Abstract: The present invention relates to immobilization compounds, immobilization products and preparations thereof as well as methods and uses for the identification of methyltransferase interacting compounds or for the purification or identification of methyltransferase proteins.

Abstract: The invention relates to a method for evaluation of a compound-target interaction in vivo, comprising the steps of administering the compound to an animal, taking a body fluid sample of the animal, determining the concentration of the compound in the body fluid sample, taking a cellular sample of the animal containing the target, preparing a protein preparation of said cellular sample, providing an immobilised ligand capable of binding to the target, contacting the protein preparation with the immobilised ligand under conditions allowing the formation of a complex between the immobilised ligand and the target, determining the amount of complexes formed in step, and correlating the amount of complexes with the concentration of the compound in the body fluid sample.

Abstract: The present invention relates to methods for the identification and characterization (e.g. selectivity profiling) of HDAC interacting compounds using protein preparations derived from cells endogenously expressing HDACs or cell preparations containing said HDACs.

Abstract: The invention provides in a first aspect a method for the identification of an ZAP-70 interacting compound, comprising the steps of a) providing a protein preparation containing phosphorylated ZAP-70, b) contacting the protein preparation with aminopyrido-pyrimidine ligand 24 immobilized on a solid support under conditions allowing the formation of an aminopyrido-pyrimidine ligand 24—phosphorylated ZAP-70 complex, c) incubating the aminopyrido-pyrimidine ligand 24—phosphorylated ZAP-70 complex with a given compound, and d) determining whether the compound is able to separate phosphorylated ZAP-70 from the immobilized aminopyrido-pyrimidine ligand 24.

Abstract: The invention features methods for the identification of leucine-rich kinase 2 (LRRK2) inhibitors using indol ligand 91. Generally, these methods include identifying compounds that compete with indol ligand 91 for binding to LRRK2.

Abstract: The invention relates to compounds of formula (I) wherein R1 to R9 and R4a have the meaning as cited in the description and the claims. Said compounds are useful as inhibitors of ZAP-70 for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.

Abstract: The present invention relates to immobilization compounds and methods useful for the identification of PARP interacting compounds or for the purification or identification of PARP proteins.

Abstract: The invention relates to compounds of formula (I) wherein X, R1, R2, R3, R8, R9 have the meaning as cited in the description and the claims. Said compounds are useful as inhibitors of ZAP-70 for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the use as medicaments.

Abstract: The present invention relates to methods for the characterization of enzymes or of enzyme-compound complexes, wherein the enzyme is obtained from a protein preparation with the help of at least one broad spectrum ligand immobilized on a solid support and wherein the enzyme is characterized by mass spectrometry. These methods are useful for the screening of non-immobilized compound libraries, selectivity profiling of lead compounds and mechanism of action studies in living cells.

Abstract: The invention provides in a first aspect a method for the identification of an LRRK2 interacting compound, comprising the steps of providing a protein preparation containing LRRK2, contacting the protein preparation with indol ligand 91 immobilized on a solid support under conditions allowing the formation of an indol ligand 91-LRRK2 complex, incubating the indol ligand 91-LRRK2 complex with a given compound, and determining whether the compound is able to separate LRRK2 from the immobilized indol ligand 91. Furthermore, the invention relates to a method for the identification of an LRRK2 interacting compound, comprising the steps of providing a protein preparation containing LRRK2, contacting the protein preparation with indol ligand 91 immobilized on a solid support and with a given compound under conditions allowing the formation of an indol ligand 91-LRRK2 complex, and detecting the indol ligand 91-LRRK2 complex.

Abstract: The invention relates to epitopes of the tau protein which are specifically occurring in a phosphorylated state in tau protein from Alzheimer paired helical filaments, to protein kinases which are responsible for the phosphorylation of the amino acids of the tau protein giving rise to said epitopes, and to antibodies specific for said epitopes. The invention further relates to pharmaceutical compositions for the treatment or prevention of Alzheimer's disease, to diagnostic compositions and methods for the detection of Alzheimer's disease and to the use of said epitopes for the generation of antibodies specifically detecting Alzheimer tau protein. Additionally, the invention relates to methods for testing drugs effective in dissolving Alzheimer paired helical filaments or preventing the formation thereof.

Abstract: The present invention relates to the use of SCD4 interacting molecules, especially SCD4 inhibitors, for the preparation of a medicament for the treatment of neurodegenerative diseases, particularly Alzheimer's disease.

Abstract: The present invention relates to a DNA sequence encoding a novel neuronal protein kinase (NPK) which phosphorylates tau proteins as well as other microtubule associated proteins (MAPs) in positions crucial for the binding to microtubules. The invention further relates to Serine or Theorine residues and epitopes comprising said residues phosphorylated by said NPK on said MAPs, to antibodies specifically binding to said protein kinase, pharmaceutical compositions comprising inhibitors to said protein kinase, in particular for the treatment of Alzheimer's disease and cancer, to diagnostic kits and to in vitro diagnostic methods for the detection of Alzheimer's disease and cancer.

Abstract: The present invention relates to methods for the screening of gamma secretase modulators, preferably inhibitors as well as to the use of Eph receptor inhibitors for the treatment of neurodegenerative diseases.

Abstract: The invention relates to epitopes of the tau protein which are specifically occurring in a phosphorylated state in tau protein from Alzheimer paired helical filaments, to protein kinases which are responsible for the phosphorylation of the amino acids of the tau protein giving rise to said epitopes, and to antibodies specific for said epitopes. The invention further relates to pharmaceutical compositions for the treatment or prevention of Alzheimer's disease, to diagnostic compositions and methods for the detection of Alzheimer's disease and to the use of said epitopes for the generation of antibodies specifically detecting Alzheimer tau protein. Additionally, the invention relates to methods for testing drugs effective in dissolving Alzheimer paired helical filaments or preventing the formation thereof.

Abstract: The invention relates to the use of a LAPTM4A-interacting molecule for the preparation of a pharmaceutical composition for the treatment of a neurogenerative disease. Hereby the LAPTM4A-interacting molecule is preferably an inhibitor of LAPTM4A and particularly it has the capacity to modulate the activity of gamma-secretase and/or beta-secretase. Furthermore the invention concerns a process for identifying a gamma-secretase and/or a beta-secretase modulator, comprising the following steps: a. identifying of a LAPTM4A-interacting molecule by determining whether a given test compound is a LAPTM4A-interacting molecule, b. determining whether the LAPTM4A-interacting molecule of step a) is capable of modulating gamma-secretase and/or beta-secretase activity.

Abstract: The invention relates to the use of a GPR49-interacting molecule for the preparation of a pharmaceutical composition for the treatment of a neurogenerative disease. Hereby s the GPR49-interacting molecule is preferably an inhibitor of GPR49 and particularly it has the capacity to modulate the activity of gamma-secretase and/or beta-secretase. Furthermore the invention concerns a process for identifying a gamma-secretase and/or a beta-secretase modulator, comprising the following steps: a. identifying of a GPR49-interacting molecule by determining whether a given test compound is a GPR49-interacting molecule, b. determining whether the GPR49-interacting molecule of step a) is capable of modulating gamma-secretase and/or beta-secretase activity.

Abstract: The present invention relates to the use of DEGS interacting molecules, especially DEGS inhibitors, for the preparation of a medicament for the treatment of neurodegenerative diseases, particularly Alzheimer's disease.

Abstract: The invention relates to the use of a ATP7A-interacting molecule for the preparation of a pharmaceutical composition for the treatment of a neurogenerative disease. Hereby the ATP7A-interacting molecule is preferably an inhibitor of ATP7A and particularly it has the capacity to modulate the activity of gamma-secretase and/or beta-secretase. Furthermore the invention concerns a process for identifying a gamma-secretase and/or a beta-secretase modulator comprising the following steps: a. identifying of a ATP7A-interacting molecule by determining whether a given test compound is a ATP7A-interacting molecule, b. determining whether the ATP7A-interacting molecule of step a) is capable of modulating gamma-secretase and/or beta-secretase activity.

Abstract: The invention relates to the use of a LAPTM4B-interacting molecule for the preparation of a pharmaceutical composition for the treatment of a neurogenerative disease. Hereby the LAPTM4B-interacting molecule is preferably an inhibitor of LAPTM4B and particularly it has the capacity to modulate the activity of gamma-secretase and/or beta-secretase. Furthermore the invention concerns a process for identifying a gamma-secretase and/or a beta-secretase modulator, comprising the following steps: a. identifying of a LAPTM4B-interacting molecule by determining whether a given test compound is a LAPTM4B-interacting molecule, b. determining whether the LAPTM4B-interacting molecule of step a) is capable of modulating gamma-secretase and/or beta-secretase activity.