7twm: Difference between revisions
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=7twm FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7twm OCA], [https://pdbe.org/7twm PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7twm RCSB], [https://www.ebi.ac.uk/pdbsum/7twm PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7twm ProSAT]</span></td></tr> | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=7twm FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7twm OCA], [https://pdbe.org/7twm PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7twm RCSB], [https://www.ebi.ac.uk/pdbsum/7twm PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7twm ProSAT]</span></td></tr> | ||
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== Publication Abstract from PubMed == | |||
N-methylation of peptide backbones has often been utilized as a strategy towards the development of peptidic drugs. However, difficulties in the chemical synthesis, high cost of enantiopure N-methyl building blocks, and subsequent coupling inefficiencies have hampered larger-scale medicinal chemical efforts. Here, we present a chemoenzymatic strategy for backbone N-methylation by bioconjugation of peptides of interest to the catalytic scaffold of a borosin-type methyltransferase. Crystal structures of a substrate tolerant enzyme from Mycena rosella guided the design of a decoupled catalytic scaffold that can be linked via a heterobifunctional crosslinker to any peptide substrate of choice. Peptides linked to the scaffold, including those with non-proteinogenic residues, show robust backbone N-methylation. Various crosslinking strategies were tested to facilitate substrate disassembly, which enabled a reversible bioconjugation approach that efficiently released modified peptide. Our results provide general framework for the backbone N-methylation on any peptide of interest and may facilitate the production of large libraries of N-methylated peptides. | |||
Bioconjugate Platform for Iterative Backbone N-Methylation of Peptides.,Zheng Y, Ongpipattanakul C, Nair SK ACS Catal. 2022 Nov 18;12(22):14006-14014. doi: 10.1021/acscatal.2c04681. Epub , 2022 Oct 31. PMID:36793448<ref>PMID:36793448</ref> | |||
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |||
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== References == | |||
<references/> | |||
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