98541-64-1Relevant articles and documents
Stereoselective synthesis of Boc-protected L-seleno- and tellurolanthionine, L-seleno- and tellurocystine and derivatives
Schneider, Alex,Rodrigues, Oscar E. D.,Paix?o, Márcio W.,Appelt, Helmoz R.,Braga, Antonio L.,Wessjohann, Ludger A.
, p. 1019 - 1021 (2006)
Optically active seleno- and telluro amino acids can be synthesized from serine via its β-lactone with selenides and tellurides under overall retention of the serine stereochemistry. Boc-protected l-selenolanthionine, l-tellurolanthionine, l-selenocystine
Gatorbulin-1, a distinct cyclodepsipeptide chemotype, targets a seventh tubulin pharmacological site
Matthew, Susan,Chen, Qi-Yin,Ratnayake, Ranjala,Fermaintt, Charles S.,Lucena-Agell, Daniel,Bonato, Francesca,Prota, Andrea E.,Lim, Seok Ting,Wang, Xiaomeng,Díaz, J. Fernando,Risinger, April L.,Paul, Valerie J.,Oliva, Maria ángela,Luesch, Hendrik
, (2021/03/03)
Tubulin-targeted chemotherapy has proven to be a successful and wide spectrum strategy against solid and liquid malignancies. Therefore, new ways to modulate this essential protein could lead to new antitumoral pharmacological approaches. Currently known tubulin agents bind to six distinct sites at α/β-tubulin either promoting microtubule stabilization or depolymerization. We have discovered a seventh binding site at the tubulin intradimer interface where a novel microtubule-destabilizing cyclodepsipeptide, termed gatorbulin-1 (GB1), binds. GB1 has a unique chemotype produced by a marine cyanobacterium. We have elucidated this dual, chemical and mechanistic, novelty through multidimensional characterization, starting with bioactivity-guided natural product isolation and multinuclei NMR-based structure determination, revealing the modified pentapeptide with a functionally critical hydroxamate group; and validation by total synthesis. We have investigated the pharmacology using isogenic cancer cell screening, cellular profiling, and complementary phenotypic assays, and unveiled the underlying molecular mechanism by in vitro biochemical studies and high-resolution structural determination of the α/β-tubulin?GB1 complex.
PNA Hybrid Sequences as Recognition Units in SNARE-Protein-Mimicking Peptides
Hubrich, Barbara E.,Kumar, Pawan,Neitz, Hermann,Grunwald, Matthias,Grothe, Tobias,Walla, Peter Jomo,Jahn, Reinhard,Diederichsen, Ulf
supporting information, p. 14932 - 14936 (2018/10/15)
Membrane fusion is an essential process in nature and is often accomplished by the specific interaction of SNARE proteins. SNARE model systems, in which SNARE domains are replaced by small artificial units, represent valuable tools to study membrane fusio
ANTIBACTERIAL COMPOUNDS
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Page/Page column 28, (2018/10/19)
Novel compounds having antimicrobial activitiy, in particular against Pseudomonas aeruginosa, Burkholderia cepaciaand/or Clostridium difficile, and a pharmaceutical composition containing the novel compound.