Abstract: The present invention relates to small molecules as entry inhibitors of the HIV virus, processes for their preparation as well as pharmaceutical compositions, their use as medicines, and diagnostic kits comprising them. The present invention also concerns combinations of the present entry inhibitors with other anti-retroviral agents. It further relates to their use in assays as reference compounds or as reagents. The compounds of the present invention are useful for preventing or treating infection by HIV and for treating AIDS.

Abstract: The present invention concerns a fluorescence resonance energy transfer based high throughput test system to measure the formation of the RSV F1 six-helix bundle. In a first embodiment the current invention relates to a homogeneous time resolved fluorescence-based test system comprising a first helical polypeptide consisting essentially of the sequence of IQN57 (SEQ ID NO: 1); a second helical polypeptide consisting essentially of the sequence of C45 (SEQ ID NO: 2) wherein said IQN57 is labeled with a light emitting fluorophore and said C45 is labeled with an ultra-violet excitable fluorophore.

Abstract: This invention relates to hydrolase fluorogenic substrates with improved cell permeability, methods for the preparation thereof, and methods of measuring activities of hydrolases, particularly in cell-based assays. The substrates easily diffuse into the cells, where they are enzymatically processed to yield photostable fluorescent products, and are particularly fitted for visualising enzyme-derived activities in cell-based assays.

Abstract: The present invention concerns a fluorescence resonance energy transfer based high throughput test system to measure the formation of the HIV gp41 six-helix bundle. In a first embodiment the current invention relates to a homogeneous time resolved fluorescence-based test system comprising a first helical polypeptide consisting essentially of the sequence of IQN36 (SEQ ID NO:1); a second helical polypeptide consisting essentially of the sequence of C34 (SEQ ID NO: 2) wherein said IQN36 is labeled with a light emitting fluorophore and said C34 is labeled with an ultra-violet excitable fluorophore.

Abstract: The present invention concerns a method for identifying compounds that decrease the ability of Human Immunodeficiency Virus (HIV) to enter previously uninfected cells. More specifically it relates to a homogeneous competitive cell-based binding assay for the identification of HIV-1 entry fusion inhibitors on a high content screening platform or flow cytometric-based read out.

Abstract: The present invention concerns a fluorescence resonance energy transfer based high throughput test system to measure the formation of the RSV F1 six-helix bundle. In a first embodiment the current invention relates to a homogeneous time resolved fluorescence-based test system comprising a first helical polypeptide consisting essentially of the sequence of IQN57 (SEQ ID NO: 1); a second helical polypeptide consisting essentially of the sequence of C45 (SEQ ID NO: 2) wherein said IQN57 is labeled with a light emitting fluorophore and said C45 is labeled with an ultra-violet excitable fluorophore.

Abstract: The present invention concerns sulfonamide derivatives having the general formula and N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs and esters thereof, wherein Q1 is —S— or —O—; R1 is hydrogen, C1-6alkyl, hydroxy, amino, halogen, aminoC1-4alkyl and mono- or di(C1-4alkyl)amino; R2 is hydrogen or C1-6alkyl; R3 is C1-6alkyl, aryl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, or arylC1-4alkyl; R4 is hydrogen, C1-4alkyloxycarbonyl, carboxyl, optionally mono- or disubstituted aminocarbonyl, mono- or di(C1-4alkyl)aminocarbonyl, C3-7cycloalkyl, C2-6alkenyl, C2-6alkynyl or C1-6alkyl optionally substituted with one or more substituents each independently selected from aryl, Het1, Het2, C3-7cycloalkyl, C1-4alkyloxy-carbonyl, carboxyl, aminocarbonyl, mono- or di(C1-4alkyl)aminocarbonyl, aminosulfonyl, C1-4alkylS(?O)t, hydroxy, cyano, halogen or amino optionally mono- or di-substituted where the substituents are each independently selected from C1-4alkyl, aryl, arylC1-4alkyl, C3-7cycloalkyl, C3-7cycloa

Abstract: The present invention realtes to 5H-pyrazolo[1,5-c][1,3]benzoxazin-5-yl)phenyl methanone derivatives as inhibitors of the viral replication of the HIV virus, processes for their preparation as well as pharmaceutical compositions, their use as medicines, and diagnostic kits comprising them. The present invention also concerns combinations of the present HIV inhibitors with other anti-retroviral agents. It further relates to their use in assays as reference compounds or as reagents. The compounds of the present invention are useful for preventing or treating infection by HIV and for treating AIDS.

Abstract: The invention relates to reporter molecules comprising at least one detection domain capable of emitting a signal and at least one membrane anchoring domain, which promotes the association of the reporter molecule with a membrane. The degree and rate of membrane association of the reporter molecule is approximated by the signal emitted by the detection domain. This signal provides a marker for the membrane association status of the membrane anchoring portion, or of the reporter molecule as a whole. Treatments or agents may be tested for their ability to alter membrane association or localization by observing or measuring the signal emitted by the detection domain. Thus, the invention provides means and methods for determining the capability of an agent to interfere at least in part with the distribution of a reporter molecule in a cell. These methods are useful for drug discovery; the phenotypic evaluation of cells, preferably patient cells; and for tailoring a therapeutic program for treating a patient.

Abstract: The present invention is directed to reporter molecules and tags that may be used to monitor a target substance in a biological system. More particularly, the present invention relates to the use of an apo metal binding protein as a reporter molecule or tag. An apo metal binding protein may be bound to a protein or tissue or introduced into a cell. The invention also relates to methods of utilizing the apo metal binding protein for detecting a cell expressing a protein of interest, localizing a protein in a cell, and designing a therapeutic agent for treating a disease or infection.

Abstract: The present invention is directed to reporter molecules and tags that may be used to monitor a target substance in a biological system. More particularly, the present invention relates to the use of an apo metal binding protein as a reporter molecule or tag. An apo metal binding protein may be bound to a protein or tissue or introduced into a cell. The invention also relates to methods of utilizing the apo metal binding protein for detecting a cell expressing a protein of interest, localizing a protein in a cell, and designing a therapeutic agent for treating a disease or infection.

Abstract: A method for the rapid screening of analytes, such as potential drug candidates, comprises the steps of applying a plurality of analytes to be screened onto one or more, solid support(s) (61) such that the analytes remain isolated from one another; contacting said analyte-carrying solid support(s) (61) with targets provided in a semi-solid or liquid medium, whereby said analytes are released from the solid support(s) (61) to the targets; and measuring analyte-target interactions. This method allows for the manipulation of thousands of different analytes simultaneously. When the analyte is applied to the solid support (61) it can diffuse thereon so as to produce a concentration gradient and serial dilution of analyte if a dose response curve for a candidate drug is required. The method described can be readily automated.