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Substrate-mimicking peptidomimetics have been developed that potently inhibit plasmepsin V but show modest parasite activity. To advance these inhibitors, we optimized their potency by introducing a 2-chloro aryl group at P2 and an N-terminal sulfonamide that yielded WM960, which showed markedly improved plasmepsin V inhibition while retaining high selectivity over plasmepsin IX and X and human aspartyl proteases. WM960 also demonstrated enhanced activity against asexual blood-stage parasites and effectively suppressed protein export. However, WM960 displayed low metabolic stability and limited systemic exposure in mice, highlighting the need to improve pharmacokinetic properties in future development of peptidomimetic plasmepsin V targeted antimalarials.<\/jats:p>","DOI":"10.1021\/acsinfecdis.6c00314","type":"journal-article","created":{"date-parts":[[2026,8,15]],"date-time":"2026-08-15T15:01:44Z","timestamp":1786806104000},"page":"3114-3126","source":"Crossref","is-referenced-by-count":0,"title":["Activity Refinement\nand Property Assessment of Peptidomimetics\nwith Potent Antimalarial Activity That Target Plasmepsin V"],"prefix":"10.1021","volume":"12","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-3452-7439","authenticated-orcid":true,"given":"Gregory L.","family":"Adams","sequence":"first","affiliation":[{"name":"Merck & Co., Inc. , , ,","place":["West Point, Pennsylvania, United States, 19486"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-9386-0648","authenticated-orcid":true,"given":"Madeline G.","family":"Dans","sequence":"additional","affiliation":[{"name":"The Walter and Eliza Hall Institute of Medical Research , ,","place":["Parkville, Australia, 3052"]},{"name":"The University of Melbourne , , ,","place":["Parkville, Australia, 3010"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Qingmiao","family":"Zhou","sequence":"additional","affiliation":[{"name":"The Walter and Eliza Hall Institute of Medical Research , ,","place":["Parkville, Australia, 3052"]},{"name":"The University of Melbourne , , ,","place":["Parkville, Australia, 3010"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-6400-644X","authenticated-orcid":true,"given":"Wenyin","family":"Su","sequence":"additional","affiliation":[{"name":"The Walter and Eliza Hall Institute of Medical Research , ,","place":["Parkville, Australia, 3052"]},{"name":"The University of Melbourne , , ,","place":["Parkville, Australia, 3010"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Anna","family":"Ngo","sequence":"additional","affiliation":[{"name":"The Walter and Eliza Hall Institute of Medical Research , ,","place":["Parkville, Australia, 3052"]},{"name":"The University of Melbourne , , ,","place":["Parkville, Australia, 3010"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Kate E.","family":"Jarman","sequence":"additional","affiliation":[{"name":"The Walter and Eliza Hall Institute of Medical Research , ,","place":["Parkville, Australia, 3052"]},{"name":"The University of Melbourne , , ,","place":["Parkville, Australia, 3010"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Maria V.","family":"Fawaz","sequence":"additional","affiliation":[{"name":"Merck & Co., Inc. , , ,","place":["West Point, Pennsylvania, United States, 19486"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"suffix":"III","given":"Michael J.","family":"Kelly","sequence":"additional","affiliation":[{"name":"Merck & Co., Inc. , , ,","place":["West Point, Pennsylvania, United States, 19486"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"John A.","family":"McCauley","sequence":"additional","affiliation":[{"name":"Merck & Co., Inc. , , ,","place":["West Point, Pennsylvania, United States, 19486"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"David B.","family":"Olsen","sequence":"additional","affiliation":[{"name":"Merck & Co., Inc. , , ,","place":["West Point, Pennsylvania, United States, 19486"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-7322-2040","authenticated-orcid":true,"given":"Justin A.","family":"Boddey","sequence":"additional","affiliation":[{"name":"The Walter and Eliza Hall Institute of Medical Research , ,","place":["Parkville, Australia, 3052"]},{"name":"The University of Melbourne , , ,","place":["Parkville, Australia, 3010"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Alan F.","family":"Cowman","sequence":"additional","affiliation":[{"name":"The Walter and Eliza Hall Institute of Medical Research , ,","place":["Parkville, Australia, 3052"]},{"name":"The University of Melbourne , , ,","place":["Parkville, Australia, 3010"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-9117-1048","authenticated-orcid":true,"given":"Brad E.","family":"Sleebs","sequence":"additional","affiliation":[{"name":"The Walter and Eliza Hall Institute of Medical Research , ,","place":["Parkville, Australia, 3052"]},{"name":"The University of Melbourne , , ,","place":["Parkville, Australia, 3010"]}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"316","published-online":{"date-parts":[[2026,8,15]]},"reference":[{"issue":"23","key":"2026091109074211800_cit1","doi-asserted-by":"publisher","first-page":"10526","DOI":"10.1021\/acs.jmedchem.9b00761","article-title":"The development\nprocess for discovery and clinical advancement of modern antimalarials","volume":"62","author":"Ashton","year":"2019","journal-title":"J. Med. Chem."},{"issue":"3","key":"2026091109074211800_cit2","doi-asserted-by":"publisher","first-page":"178","DOI":"10.1038\/s41579-024-01099-x","article-title":"Towards next-generation\ntreatment options to combat Plasmodium falciparum malaria","volume":"23","author":"Okombo","year":"2025","journal-title":"Nat. Rev. Microbiol."},{"issue":"10","key":"2026091109074211800_cit3","doi-asserted-by":"publisher","first-page":"807","DOI":"10.1038\/s41573-023-00772-9","article-title":"Antimalarial drug\ndiscovery: progress and approaches","volume":"22","author":"Siqueira-Neto","year":"2023","journal-title":"Nat. Rev.\nDrug Discovery"},{"key":"2026091109074211800_cit4","doi-asserted-by":"crossref","unstructured":"Sleebs, B. E.\n          \n          Plasmepsins\nas antimalarial drug targets-then, now, and the future\n          Med. Res. 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Agents Chemother."},{"issue":"1","key":"2026091109074211800_cit23","doi-asserted-by":"publisher","first-page":"48","DOI":"10.1016\/j.cell.2008.04.051","article-title":"Exported proteins required for virulence\nand rigidity of Plasmodium falciparum-infected human erythrocytes","volume":"134","author":"Maier","year":"2008","journal-title":"Cell"},{"issue":"5703","key":"2026091109074211800_cit24","doi-asserted-by":"publisher","first-page":"1930","DOI":"10.1126\/science.1102452","article-title":"Targeting\nmalaria virulence and remodeling proteins to the host erythrocyte","volume":"306","author":"Marti","year":"2004","journal-title":"Science"},{"issue":"2","key":"2026091109074211800_cit25","doi-asserted-by":"publisher","DOI":"10.1186\/gb-2006-7-2-r12","article-title":"Lineage-specific\nexpansion of proteins\nexported to erythrocytes in malaria parasites","volume":"7","author":"Sargeant","year":"2006","journal-title":"Genome Biol."},{"issue":"5","key":"2026091109074211800_cit26","doi-asserted-by":"publisher","first-page":"532","DOI":"10.1111\/tra.12053","article-title":"Role of\nplasmepsin V in export of diverse protein families from the Plasmodium falciparum exportome","volume":"14","author":"Boddey","year":"2013","journal-title":"Traffic"},{"issue":"5703","key":"2026091109074211800_cit27","doi-asserted-by":"publisher","first-page":"1934","DOI":"10.1126\/science.1102737","article-title":"A host-targeting signal in virulence\nproteins reveals a secretome in malarial infection","volume":"306","author":"Hiller","year":"2004","journal-title":"Science"},{"issue":"2","key":"2026091109074211800_cit28","doi-asserted-by":"publisher","first-page":"107","DOI":"10.1016\/j.molbiopara.2008.04.011","article-title":"N-terminal processing\nof proteins exported by malaria\nparasites","volume":"160","author":"Chang","year":"2008","journal-title":"Mol. Biochem. Parasitol."},{"issue":"7281","key":"2026091109074211800_cit29","doi-asserted-by":"publisher","first-page":"627","DOI":"10.1038\/nature08728","article-title":"An aspartyl protease\ndirects malaria effector proteins to the host cell","volume":"463","author":"Boddey","year":"2010","journal-title":"Nature"},{"issue":"7281","key":"2026091109074211800_cit30","doi-asserted-by":"publisher","first-page":"632","DOI":"10.1038\/nature08726","article-title":"Plasmepsin V licenses Plasmodium proteins\nfor export into the host erythrocyte","volume":"463","author":"Russo","year":"2010","journal-title":"Nature"},{"issue":"6","key":"2026091109074211800_cit31","doi-asserted-by":"publisher","DOI":"10.1242\/jcs.260551","article-title":"An essential endoplasmic reticulum-resident\nN-acetyltransferase ortholog in Plasmodium falciparum","volume":"136","author":"Polino","year":"2023","journal-title":"J. Cell. 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Chem."},{"issue":"9","key":"2026091109074211800_cit44","doi-asserted-by":"publisher","first-page":"1993","DOI":"10.1016\/j.bmc.2016.03.027","article-title":"Exploration\nof the P3 region of PEXEL peptidomimetics leads to a potent inhibitor\nof the Plasmodium protease, plasmepsin V","volume":"24","author":"Gazdik","year":"2016","journal-title":"Bioorg. Med. 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