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Page 1
Macrolide Inspired Macrocycles as Modulators of the IL-17A/IL-17RA Interaction.
Koštrun S, Fajdetić A, Pešić D, Brajša K, Bencetić Mihaljević V, Jelić D, Petrinić Grba A, Elenkov I, Rupčić R, Kapić S, Ozimec Landek I, Butković K, Grgičević A, Žiher D, Čikoš A, Padovan J, Saxty G, Dack K, Bladh H, Skak-Nielsen T, Feldbaek Nielsen S, Lambert M, Stahlhut M. Koštrun S, et al. Among authors: saxty g. J Med Chem. 2021 Jun 24;64(12):8354-8383. doi: 10.1021/acs.jmedchem.1c00327. Epub 2021 Jun 8. J Med Chem. 2021. PMID: 34100601
Current Trends in Macrocyclic Drug Discovery and beyond-Ro5.
Alihodžić S, Bukvić M, Elenkov IJ, Hutinec A, Koštrun S, Pešić D, Saxty G, Tomašković L, Žiher D. Alihodžić S, et al. Among authors: saxty g. Prog Med Chem. 2018;57(1):113-233. doi: 10.1016/bs.pmch.2018.01.002. Epub 2018 Mar 22. Prog Med Chem. 2018. PMID: 29680148 Review.
Novel Macrocyclic Antagonists of the Calcitonin Gene-Related Peptide Receptor: Design, Realization, and Structural Characterization of Protein-Ligand Complexes.
Cansfield AD, Ator MA, Banerjee J, Bestwick M, Bortolato A, Brown GA, Brown J, Butkovic K, Cansfield JE, Christopher JA, Congreve M, Cseke G, Deflorian F, Dugan B, Hunjadi MP, Hutinec A, Inturi TK, Landek G, Mason J, O'Brien A, Ott GR, Rupcic R, Saxty G, Southall SM, Zadravec R, Watson SP. Cansfield AD, et al. Among authors: saxty g. ACS Chem Neurosci. 2022 Mar 16;13(6):751-765. doi: 10.1021/acschemneuro.1c00696. Epub 2022 Mar 4. ACS Chem Neurosci. 2022. PMID: 35245037
Novel Macrocyclic Antagonists of the CGRP Receptor Part 2: Stereochemical Inversion Induces an Unprecedented Binding Mode.
Southall SM, Banerjee J, Brown J, Butkovic K, Cansfield AD, Cansfield JE, Congreve MS, Cseke G, Deflorian F, Hunjadi MP, Hutinec A, Inturi TK, Rupcic R, Saxty G, Watson SP. Southall SM, et al. Among authors: saxty g. ACS Med Chem Lett. 2022 Oct 19;13(11):1776-1782. doi: 10.1021/acsmedchemlett.2c00400. eCollection 2022 Nov 10. ACS Med Chem Lett. 2022. PMID: 36385934 Free PMC article.
Structure-Activity and Structure-Conformation Relationships of Aryl Propionic Acid Inhibitors of the Kelch-like ECH-Associated Protein 1/Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1/NRF2) Protein-Protein Interaction.
Heightman TD, Callahan JF, Chiarparin E, Coyle JE, Griffiths-Jones C, Lakdawala AS, McMenamin R, Mortenson PN, Norton D, Peakman TM, Rich SJ, Richardson C, Rumsey WL, Sanchez Y, Saxty G, Willems HMG, Wolfe L 3rd, Woolford AJ, Wu Z, Yan H, Kerns JK, Davies TG. Heightman TD, et al. Among authors: saxty g. J Med Chem. 2019 May 9;62(9):4683-4702. doi: 10.1021/acs.jmedchem.9b00279. Epub 2019 Apr 25. J Med Chem. 2019. PMID: 30973731
The exploration of aza-quinolines as hematopoietic prostaglandin D synthase (H-PGDS) inhibitors with low brain exposure.
Cadilla R, Deaton DN, Do Y, Elkins PA, Ennulat D, Guss JH, Holt J, Jeune MR, King AG, Klapwijk JC, Kramer HF, Kramer NJ, Laffan SB, Masuria PI, McDougal AV, Mortenson PN, Musetti C, Peckham GE, Pietrak BL, Poole C, Price DJ, Rendina AR, Sati G, Saxty G, Shearer BG, Shewchuk LM, Sneddon HF, Stewart EL, Stuart JD, Thomas DN, Thomson SA, Ward P, Wilson JW, Xu T, Youngman MA. Cadilla R, et al. Among authors: saxty g. Bioorg Med Chem. 2020 Dec 1;28(23):115791. doi: 10.1016/j.bmc.2020.115791. Epub 2020 Oct 3. Bioorg Med Chem. 2020. PMID: 33059303
Identification of N-(4-piperidinyl)-4-(2,6-dichlorobenzoylamino)-1H-pyrazole-3-carboxamide (AT7519), a novel cyclin dependent kinase inhibitor using fragment-based X-ray crystallography and structure based drug design.
Wyatt PG, Woodhead AJ, Berdini V, Boulstridge JA, Carr MG, Cross DM, Davis DJ, Devine LA, Early TR, Feltell RE, Lewis EJ, McMenamin RL, Navarro EF, O'Brien MA, O'Reilly M, Reule M, Saxty G, Seavers LC, Smith DM, Squires MS, Trewartha G, Walker MT, Woolford AJ. Wyatt PG, et al. Among authors: saxty g. J Med Chem. 2008 Aug 28;51(16):4986-99. doi: 10.1021/jm800382h. Epub 2008 Jul 26. J Med Chem. 2008. PMID: 18656911
Monoacidic Inhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1:NRF2) Protein-Protein Interaction with High Cell Potency Identified by Fragment-Based Discovery.
Davies TG, Wixted WE, Coyle JE, Griffiths-Jones C, Hearn K, McMenamin R, Norton D, Rich SJ, Richardson C, Saxty G, Willems HM, Woolford AJ, Cottom JE, Kou JP, Yonchuk JG, Feldser HG, Sanchez Y, Foley JP, Bolognese BJ, Logan G, Podolin PL, Yan H, Callahan JF, Heightman TD, Kerns JK. Davies TG, et al. Among authors: saxty g. J Med Chem. 2016 Apr 28;59(8):3991-4006. doi: 10.1021/acs.jmedchem.6b00228. Epub 2016 Apr 12. J Med Chem. 2016. PMID: 27031670
A Fragment-Derived Clinical Candidate for Antagonism of X-Linked and Cellular Inhibitor of Apoptosis Proteins: 1-(6-[(4-Fluorophenyl)methyl]-5-(hydroxymethyl)-3,3-dimethyl-1 H,2 H,3 H-pyrrolo[3,2- b]pyridin-1-yl)-2-[(2 R,5 R)-5-methyl-2-([(3R)-3-methylmorpholin-4-yl]methyl)piperazin-1-yl]ethan-1-one (ASTX660).
Johnson CN, Ahn JS, Buck IM, Chiarparin E, Day JEH, Hopkins A, Howard S, Lewis EJ, Martins V, Millemaggi A, Munck JM, Page LW, Peakman T, Reader M, Rich SJ, Saxty G, Smyth T, Thompson NT, Ward GA, Williams PA, Wilsher NE, Chessari G. Johnson CN, et al. Among authors: saxty g. J Med Chem. 2018 Aug 23;61(16):7314-7329. doi: 10.1021/acs.jmedchem.8b00900. Epub 2018 Aug 9. J Med Chem. 2018. PMID: 30091600
15 results