Efficacy of Vafidemstat in Experimental Autoimmune Encephalomyelitis Highlights the KDM1A/RCOR1/HDAC Epigenetic Axis in Multiple Sclerosis

Autor: Fernando Cavalcanti, Elena Gonzalez-Rey, Mario Delgado, Clara P. Falo, Leyre Mestre, Carmen Guaza, Francisco O’Valle, Michele M. P. Lufino, Jordi Xaus, Cristina Mascaró, Serena Lunardi, Natalia Sacilotto, Paola Dessanti, David Rotllant, Xavier Navarro, Mireia Herrando-Grabulosa, Carlos Buesa, Tamara Maes

Publikováno v: Pharmaceutics, Vol 14, Iss 7, p 1420 (2022)

Lysine specific demethylase 1 (LSD1; also known as KDM1A), is an epigenetic modulator that modifies the histone methylation status. KDM1A forms a part of protein complexes that regulate the expression of genes involved in the onset and progression of

Externí odkaz: https://doaj.org/article/df089ff6678843aa91f71f1d603fc7ce

Specific Jak3 Downregulation in Lymphocytes Impairs γc Cytokine Signal Transduction and Alleviates Antigen-driven Inflammation In Vivo

Autor: Alicia G Gómez-Valadés, María Llamas, Sílvia Blanch, José C Perales, Juan Román, Lluís Gómez-Casajús, Cristina Mascaró

Publikováno v: Molecular Therapy: Nucleic Acids, Vol 1, Iss C (2012)

Jak3, one of the four members comprising the Jak family of cytosolic tyrosine kinases, has emerged as a promising target for nontoxic immunotherapies. Although a number of Jak inhibitors has already demonstrated efficacy, they suffer from secondary e

Externí odkaz: https://doaj.org/article/b0d6ece5873b4ec8bb0d018c2af6230a

First-in-Human Randomized Trial to Assess Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of the KDM1A Inhibitor Vafidemstat

Autor: Juan Manuel Ferrero-Cafiero, Rosa M. Antonijoan, Cesar Molinero, Tamara Maes, Maria Isabel Arevalo, Montse Puntes, Cristina Mascaró, Jimena Coimbra, Joan Martínez-Colomer, Carlos Buesa

Publikováno v: CNS Drugs
Dipòsit Digital de Documents de la UAB
Universitat Autònoma de Barcelona
CNS DRUGS
r-IIB SANT PAU. Repositorio Institucional de Producción Científica del Instituto de Investigación Biomédica Sant Pau
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Background Vafidemstat, an inhibitor of the histone lysine-specific demethylase KDM1A, corrects cognition deficits and behavior alterations in rodent models. Here, we report the results from the first-in-human trial of vafidemstat in healthy young an

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6f9fea48ac368201b2b0b39aa0a7cb29
http://europepmc.org/articles/PMC7985749

Efficacy of vafidemstat in experimental autoimmune encephalomyelitis highlights the KDM1A/RCOR1/HDAC epigenetic axis in multiple sclerosis

Autor: Michele M.P. Lufino, Serena Lunardi, Natalia Sacilotto, Tamara Maes, Mireia Herrando-Grabulosa, David Rotllant, Carlos Buesa, Jordi Xaus, Paola Dessanti, Carmen Guaza, Xavier Navarro, Elena Gonzalez-Rey, Cristina Mascaró, Mario Delgado, F. L. Cavalcanti, Leyre Mestre

Background Vafidemstat (ORY-2001) is a clinical stage inhibitor of the Lysine Specific Demethylase KDM1A in development for treatment of neurodegenerative and psychiatric diseases. KDM1A demethylates H3K4me1/2 and together with the histone deacetylas

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::afc502a6fe4bd89e62039ecf96871e3e
https://doi.org/10.21203/rs.3.rs-114482/v4

Direct Measurement of KDM1A Target Engagement Using Chemoprobe-based Immunoassays

Autor: Raquel Ruiz Rodriguez, Tamara Maes, Cristina Mascaró

Publikováno v: Journal of Visualized Experiments.

The assessment of the target engagement, defined as the interaction of a drug with the protein it was designed for, is a basic requirement for the interpretation of the biological activity of any compound in drug development or in basic research proj

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0a1b90e14e85fc7600a3efb509b65306
https://doi.org/10.3791/59390-v