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Page 1
Melanocortin 1 Receptor Agonists Based on a Bivalent, Bicyclic Peptide Framework.
Durek T, Kaas Q, White AM, Weidmann J, Fuaad AA, Cheneval O, Schroeder CI, de Veer SJ, Dellsén A, Österlund T, Larsson N, Knerr L, Bauer U, Plowright AT, Craik DJ. Durek T, et al. J Med Chem. 2021 Jul 22;64(14):9906-9915. doi: 10.1021/acs.jmedchem.1c00095. Epub 2021 Jul 1. J Med Chem. 2021. PMID: 34197114
Potent Anti-SARS-CoV-2 Activity by the Natural Product Gallinamide A and Analogues via Inhibition of Cathepsin L.
Ashhurst AS, Tang AH, Fajtová P, Yoon MC, Aggarwal A, Bedding MJ, Stoye A, Beretta L, Pwee D, Drelich A, Skinner D, Li L, Meek TD, McKerrow JH, Hook V, Tseng CT, Larance M, Turville S, Gerwick WH, O'Donoghue AJ, Payne RJ. Ashhurst AS, et al. J Med Chem. 2022 Feb 24;65(4):2956-2970. doi: 10.1021/acs.jmedchem.1c01494. Epub 2021 Nov 3. J Med Chem. 2022. PMID: 34730959 Free PMC article.
Antimalarial Inhibitors Targeting Serine Hydroxymethyltransferase (SHMT) with in Vivo Efficacy and Analysis of their Binding Mode Based on X-ray Cocrystal Structures.
Schwertz G, Witschel MC, Rottmann M, Bonnert R, Leartsakulpanich U, Chitnumsub P, Jaruwat A, Ittarat W, Schäfer A, Aponte RA, Charman SA, White KL, Kundu A, Sadhukhan S, Lloyd M, Freiberg GM, Srikumaran M, Siggel M, Zwyssig A, Chaiyen P, Diederich F. Schwertz G, et al. J Med Chem. 2017 Jun 22;60(12):4840-4860. doi: 10.1021/acs.jmedchem.7b00008. Epub 2017 Jun 13. J Med Chem. 2017. PMID: 28537728
Bioactive Cyclization Optimizes the Affinity of a Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) Peptide Inhibitor.
Tombling BJ, Lammi C, Lawrence N, Gilding EK, Grazioso G, Craik DJ, Wang CK. Tombling BJ, et al. J Med Chem. 2021 Mar 11;64(5):2523-2533. doi: 10.1021/acs.jmedchem.0c01766. Epub 2020 Dec 23. J Med Chem. 2021. PMID: 33356222
This PCSK9 inhibitor is one of many peptides that could benefit from bioactive cyclization, a strategy that is amenable to broad application in pharmaceutical design....
This PCSK9 inhibitor is one of many peptides that could benefit from bioactive cyclization, a strategy that is amenable to broad application …
Inhibitors of plasmodial serine hydroxymethyltransferase (SHMT): cocrystal structures of pyrazolopyrans with potent blood- and liver-stage activities.
Witschel MC, Rottmann M, Schwab A, Leartsakulpanich U, Chitnumsub P, Seet M, Tonazzi S, Schwertz G, Stelzer F, Mietzner T, McNamara C, Thater F, Freymond C, Jaruwat A, Pinthong C, Riangrungroj P, Oufir M, Hamburger M, Mäser P, Sanz-Alonso LM, Charman S, Wittlin S, Yuthavong Y, Chaiyen P, Diederich F. Witschel MC, et al. J Med Chem. 2015 Apr 9;58(7):3117-30. doi: 10.1021/jm501987h. Epub 2015 Mar 18. J Med Chem. 2015. PMID: 25785478