Patent classifications
G01N2500/02
Anti-FcRn Antibodies
The disclosure relates to antibodies specific to FcRn, formulations comprising the same, use of each in therapy, processes for expressing and optionally formulating said antibody, DNA encoding the antibodies and hosts comprising said DNA.
PROBE FOR DETECTION OF CATHEPSIN ACTIVITY
In this vein, we present CTLAP, a fluorogenic probe that is rapidly activated by CTL and displays good selectivity over CTB and CTV, the closest competing analytes for CTL activity probes. CTLAP exhibits intrinsically low background fluorescence, which we attribute to the notably low quantum yield measured for the probe. CTLAP demonstrates markedly higher turn-on ratios (24-fold) and moderately improved enzyme selectivity (6- to 10-fold) when compared to Z-FR-AMC (10-fold turn-on ratio, 6- to 7-fold selectivity), a commercially available CTL-selective probe commonly used to detect CTL activity in mixed samples. Optimum selectivity for CTL is achieved within 10 min of incubation with the enzyme, suggesting that CTLAP is amenable for rapid detection of CTL, even in the presence of competing cathepsins.
Screening method for materials that suppress characteristic body odor of elderly people
The present invention relates to a screening method for materials that suppress the characteristic body odor of elderly people. The screening method of the present invention is designed such that test substances are screened with olfactory receptors responsive to substances responsible for the characteristic body odor of elderly people to select candidate substances for materials that suppress the characteristic body odor of elderly people, and this method comprises adding a test substance and a substance responsible for the characteristic body odor of elderly people to at least one olfactory receptor polypeptide selected from the group consisting of (a) OR2C1, OR2J2, OR4E2 and OR5P3, and (b) polypeptides which comprise an amino acid sequence sharing an identity of at least 80% with the amino acid sequence of any of the polypeptides in (a) and which are responsive to the substance responsible for the characteristic body odor of elderly people; measuring the response of the olfactory receptor polypeptide to the substance responsible for the characteristic body odor of elderly people; and identifying a test substance that suppresses the response of the olfactory receptor polypeptide on the basis of the measured response. Moreover, the present invention relates to a screening method for trans-2-nonenal odor suppressors and a screening method for trans-2-octenal odor suppressors.
HIF-1 and HIF-2 inhibitors
The present invention relates to inhibitors of HIF-1 and HIF-2 and uses thereof. The present invention further relates to the inhibitors for use in treatment of diseases. An isolated polypeptide is provided, that prevents dimerization of HIF-1α with HIF-1β and HIF-2α with HIF-1β and/or inhibits the activity of HIF-1 and HIF-2, wherein the polypeptide comprises the amino acid sequence C-X1-X2-X3-Z-X4 (SEQ ID NO: 1) and wherein X1, X2, X3 and X4 are any amino acid and wherein Z is leucine, valine of isoleucine or a non-natural derivative or leucine, valine or isoleucine. The isolated polypeptide prevents dimerization of HIF-1α with HIF-1β and HIF-2α with HIF-1β and inhibits the activity of HIF-1 and HIF-2 by binding to HIF-1α or HIF-1β and/or HIF-2α or HIF-1β.
Method for Measuring Modulation in the Activity of a G Protein-Coupled Receptor
The invention relates to a method for determining the ability of a molecule to modulate the activity of a G protein-coupled receptor (GPCR), said method comprising the following steps: a) introducing, into a first container:—a first membrane preparation bearing one or more GPCRs and one or more G protein(s),—a source of GDP or a source of GTP,—a first ligand of the alpha subunit of a G protein (Galpha protein) labelled with a first member of a pair of RET partners, and a second ligand of the Galpha protein labelled with a second member of the pair of RET partners, said ligands being able to specifically bind, either individually or in combination, to the empty Galpha protein or to the full Galpha protein; b) measuring the RET signal emitted in the first container; c) introducing (i) into a second container, the same reactants as in step a) and the molecule to be tested or (ii) into the first container, the molecule to be tested; d) measuring the RET signal emitted in the second container or in the first container obtained in step c); e) comparing the signals obtained in steps b) and d).
TABLE-US-00001 AA GPCR activation BB from “full” G to “empty” G form CC Agonist DD Format 1 EE Format 2 FF G.sub.empty GG Before activation HH After activation
VIRAL INFECTION THERAPEUTIC
The present invention relates to an inhibitory agent of membrane fusion between a virus envelope and a cell membrane of a host cell for the virus, wherein the inhibitory agent comprises a serine protease inhibitor, and a therapeutic agent or a therapeutic composition, comprising the inhibitory agent. More specifically, the present invention relates to the inhibitory agent, wherein the serine protease inhibitor is one or more of a compound represented by the following general formula (I) or a salt thereof, or a solvate or hydrate thereof, and a therapeutic agent or a therapeutic composition, comprising the inhibitory agent:
##STR00001## wherein R.sub.1 represents a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted lower alkenyl group, a substituted or unsubstituted aromatic hydrocarbon group, or a substituted or unsubstituted aromatic heterocyclic group, each of which may optionally comprise a heteroatom.
Macrocyclic inhibitors of the PD-1/PD-L1 and CD80(B7-1)/PD-L1 protein/protein interactions
The present disclosure provides novel macrocyclic peptides which inhibit the PD-1/PD-L1 and PD-L1/CD80 protein/protein interaction, and thus are useful for the amelioration of various diseases, including cancer and infectious diseases.
USE OF BLOCKING-REAGENTS FOR REDUCING UNSPECIFIC T CELL-ACTIVATION
The present invention relates to a blocking-reagent for use in reducing unspecific T cell activation in T cell engaging therapies. The present invention further relates to pharmaceutical kit of parts and an in vitro method for evaluating unspecific T cell activation.
METHOD FOR DETECTING MOLECULES THAT INHIBIT THE INTERACTION OF CD36 PROTEIN WITH AMYLOID BETA
Disclosed is a method for identifying inhibitors of the interaction of CD36 receptor and amyloid-beta protein (Aβ), which consists in: immobilizing CD36 on a polystyrene plate; and detecting by colorimetric, the interaction thereof with fibrillar Aβ (fAβ), using a polyclonal anti-Aβ antibody and a secondary antibody conjugated to horseradish peroxidase (HRP). The inhibitors identified are potential agents for the treatment of Alzheimer's disease.
Compounds for Treating Tauopathies and Restless Leg Syndrome and Methods of Using and Screening for Same
Provided are compounds capable of enhancing the ability of receptor-type tyrosine-protein phosphatase delta (PTPRD) to dephosphorylate a kinase. Also disclosed is a method of treating a tauopathy or restless leg syndrome in a subject comprising administering to the subject an effective amount of a disclosed compound. Also disclosed are kits comprising the compounds together with instructions for treating a condition and/or a compound known for treating the condition. Finally, disclosed herein is a screening method suitable for identifying positive allosteric modulators of the ability of a receptor-type tyrosine-protein phosphatase delta (PTPRD) to dephosphorylate a kinase.