trypanosomiasis (HAT) is an endemic protozoan disease widespread in the sub-Saharan region that is caused by <i>T. b. gambiense</i> and <i>T. b. rhodesiense</i>. The development of molecules targeting rhodesain, the main cysteine protease of <i>T. b. rhodesiense</i>, has led to a panel of inhibitors endowed with micro/sub-micromolar activity towards the protozoa. However, whilst impressive binding affinity against rhodesain has been observed, the limited selectivity towards the target still remains a hard challenge for the development of antitrypanosomal agents. In this paper, we report the synthesis, biological evaluation, as well as docking studies of a series of reduced peptide bond pseudopeptide Michael acceptors (<b>SPR10</b>-<b>SPR19</b>) as potential anti-HAT agents. T"],"journal":["Molecules (Basel, Switzerland)"],"pubmed_title":["Development of Reduced Peptide Bond Pseudopeptide Michael Acceptors for the Treatment of Human African Trypanosomiasis."],"pmcid":["PMC9229991"],"funding_grant_id":["FFABR 2020"],"pubmed_authors":["Bogacz M","Cosconati S","Di Chio C","Ettari R","Previti S","Ravichandran R","Schirmeister T","Hellmich UA","Zappala M"],"additional_accession":[]},"is_claimable":false,"name":"Development of Reduced Peptide Bond Pseudopeptide Michael Acceptors for the Treatment of Human African Trypanosomiasis.","description":"Human African Trypanosomiasis (HAT) is an endemic protozoan disease widespread in the sub-Saharan region that is caused by <i>T. b. gambiense</i> and <i>T. b. rhodesiense</i>. The development of molecules targeting rhodesain, the main cysteine protease of <i>T. b. rhodesiense</i>, has led to a panel of inhibitors endowed with micro/sub-micromolar activity towards the protozoa. However, whilst impressive binding affinity against rhodesain has been observed, the limited selectivity towards the target still remains a hard challenge for the development of antitrypanosomal agents. In this paper, we report the synthesis, biological evaluation, as well as docking studies of a series of reduced peptide bond pseudopeptide Michael acceptors (<b>SPR10</b>-<b>SPR19</b>) as potential anti-HAT agents. T","dates":{"release":"2022-01-01T00:00:00Z","publication":"2022 Jun","modification":"2025-05-29T19:47:07.642Z","creation":"2025-04-05T07:15:36.912Z"},"accession":"S-EPMC9229991","cross_references":{"pubmed":["35744891"],"doi":["10.3390/molecules27123765"]}}