The J. David Gladstone Institutes

Gesellschaft Fur Biotechnologische Forschung Mbh

Gesellschaft Fur Biotechnologische Forschung Gmbh

Victor Wray

Heinrich Steinmetz

Klaus Gerth

Hans Reichenbach

Norbert Bedorf

Rolf Jansen

Gerhard Hofle

Herbert Irschik

Brigitte Kunze

Wolfram Trowitzsch-Kienast

Dietmar Schomburg

Peter Henklein

Ulrich Schubert

Hermann Augustiniak

Warner C Greene

Michael P Sherman

Uwe Tessmer

Karsten Bruns

The present invention provides screening methods for identifying a compound that induces loss of the lentiviral protein Vpr; screening methods for identifying compounds that inhibit the peptidyl-prolyl cis/trans isomerase (PPIase) activity of a protein that catalyzes cis-trans isomerization of cis-peptidylprolyl bonds in Vpr; and compounds identified by the screening methods. The compounds are useful for treating a lentiviral infection. The present invention further provides methods of inducing loss of the lentiviral protein Vpr; methods of inhibiting lentivirus viral replication; and methods of treating a lentivirus infection in an individual. The methods generally involve administering to an individual infected with the lentivirus an effective amount of a compound that induces Vpr loss and/or that inhibits PPIase activity of a protein that catalyzes cis-trans isomerization of cis-peptidylprolyl bonds in Vpr.

Methods of identifying agents for inhibiting lentivirus replication

The invention pertains to synthetic (s) peptides derived from the viral regulatory protein R (Vpr) of the human immunodeficiency virus type 1 (HIV-1), particularly the chemical synthesis of the 96 amino acid full length Vpr protein (sVpr), of a 47 amino acid long N-terminal (sVpr), of a 49 amino acid long C-terminal fragment (sVpr) as well as fragments thereof (sVprand sVpr) and further approximately 15 amino acid long fragments of sVpr. As fragments or full length products of the HIV-1 regulatory protein, those products are used in biological assays, for molecular and structural characterization of Vpr and domains thereof, as well as for the development of anti-Vpr antibodies directed against Vpr peptide sequences.

Synthetic peptide of regulatory virus protein R (VPR) of human immunodeficiency virus type 1 (HIV-1) and the utilization thereof

The invention relates to cyclic antibiotics of formula ##STR1## wherein the prefix R represents that the substituents on the adjacent carbon atom are in the R configuration; the prefix S represents that the substituents on the adjacent carbon atom are in the S configuration;

Macrocyclic antibodies

The invention relates to cyclic antibiotics of formula ##STR1## wherein the prefix R represents that the substituents on the adjacent carbon atom are in the R configuration; the prefix S represents that the substituents on the adjacent carbon atom are in the S configuration; R.sub.1 is hydrogen or hydroxy and R.sub.2 is hydroxy or .beta.-glucopyranosyloxy, and to the hydrates and salts thereof, especially pharmaceutically acceptable salts. The compounds of formula I are prepared by fermentation using the strain So ce 12 (NCIB 12134) of the species Sorangium celulosum and are effective antiobiotics.

Macrocyclic antibiotics

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Braunschweig, Germany

Victor Wray