Development of antiviral drugs targeting the flaviviruses fusion mechanism

Kampmann, T., Yennamalli, R., Stoermer, M., Kobe, B. and Young, P. (2005). Development of antiviral drugs targeting the flaviviruses fusion mechanism. In: FEBS Journal: Abstracts. 30th FEBS Congress - 9th IUBMB Conference, Budapest, Hungary, (553-553). 2-7tJuly 2005. doi:10.1111/j.1742-4658.2005.4739_15.x

Author Kampmann, T.
Yennamalli, R.
Stoermer, M.
Kobe, B.
Young, P.
Title of paper Development of antiviral drugs targeting the flaviviruses fusion mechanism
Conference name 30th FEBS Congress - 9th IUBMB Conference
Conference location Budapest, Hungary
Conference dates 2-7tJuly 2005
Proceedings title FEBS Journal: Abstracts   Check publisher's open access policy
Journal name Febs Journal   Check publisher's open access policy
Place of Publication Oxford, England
Publisher Blackwell Publishing
Publication Year 2005
Sub-type Published abstract
DOI 10.1111/j.1742-4658.2005.4739_15.x
ISSN 1742-464X
Volume 272
Issue Suppl. 1
Start page 553
End page 553
Total pages 2
Language eng
Formatted Abstract/Summary
We have successfully identified and tested small molecules which
inhibit the dengue virus fusion mechanism, a process essential for
viral infection of cells. The compounds were identified by in silico
docking of a compound library against the dengue virus envelope
(E) protein. We hypothesize that these compounds inhibit the
transition of the E protein from its metastable pre-fusion form to
its stable post-fusion form. We tested the compounds in plaque
and MTT assays and identified one compound with an IC50 of
1 μM with no mammalian cytotoxicity. This lead compound is
now undergoing further studies for the development of a dengue
virus fusion inhibitor. Furthermore, the high conservation of E
protein structural elements amongst the flaviviruses suggests that
this compound may also serve as a lead for the development of
fusion inhibitors against other members of the flavivirus family,
for example the West Nile fever and Japanese encephalitis viruses.
Flaviviruses, in particular, dengue virus are a major public
health problem in tropical and subtropical areas of the world.
Up too 100 million people are infected annually and the incidence
of these diseases is increasing over the last two decades.
Infection with dengue virus can result in acute and potentially
fatal haemorrhagic fever. Currently there are no therapeutic
agents available for treating flavivirus infections. The identification
of our lead compound is a first step toward their development.
Subjects 0605 Microbiology
Keyword Biochemistry & Molecular Biology
Q-Index Code CX
Q-Index Status Provisional Code
Institutional Status UQ
Additional Notes V1-051P

Version Filter Type
Citation counts: TR Web of Science Citation Count  Cited 0 times in Thomson Reuters Web of Science Article
Google Scholar Search Google Scholar
Created: Mon, 13 Aug 2007, 15:55:44 EST