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Design-rules for stapled peptides with in vivo activity and their application to Mdm2/X antagonists.
Chandramohan A, Josien H, Yuen TY, Duggal R, Spiegelberg D, Yan L, Juang YA, Ge L, Aronica PG, Kaan HYK, Lim YH, Peier A, Sherborne B, Hochman J, Lin S, Biswas K, Nestor M, Verma CS, Lane DP, Sawyer TK, Garbaccio R, Henry B, Kannan S, Brown CJ, Johannes CW, Partridge AW. Chandramohan A, et al. Among authors: sawyer tk. Nat Commun. 2024 Jan 12;15(1):489. doi: 10.1038/s41467-023-43346-4. Nat Commun. 2024. PMID: 38216578 Free PMC article.
Discovery of Sulanemadlin (ALRN-6924), the First Cell-Permeating, Stabilized α-Helical Peptide in Clinical Development.
Guerlavais V, Sawyer TK, Carvajal L, Chang YS, Graves B, Ren JG, Sutton D, Olson KA, Packman K, Darlak K, Elkin C, Feyfant E, Kesavan K, Gangurde P, Vassilev LT, Nash HM, Vukovic V, Aivado M, Annis DA. Guerlavais V, et al. Among authors: sawyer tk. J Med Chem. 2023 Jul 27;66(14):9401-9417. doi: 10.1021/acs.jmedchem.3c00623. Epub 2023 Jul 13. J Med Chem. 2023. PMID: 37439511
Demonstration of a Common DPhe7 to DNal(2')7 Peptide Ligand Antagonist Switch for Melanocortin-3 and Melanocortin-4 Receptors Identifies the Systematic Mischaracterization of the Pharmacological Properties of Melanocortin Peptides.
Gimenez LE, Noblin TA, Williams SY, Mullick Bagchi S, Ji RL, Tao YX, Jeppesen CB, Conde-Frieboes KW, Sawyer TK, Grieco P, Cone RD. Gimenez LE, et al. Among authors: sawyer tk. J Med Chem. 2022 Apr 28;65(8):5990-6000. doi: 10.1021/acs.jmedchem.1c01295. Epub 2022 Apr 11. J Med Chem. 2022. PMID: 35404053 Free PMC article.
Discovery of cell active macrocyclic peptides with on-target inhibition of KRAS signaling.
Lim S, Boyer N, Boo N, Huang C, Venkatachalam G, Angela Juang YC, Garrigou M, Kaan HYK, Duggal R, Peh KM, Sadruddin A, Gopal P, Yuen TY, Ng S, Kannan S, Brown CJ, Verma CS, Orth P, Peier A, Ge L, Yu X, Bhatt B, Chen F, Wang E, Li NJ, Gonzales RJ, Stoeck A, Henry B, Sawyer TK, Lane DP, Johannes CW, Biswas K, Partridge AW. Lim S, et al. Among authors: sawyer tk. Chem Sci. 2021 Nov 25;12(48):15975-15987. doi: 10.1039/d1sc05187c. eCollection 2021 Dec 15. Chem Sci. 2021. PMID: 35024121 Free PMC article.
202 results