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Identification and Optimization of Novel Inhibitors of the Polyketide Synthase 13 Thioesterase Domain with Antitubercular Activity.
Green SR, Wilson C, Eadsforth TC, Punekar AS, Tamaki FK, Wood G, Caldwell N, Forte B, Norcross NR, Kiczun M, Post JM, Lopez-Román EM, Engelhart CA, Lukac I, Zuccotto F, Epemolu O, Boshoff HIM, Schnappinger D, Walpole C, Gilbert IH, Read KD, Wyatt PG, Baragaña B. Green SR, et al. Among authors: lukac i. J Med Chem. 2023 Nov 23;66(22):15380-15408. doi: 10.1021/acs.jmedchem.3c01514. Epub 2023 Nov 10. J Med Chem. 2023. PMID: 37948640 Free PMC article.
Cryptosporidium lysyl-tRNA synthetase inhibitors define the interplay between solubility and permeability required to achieve efficacy.
Caldwell N, Peet C, Miller P, Colon BL, Taylor MG, Cocco M, Dawson A, Lukac I, Teixeira JE, Robinson L, Frame L, Seizova S, Damerow S, Tamaki F, Post J, Riley J, Mutter N, Hanna JC, Ferguson L, Hu X, Tinti M, Forte B, Norcross NR, Campbell PS, Svensen N, Caldwell FC, Jansen C, Postis V, Read KD, Huston CD, Gilbert IH, Baragaña B, Pawlowic MC. Caldwell N, et al. Among authors: lukac i. Sci Transl Med. 2024 Oct 23;16(770):eadm8631. doi: 10.1126/scitranslmed.adm8631. Epub 2024 Oct 23. Sci Transl Med. 2024. PMID: 39441903
DNDI-6148: A Novel Benzoxaborole Preclinical Candidate for the Treatment of Visceral Leishmaniasis.
Mowbray CE, Braillard S, Glossop PA, Whitlock GA, Jacobs RT, Speake J, Pandi B, Nare B, Maes L, Yardley V, Freund Y, Wall RJ, Carvalho S, Bello D, Van den Kerkhof M, Caljon G, Gilbert IH, Corpas-Lopez V, Lukac I, Patterson S, Zuccotto F, Wyllie S. Mowbray CE, et al. Among authors: lukac i. J Med Chem. 2021 Nov 11;64(21):16159-16176. doi: 10.1021/acs.jmedchem.1c01437. Epub 2021 Oct 28. J Med Chem. 2021. PMID: 34711050 Free PMC article.
Scaffold-Hopping Strategy on a Series of Proteasome Inhibitors Led to a Preclinical Candidate for the Treatment of Visceral Leishmaniasis.
Thomas M, Brand S, De Rycker M, Zuccotto F, Lukac I, Dodd PG, Ko EJ, Manthri S, McGonagle K, Osuna-Cabello M, Riley J, Pont C, Simeons F, Stojanovski L, Thomas J, Thompson S, Viayna E, Fiandor JM, Martin J, Wyatt PG, Miles TJ, Read KD, Marco M, Gilbert IH. Thomas M, et al. Among authors: lukac i. J Med Chem. 2021 May 13;64(9):5905-5930. doi: 10.1021/acs.jmedchem.1c00047. Epub 2021 Apr 27. J Med Chem. 2021. PMID: 33904304 Free PMC article.
44 results