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Page 1
Biochemical and Structural Characterization of Selective Allosteric Inhibitors of the Plasmodium falciparum Drug Target, Prolyl-tRNA-synthetase.
Hewitt SN, Dranow DM, Horst BG, Abendroth JA, Forte B, Hallyburton I, Jansen C, Baragaña B, Choi R, Rivas KL, Hulverson MA, Dumais M, Edwards TE, Lorimer DD, Fairlamb AH, Gray DW, Read KD, Lehane AM, Kirk K, Myler PJ, Wernimont A, Walpole C, Stacy R, Barrett LK, Gilbert IH, Van Voorhis WC. Hewitt SN, et al. Among authors: walpole c. ACS Infect Dis. 2017 Jan 13;3(1):34-44. doi: 10.1021/acsinfecdis.6b00078. Epub 2016 Nov 16. ACS Infect Dis. 2017. PMID: 27798837 Free PMC article.
Lysyl-tRNA synthetase as a drug target in malaria and cryptosporidiosis.
Baragaña B, Forte B, Choi R, Nakazawa Hewitt S, Bueren-Calabuig JA, Pisco JP, Peet C, Dranow DM, Robinson DA, Jansen C, Norcross NR, Vinayak S, Anderson M, Brooks CF, Cooper CA, Damerow S, Delves M, Dowers K, Duffy J, Edwards TE, Hallyburton I, Horst BG, Hulverson MA, Ferguson L, Jiménez-Díaz MB, Jumani RS, Lorimer DD, Love MS, Maher S, Matthews H, McNamara CW, Miller P, O'Neill S, Ojo KK, Osuna-Cabello M, Pinto E, Post J, Riley J, Rottmann M, Sanz LM, Scullion P, Sharma A, Shepherd SM, Shishikura Y, Simeons FRC, Stebbins EE, Stojanovski L, Straschil U, Tamaki FK, Tamjar J, Torrie LS, Vantaux A, Witkowski B, Wittlin S, Yogavel M, Zuccotto F, Angulo-Barturen I, Sinden R, Baum J, Gamo FJ, Mäser P, Kyle DE, Winzeler EA, Myler PJ, Wyatt PG, Floyd D, Matthews D, Sharma A, Striepen B, Huston CD, Gray DW, Fairlamb AH, Pisliakov AV, Walpole C, Read KD, Van Voorhis WC, Gilbert IH. Baragaña B, et al. Among authors: walpole c. Proc Natl Acad Sci U S A. 2019 Apr 2;116(14):7015-7020. doi: 10.1073/pnas.1814685116. Epub 2019 Mar 20. Proc Natl Acad Sci U S A. 2019. PMID: 30894487 Free PMC article.
Bicyclic azetidines kill the diarrheal pathogen Cryptosporidium in mice by inhibiting parasite phenylalanyl-tRNA synthetase.
Vinayak S, Jumani RS, Miller P, Hasan MM, McLeod BI, Tandel J, Stebbins EE, Teixeira JE, Borrel J, Gonse A, Zhang M, Yu X, Wernimont A, Walpole C, Eckley S, Love MS, McNamara CW, Sharma M, Sharma A, Scherer CA, Kato N, Schreiber SL, Melillo B, Striepen B, Huston CD, Comer E. Vinayak S, et al. Among authors: walpole c. Sci Transl Med. 2020 Sep 30;12(563):eaba8412. doi: 10.1126/scitranslmed.aba8412. Sci Transl Med. 2020. PMID: 32998973 Free PMC article.
MalDA, Accelerating Malaria Drug Discovery.
Yang T, Ottilie S, Istvan ES, Godinez-Macias KP, Lukens AK, Baragaña B, Campo B, Walpole C, Niles JC, Chibale K, Dechering KJ, Llinás M, Lee MCS, Kato N, Wyllie S, McNamara CW, Gamo FJ, Burrows J, Fidock DA, Goldberg DE, Gilbert IH, Wirth DF, Winzeler EA; Malaria Drug Accelerator Consortium. Yang T, et al. Among authors: walpole c. Trends Parasitol. 2021 Jun;37(6):493-507. doi: 10.1016/j.pt.2021.01.009. Epub 2021 Feb 26. Trends Parasitol. 2021. PMID: 33648890 Free PMC article. Review.
Chemogenomics identifies acetyl-coenzyme A synthetase as a target for malaria treatment and prevention.
Summers RL, Pasaje CFA, Pisco JP, Striepen J, Luth MR, Kumpornsin K, Carpenter EF, Munro JT, Lin D, Plater A, Punekar AS, Shepherd AM, Shepherd SM, Vanaerschot M, Murithi JM, Rubiano K, Akidil A, Ottilie S, Mittal N, Dilmore AH, Won M, Mandt REK, McGowen K, Owen E, Walpole C, Llinás M, Lee MCS, Winzeler EA, Fidock DA, Gilbert IH, Wirth DF, Niles JC, Baragaña B, Lukens AK. Summers RL, et al. Among authors: walpole c. Cell Chem Biol. 2022 Feb 17;29(2):191-201.e8. doi: 10.1016/j.chembiol.2021.07.010. Epub 2021 Aug 3. Cell Chem Biol. 2022. PMID: 34348113 Free PMC article.
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: walpole c. 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.
Optimization of TAM16, a Benzofuran That Inhibits the Thioesterase Activity of Pks13; Evaluation toward a Preclinical Candidate for a Novel Antituberculosis Clinical Target.
Wilson C, Ray P, Zuccotto F, Hernandez J, Aggarwal A, Mackenzie C, Caldwell N, Taylor M, Huggett M, Mathieson M, Murugesan D, Smith A, Davis S, Cocco M, Parai MK, Acharya A, Tamaki F, Scullion P, Epemolu O, Riley J, Stojanovski L, Lopez-Román EM, Torres-Gómez PA, Toledo AM, Guijarro-Lopez L, Camino I, Engelhart CA, Schnappinger D, Massoudi LM, Lenaerts A, Robertson GT, Walpole C, Matthews D, Floyd D, Sacchettini JC, Read KD, Encinas L, Bates RH, Green SR, Wyatt PG. Wilson C, et al. Among authors: walpole c. J Med Chem. 2022 Jan 13;65(1):409-423. doi: 10.1021/acs.jmedchem.1c01586. Epub 2021 Dec 15. J Med Chem. 2022. PMID: 34910486 Free PMC article.
Development of a Novel Lead that Targets M. tuberculosis Polyketide Synthase 13.
Aggarwal A, Parai MK, Shetty N, Wallis D, Woolhiser L, Hastings C, Dutta NK, Galaviz S, Dhakal RC, Shrestha R, Wakabayashi S, Walpole C, Matthews D, Floyd D, Scullion P, Riley J, Epemolu O, Norval S, Snavely T, Robertson GT, Rubin EJ, Ioerger TR, Sirgel FA, van der Merwe R, van Helden PD, Keller P, Böttger EC, Karakousis PC, Lenaerts AJ, Sacchettini JC. Aggarwal A, et al. Among authors: walpole c. Cell. 2017 Jul 13;170(2):249-259.e25. doi: 10.1016/j.cell.2017.06.025. Epub 2017 Jun 29. Cell. 2017. PMID: 28669536 Free PMC article.
85 results