Abstract: 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.

Abstract: 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 (sVpr1-96), of a 47 amino acid long N-terminal (sVpr1-47), of a 49 amino acid long C-terminal fragment (sVpr48-96) as well as fragments thereof (sVpr1-20 and sVpr21-40) and further approximately 15 amino acid long fragments of sVpr1-96. 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.

Abstract: 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.

Abstract: Provided is a composition comprising a Vpr polypeptide conjugated to a therapeutic molecule. Preferably, the Vpr comprises synthetic Vpr. The therapeutic molecule can comprise any molecule capable of being conjugated to Vpr or a fragment thereof, including a polypeptide, a polynucleotide, and/or a toxin. The invention additionally provides a method for delivering a molecule into a cell. The method comprises contacting the cell with a conjugate comprising a Vpr polypeptide conjugated to the molecule. The invention further provides a method for modulating the expression of a transgene in a cell, a method for killing a target cell population in a subject, a method for increasing the sensitivity of cells to radiation therapy, and a method for inhibiting cell proliferation.

Abstract: Provided is a composition comprising a Vpr polypeptide conjugated to a therapeutic molecule. Preferably, the Vpr comprises synthetic Vpr. The therapeutic molecule can comprise any molecule capable of being conjugated to Vpr or a fragment thereof, including a polypeptide, a polynucleotide, and/or a toxin. The invention additionally provides a method for delivering a molecule into a cell. The method comprises contacting the cell with a conjugate comprising a Vpr polypeptide conjugated to the molecule. The invention further provides a method for modulating the expression of a transgene in a cell, a method for killing a target cell population in a subject, a method for increasing the sensitivity of cells to radiation therapy, and a method for inhibiting cell proliferation.

Abstract: The present invention concerns novel complexes for use in the diagnosis of vascular diseases, methods of manufacturing such complexes and diagnostic agents containing them. These complexes strongly enrich themselves in atherosclerotic plaques and are thus suitable for use in non-invasive procedures for diagnosing atherosclerosis.

Abstract: A new compound is disclosed, N-(chlorocarbonyloxy-5-norbornene-2,3-dicarboximide I, in addition to processes for its production and employment of the compound as starting product for the manufacture of non-symmetrical carbonate, urethane-protected amino acid or peptide, activated carrier and carrier-ligand-complexes. The new compound is reacted with alcohols as well as with hydroxyl-group-containing or amino-group-containing polymers.