126330-77-6Relevant articles and documents
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
, p. 14932 - 14936 (2018)
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
Exploring the dNTP -binding site of HIV-1 reverse transcriptase for inhibitor design
Gu, Weijie,Martinez, Sergio,Singh, Abhimanyu K.,Nguyen, Hoai,Rozenski, Jef,Schols, Dominique,Herdewijn, Piet,Das, Kalyan,De Jonghe, Steven
, (2021/08/24)
HIV-1 reverse transcriptase (RT) plays a central role in the viral life cycle, and roughly half of the FDA-approved anti-HIV drugs are targeting RT. Nucleoside analogs (NRTIs) require cellular phosphorylation for binding to RT, and to bypass this rate-limiting path, we designed a new series of acyclic nucleoside phosphonate analogs as nucleoside triphosphate mimics, aiming at the chelation of the catalytic Mg2+ ions via a phosphonate and/or a carboxylic acid group. Novel synthetic procedures were developed to access these nucleoside phosphonate analogs. X-ray structures in complex with HIV-1 RT/dsDNA demonstrated that their binding modes are distinct from that of our previously reported compound series. The impact of chain length, chirality and linker atom have been discussed. The detailed structural understanding of these new compounds provides opportunities for designing new class of HIV-1 RT inhibitors.
Novel Easily Recyclable Bifunctional Phosphonic Acid Carrying Tripeptides for the Stereoselective Michael Addition of Aldehydes with Nitroalkenes
Cortes-Clerget, Margery,Gager, Olivier,Monteil, Maelle,Pirat, Jean-Luc,Migianu-Griffoni, Evelyne,Deschamp, Julia,Lecouvey, Marc
, p. 34 - 40 (2016/01/25)
A novel bifunctional organocatalyst library combining both aminocatalysis and phosphonic acid activation was used for the first time as an efficient tool for the stereoselective Michael addition of aldehydes with several aromatic nitroalkenes with good selectivities up to 95:5 dr and 93:7 er. Due to their high water solubility, the catalysts were easily recyclable and could be reused over several cycles without any significant loss of selectivity.
