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Synthetic small molecule furin inhibitors derived from 2,5-dideoxystreptamine
- G. Jiao, L. Cregar, +7 authors G. Thomas
- Biology, MedicineProceedings of the National Academy of Sciences
- 26 December 2006
The compounds presented here are bona fide synthetic small molecule furin inhibitors that exhibit potency in the nanomolar range, suggesting that they may serve as valuable tools for studying furin action and potential therapeutics agents for furin-dependent diseases.
Small Molecule Pan-Dengue and West Nile Virus NS3 Protease Inhibitors
- Lynne Cregar-Hernandez, G. Jiao, Alan T. Johnson, A. Lehrer, T. Wong, S. Margosiak
- Biology, MedicineAntiviral chemistry & chemotherapy
- 1 June 2011
This class of compounds is the first to demonstrate competitive pan-dengue and WNV NS3 protease inhibition and, given the sequence conservation among flavivirus NS3 proteins, suggests that developing a pan- dengue or possibly pan-flavivirus therapeutic is feasible.
Structural characterization of three novel hydroxamate-based zinc chelating inhibitors of the Clostridium botulinum serotype A neurotoxin light chain metalloprotease reveals a compact binding site…
X-ray crystal structures of the complex of BoNT serotype A light chain (BoNT/A LC) with three different micromolar-potency hydroxamate-based inhibitors are reported here, revealing significant changes in the active site as a result of binding by the unique inhibitor scaffolds.
Fluorescent, through-bond energy transfer cassettes for labeling multiple biological molecules in one experiment.
- G. Jiao, L. Thoresen, K. Burgess
- Chemistry, MedicineJournal of the American Chemical Society
- 11 November 2003
Through-bond energy transfer cassettes based on a fluorescein donor component electronically conjugated to rhodamine-like acceptors have been designed and synthesized and form the basis for improved detection of chain-terminated DNA in high-throughput sequencing and other applications in biotechnology.
Syntheses of regioisomerically pure 5- or 6-halogenated fluoresceins.
Three routes to regioisomerically pure 5- and 6-iodofluoresceins or 5-and- 6-bromofluorsceins are described and an approach to sulfonic acid derivatives 3 and 4 of 5-iodo isomers is shown.
Structural Studies Revealed Active Site Distortions of Human Furin by a Small Molecule Inhibitor.
The observed binding modes represent a new inhibition strategy of furin and imply the possibility to attain specificity among the PCs providing an innovative starting point of structure guided inhibitor development for furin.
Small-Molecule Inhibitors of Lethal Factor Protease Activity Protect against Anthrax Infection
- M. Moayeri, D. Crown, +4 authors S. Leppla
- Biology, MedicineAntimicrobial Agents and Chemotherapy
- 17 June 2013
It is shown that small-molecule inhibitors of lethal factor proteolytic activity protect against lethality caused by anthrax infection in mice when combined with subprotective doses of either antibiotics or neutralizing monoclonal antibodies that target edema factor.
Rigid, conjugated, fluoresceinated thymidine triphosphates: syntheses and polymerase mediated incorporation into DNA analogues.
- L. Thoresen, G. Jiao, Wade C. Haaland, M. Metzker, K. Burgess
- Chemistry, MedicineChemistry
- 6 October 2003
Syntheses of a unique set of energy transfer dye labeled nucleoside triphosphates, compounds 1-3, are described, which feature progressively longer rigid conjugated linkers connecting the nucleobase and the hydroxyxanthone moiety.
Syntheses and spectroscopic properties of energy transfer systems based on squaraines
The purpose of this project was to prepare fluorescent dyes that could absorb energy at relatively short wavelengths, and fluoresce in the near-IR region. To achieve this, copper- and…
Identification of potent and compartment-selective small molecule furin inhibitors using cell-based assays.
- B. Ramos-Molina, Adam N. Lick, +5 authors I. Lindberg
- Biology, MedicineBiochemical pharmacology
- 15 July 2015
It is shown that certain guanidinylated 2,5-dideoxystreptamine derivatives exhibit interesting ex vivo properties and might therefore be of preferred therapeutic interest in the treatment of certain bacterial and viral infections.