Lacal, Juan CarlosZimmerman, TahlCampos, Joaquín M.2022-09-302022-09-302021-05-25Lacal JC, Zimmerman T, Campos JM. Choline Kinase: An Unexpected Journey for a Precision Medicine Strategy in Human Diseases. Pharmaceutics. 2021 May 25;13(6):788http://hdl.handle.net/10668/4203Choline kinase (ChoK) is a cytosolic enzyme that catalyzes the phosphorylation of choline to form phosphorylcholine (PCho) in the presence of ATP and magnesium. ChoK is required for the synthesis of key membrane phospholipids and is involved in malignant transformation in a large variety of human tumours. Active compounds against ChoK have been identified and proposed as antitumor agents. The ChoK inhibitory and antiproliferative activities of symmetrical bispyridinium and bisquinolinium compounds have been defined using quantitative structure-activity relationships (QSARs) and structural parameters. The design strategy followed in the development of the most active molecules is presented. The selective anticancer activity of these structures is also described. One promising anticancer compound has even entered clinical trials. Recently, ChoKα inhibitors have also been proposed as a novel therapeutic approach against parasites, rheumatoid arthritis, inflammatory processes, and pathogenic bacteria. The evidence for ChoKα as a novel drug target for approaches in precision medicine is discussed.enAtribución 4.0 Internacionalhttp://creativecommons.org/licenses/by/4.0/Phospholipids metabolismCholine kinaseBispyridinium compoundsBisquinolinium compoundsQSARAnticancer drugsRheumatoid arthritisParasitesPathogenic bacteriaInflammatory diseasePhosphorylationColina quinasaRelación estructura-actividad cuantitativaAntineoplásicosArtritis reumatoideParásitosFosforilcolinaFosforilaciónMedical Subject Headings::Organisms::Eukaryota::Animals::Chordata::Vertebrates::Mammals::Primates::Haplorhini::Catarrhini::Hominidae::HumansMedical Subject Headings::Chemicals and Drugs::Enzymes and Coenzymes::Enzymes::Transferases::Phosphotransferases::Phosphotransferases (Alcohol Group Acceptor)::Choline KinaseMedical Subject Headings::Chemicals and Drugs::Organic Chemicals::Amines::Quaternary Ammonium Compounds::Trimethyl Ammonium Compounds::Choline::PhosphorylcholineMedical Subject Headings::Chemicals and Drugs::Inorganic Chemicals::Elements::Metals, Alkaline Earth::MagnesiumMedical Subject Headings::Organisms::Eukaryota::Animals::Invertebrates::ParasitesMedical Subject Headings::Phenomena and Processes::Chemical Phenomena::Biochemical Phenomena::Structure-Activity Relationship::Quantitative Structure-Activity RelationshipMedical Subject Headings::Phenomena and Processes::Metabolic Phenomena::Metabolism::PhosphorylationMedical Subject Headings::Chemicals and Drugs::Chemical Actions and Uses::Pharmacologic Actions::Therapeutic Uses::Antineoplastic AgentsMedical Subject Headings::Diseases::NeoplasmsMedical Subject Headings::Diseases::Musculoskeletal Diseases::Rheumatic Diseases::Arthritis, RheumatoidMedical Subject Headings::Chemicals and Drugs::Lipids::PhospholipidsMedical Subject Headings::Organisms::BacteriaMedical Subject Headings::Chemicals and Drugs::Heterocyclic Compounds::Heterocyclic Compounds, 2-Ring::Purines::Purine Nucleotides::Adenine Nucleotides::Adenosine Triphosphatereview article34070409Acceso abierto10.3390/pharmaceutics130607881999-4923PMC8226952