Abstract: The present disclosure relates generally to compounds and methods for inhibiting the enzymatic activity of lysine demethylase 4 (KDM4) and treating cancer. Provided herein are substituted pyridine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibiting lysine demethylase 4. Furthermore, the subject compounds and compositions are useful for the treatment of breast cancer and the like.

Abstract: The present invention is inter alia concerned with an inhibitor selected from the group consisting of a selective KMT9-inhibitor, a selective METTL21A-inhibitor and a selective METTL21B-inhibitor for use in the treatment of cancer. KMT9, METTL21A and METTL21B are characterized herein for the first time as histone methyl transferases, and inhibitors of the same can be used for treating cancer.

Abstract: The present disclosure relates generally to compounds and methods for inhibiting the enzymatic activity of lysine demethylase 4 (KDM4) and treating cancer. Provided herein are substituted pyridine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibiting lysine demethylase 4. Furthermore, the subject compounds and compositions are useful for the treatment of breast cancer and the like.

Abstract: Disclosed in the present application are: (i) a compound inhibiting the interaction between LSD1me2 and CHD1 for use in therapy, (ii) a compound inhibiting the interaction between LSD1me2 and CHD1 for use in treating cancer, in particular prostate cancer, and (iii) a method of screening for such a compound.

Abstract: The present invention relates to the use of a genetically modified non-human animal as an animal model for obesity or obesity-related disorders, wherein the amount of Lysine-specific Demethylase 1 (LSD1) in at least one tissue or at least one cell type of said animal is reduced.

Abstract: Disclosed in the present application are: (i) a compound inhibiting the interaction between LSD1me2 and CHD1 for use in therapy, (ii) a compound inhibiting the interaction between LSD1me2 and CHD1 for use in treating cancer, in particular pro state cancer, and (iii) a method of screening for such a compound.

Abstract: Disclosed is the use of at least one amine oxidase inhibitor for modulating the activity of the lysine-specific demethylase (LSD1) in a mammal and to pharmaceutical compositions for controlling the androgen receptor-dependent gene expression, comprising an effective dose of at least one amine oxidase inhibitor suitable for modulating the activity of the lysine-specific demethylase (LSD1) in a mammal.

Abstract: The present invention relates to the use of a genetically modified non-human animal as an animal model for obesity or obesity-related disorders, wherein the amount of Lysine-specific Demethylase 1 (LSD1) in at least one tissue or at least one cell type of said animal is reduced.

Abstract: Disclosed is the use of at least one amine oxidase inhibitor for modulating the activity of the lysine-specific demethylase (LSD1) in a mammal and to pharmaceutical compositions for controlling the androgen receptor-dependent gene expression, comprising an effective dose of at least one amine oxidase inhibitor suitable for modulating the activity of the lysine-specific demethylase (LSD1) in a mammal.

Abstract: The invention relates to the use of at least one amine oxidase inhibitor for modulating the activity of the lysine-specific demethylase (LSD1) in a mammal and to pharmaceutical compositions for controlling the androgen receptor-dependent gene expression, comprising an effective dose of at least one amine oxidase inhibitor suitable for modulating the activity of the lysine-specific demethylase (LSD1) in a mammal. The invention also relates to assay systems allowing to test LSD1 inhibitors for their ability to inhibit LSD1 function.

Abstract: The present invention provides in vitro methods for detecting, grading or prognosticating cancer, in particular prostate cancer. The invention further provides isolated polynucleotides suitable for reducing or inhibiting the expression of protein kinase C beta I and/or II and/or alpha (and consequently the levels of histone H3 phosphorylated at threonine 6, histone H3 monomethylated at lysine 4, histone H3 dimethylated at lysine 4, histone H3 trimethylated at lysine 4) and further relates to pharmaceutical compositions comprising said polynucleotides for the treatment or prevention of cancer, in particular prostate cancer.

Abstract: The invention relates to a multiple-specificity demethylase complex comprising a Jumonji C (JMJC) domain-containing enzyme, a process of its preparation and its use.

Abstract: The present invention relates to novel biomarker for breast cancer, namely LSD1 and its application in inter alia the diagnosis of breast cancer. Furthermore, the present invention discloses a method of determining the LSD1 protein amount and the effect of LSD1 inhibitors on cancer cells selected from breast cancer, lung carcinoma and sarcoma.

Abstract: The present invention relates to a non-human transgenic animal whose genome comprises a stably integrated transgenic nucleotide sequence encoding Lysine-specific Demethylase 1 (LSD1) operably linked to a promoter. The invention further concerns methods for generating the non-human animal and its use as a cancer model.

Abstract: The present invention relates to a process for controlling at least one androgen receptor- (AR-) regulated mechanism in mammalian cells under histone-phosphorylating conditions, said process comprising allowing at least one inhibitor with specificity for at least one protein kinase C-related kinase (PRK) to act on said at least one PRK1 thereby modulating, preferably down-regulating, the activity of said at least one PRK and optionally blocking said at least one androgen receptor-regulated mechanism in said mammalian cells.

Abstract: Polypeptide sequences which play a part in the regulation of skeletal muscle differentiation, and nucleic acids coding therefor, and the use thereof in diagnosis and therapy are disclosed. Possible uses are also indicated for antibodies which are directed against corresponding epitopes of the GRIM1 polypeptide.

Abstract: The invention relates to antibodies for use for modulating the activity of the lysine-specific demethylase (LSD1) in a mammal and to pharmaceutical and diagnostical compositions comprising such antibodies. The invention also relates to a method for identifying and/or scoring prostate carcinomas. Furthermore, the invention relates to the use of at least one siRNA (“short interfering RNA”) and/or at least one anti-LSD1 antibody for modulating the activity of the lysine-specific demethylase (LSD1) in a mammal or for the manufacture of a medicament for modulating the activity of the lysine-specific demethylase (LSD1) in a mammal. The invention also relates to a pharmaceutical composition for controlling the androgen receptor-dependent gene expression, comprising an effective dose of at least one siRNA and/or at least one anti-LSD1 antibody suitable for modulating the activity of the lysine-specific demethylase (LSD1) in a mammal.

Abstract: The present invention relates to a process for controlling at least one androgen receptor- (AR-) regulated mechanism in mammalian cells under histone-phosphorylating conditions, said process comprising allowing at least one inhibitor with specificity for at least one protein kinase C-related kinase (PRK) to act on said at least one PRK1 thereby modulating, preferably down-regulating, the activity of said at least one PRK and optionally blocking said at least one androgen receptor-regulated mechanism in said mammalian cells.

Abstract: The present invention relates to an assay system for specific inhibitors of protein kinase C-related kinases (PRKs) relating to one or more of the reactions wherein said protein kinase C-related kinases are involved under physiological conditions. The invention also relates to a process for identifying specific inhibitors for protein kinase C-related kinases.

Abstract: The invention relates to a multiple-specificity demethylase complex comprising a Jumonji C (JMJC) domain-containing enzyme, a process of its preparation and its use.