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Page 1
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: jansen c. Sci Transl Med. 2024 Oct 23;16(770):eadm8631. doi: 10.1126/scitranslmed.adm8631. Epub 2024 Oct 23. Sci Transl Med. 2024. PMID: 39441903
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: jansen 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.
Discovery and Optimization of 5-Amino-1,2,3-triazole-4-carboxamide Series against Trypanosoma cruzi.
Brand S, Ko EJ, Viayna E, Thompson S, Spinks D, Thomas M, Sandberg L, Francisco AF, Jayawardhana S, Smith VC, Jansen C, De Rycker M, Thomas J, MacLean L, Osuna-Cabello M, Riley J, Scullion P, Stojanovski L, Simeons FRC, Epemolu O, Shishikura Y, Crouch SD, Bakshi TS, Nixon CJ, Reid IH, Hill AP, Underwood TZ, Hindley SJ, Robinson SA, Kelly JM, Fiandor JM, Wyatt PG, Marco M, Miles TJ, Read KD, Gilbert IH. Brand S, et al. Among authors: jansen c. J Med Chem. 2017 Sep 14;60(17):7284-7299. doi: 10.1021/acs.jmedchem.7b00463. Epub 2017 Aug 27. J Med Chem. 2017. PMID: 28844141 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: jansen 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.
Lysyl-tRNA synthetase, a target for urgently needed M. tuberculosis drugs.
Green SR, Davis SH, Damerow S, Engelhart CA, Mathieson M, Baragaña B, Robinson DA, Tamjar J, Dawson A, Tamaki FK, Buchanan KI, Post J, Dowers K, Shepherd SM, Jansen C, Zuccotto F, Gilbert IH, Epemolu O, Riley J, Stojanovski L, Osuna-Cabello M, Pérez-Herrán E, Rebollo MJ, Guijarro López L, Casado Castro P, Camino I, Kim HC, Bean JM, Nahiyaan N, Rhee KY, Wang Q, Tan VY, Boshoff HIM, Converse PJ, Li SY, Chang YS, Fotouhi N, Upton AM, Nuermberger EL, Schnappinger D, Read KD, Encinas L, Bates RH, Wyatt PG, Cleghorn LAT. Green SR, et al. Among authors: jansen c. Nat Commun. 2022 Oct 11;13(1):5992. doi: 10.1038/s41467-022-33736-5. Nat Commun. 2022. PMID: 36220877 Free PMC article.
Molecular basis of RNA guanine-7 methyltransferase (RNMT) activation by RAM.
Varshney D, Petit AP, Bueren-Calabuig JA, Jansen C, Fletcher DA, Peggie M, Weidlich S, Scullion P, Pisliakov AV, Cowling VH. Varshney D, et al. Among authors: jansen c. Nucleic Acids Res. 2016 Dec 1;44(21):10423-10436. doi: 10.1093/nar/gkw637. Epub 2016 Jul 15. Nucleic Acids Res. 2016. PMID: 27422871 Free PMC article.
Structure-Based Discovery of a Series of Covalent, Orally Bioavailable, and Selective BFL1 Inhibitors.
Palisse A, Cheung T, Blokhuis A, Cogswell T, Martins BS, Riemens R, Schellekens R, Battocchio G, Jansen C, Cottee MA, Ornell K, Sacchetto C, Leon L, van Hoek-Emmelot M, Bostock M, Brauer BL, Beaumont K, Lucas SCC, Ahmed S, Blackwell JH, Börjesson U, Gohlke A, Gramatikov IMT, Hargreaves D, van Hoeven V, Kantae V, Kupcova L, Milbradt AG, Seneviratne U, Su N, Vales J, Wang H, White MJ, Kinzel O. Palisse A, et al. Among authors: jansen c. J Med Chem. 2024 Dec 26;67(24):22055-22079. doi: 10.1021/acs.jmedchem.4c01995. Epub 2024 Dec 6. J Med Chem. 2024. PMID: 39641779
Catechol pyrazolinones as trypanocidals: fragment-based design, synthesis, and pharmacological evaluation of nanomolar inhibitors of trypanosomal phosphodiesterase B1.
Orrling KM, Jansen C, Vu XL, Balmer V, Bregy P, Shanmugham A, England P, Bailey D, Cos P, Maes L, Adams E, van den Bogaart E, Chatelain E, Ioset JR, van de Stolpe A, Zorg S, Veerman J, Seebeck T, Sterk GJ, de Esch IJ, Leurs R. Orrling KM, et al. Among authors: jansen c. J Med Chem. 2012 Oct 25;55(20):8745-56. doi: 10.1021/jm301059b. Epub 2012 Oct 8. J Med Chem. 2012. PMID: 22963052
Aging towards walkable futures: insights from a multidisciplinary workshop held in Barcelona, Spain.
Vall-Garcia E, Delgado-Ortiz L, Alcock L, Coll-Planas L, García-Navarro JA, Iwarsson S, Jansà JM, Jansen CP, Koch S, Schwartz S, Rantakokko M, Sarukhan A, van Staalduinen W, Rochester L, Garcia-Aymerich J. Vall-Garcia E, et al. Among authors: jansen cp. BMC Public Health. 2025 Jan 17;25(1):195. doi: 10.1186/s12889-024-21223-z. BMC Public Health. 2025. PMID: 39825288 Free PMC article.
1,187 results