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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.
Inhibition of the melanocortin-3 receptor (MC3R) causes generalized sensitization to anorectic agents.
Dahir NS, Gui Y, Wu Y, Sweeney PR, Williams SY, Gimenez LE, Sawyer TK, Joy ST, Mapp AK, Cone RD. Dahir NS, et al. Among authors: sawyer tk. bioRxiv [Preprint]. 2023 Dec 7:2023.12.05.570114. doi: 10.1101/2023.12.05.570114. bioRxiv. 2023. Update in: J Clin Invest. 2024 Jul 15;134(14):e178250. doi: 10.1172/JCI178250 PMID: 38106197 Free PMC article. Updated. Preprint.
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.
204 results