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Ligands for Ser/Thr phosphoprotein phosphatases: a patent review (2005-2015).
Lajarín-Cuesta, Rocío; Arribas, Raquel L; De Los Ríos, Cristóbal.
Afiliación
  • Lajarín-Cuesta R; a Instituto Teófilo Hernando, Departamento de Farmacología y Terapéutica, Facultad de Medicina , Universidad Autónoma de Madrid , Madrid , Spain.
  • Arribas RL; a Instituto Teófilo Hernando, Departamento de Farmacología y Terapéutica, Facultad de Medicina , Universidad Autónoma de Madrid , Madrid , Spain.
  • De Los Ríos C; a Instituto Teófilo Hernando, Departamento de Farmacología y Terapéutica, Facultad de Medicina , Universidad Autónoma de Madrid , Madrid , Spain.
Expert Opin Ther Pat ; 26(3): 389-407, 2016.
Article en En | MEDLINE | ID: mdl-26853448
INTRODUCTION: The role played by phosphoprotein phosphatases (PPP) enzymes makes them of interest as therapeutic targets to treat pathologies including neurodegenerative diseases, cancer and autoimmune diseases, but also liable to cause severe side effects. This fact has hindered the study of PPP ligands as potential drugs. Fortunately, recent advances in the comprehension of PPP biochemistry have given rise to the development of refined pharmacological strategies to selectively target phosphatases and limit the possible generation of adverse reactions. AREAS COVERED: This review summarizes the most relevant patents claiming the use of PPP ligands to treat human diseases in the last decade (2005-2015). It also includes some pharmacological strategies aiming to indirectly modulate PPP functionality by interacting with PPP-regulating enzymes. EXPERT OPINION: There is still much work to be done to validate PPP enzymes as eligible targets for the development of new drugs. The most significant barrier is likely to be persuading the majority of the scientific community that PPP enzymes are not too unspecific. Few patents disclosed the rational design of direct PPP ligands, while many inventions relied on long chain peptides-based approaches. Overall, the future of ligands for PPP enzymes as therapeutics seems both challenging and exciting.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Diseño de Fármacos / Fosfoproteínas Fosfatasas / Terapia Molecular Dirigida Límite: Animals / Humans Idioma: En Revista: Expert Opin Ther Pat Asunto de la revista: TERAPEUTICA Año: 2016 Tipo del documento: Article País de afiliación: España Pais de publicación: Reino Unido

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Diseño de Fármacos / Fosfoproteínas Fosfatasas / Terapia Molecular Dirigida Límite: Animals / Humans Idioma: En Revista: Expert Opin Ther Pat Asunto de la revista: TERAPEUTICA Año: 2016 Tipo del documento: Article País de afiliación: España Pais de publicación: Reino Unido