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- W2029152175 abstract "Abstract About 330 targets bind approved drugs, 270 encoded by the human genome and 60 belonging to pathogenic organisms. A large number of druggable targets have been recently proposed from preclinical and first clinical data, but a huge reservoir of putative drug targets, possibly several thousands, remains to be explored. This overview considers the different types of ligands and their selectivity in the main superfamilies of drug targets, enzymes, membrane transporters and ion channels, and the various classes of membrane and nuclear receptors with their signalling pathway. Recently approved drugs such as monoclonal antibodies, tyrosine kinase and proteasome inhibitors, and major drugs under clinical studies are reviewed with their molecular target and therapeutic interest. The druggability of emerging targets is discussed, such as multidrug resistance transporters and cystic fibrosis transmembrane conductance regulator (CFTR), hyperpolarization‐activated cyclic nucleotides‐gated (HCN), cyclic nucleotide‐gated (CNG) and transient receptor potential (TRP) ion channels, tumour necrosis factor (TNF) and receptor activator of NFκB (RANK) receptors, integrins, and orphan or recently deorphanized G‐protein‐coupled and nuclear receptors. Large advances have been made in the therapeutical use of recombinant cytokines and growth factors (i.e. tasonermin, TNFα‐1a; becaplermin, platelet‐derived growth factor (PDGF); dibotermin‐alpha, bone morphogenetic proteins (BMP)2; anakinra, interleukin‐1 receptor antagonist protein (IRAP), and in enzyme replacement therapy, i.e. algasidase (alpha‐galactosidase) and laronidase (alpha‐ l ‐iduronidase). New receptor classes are emerging, e.g. membrane aminopeptidases, and novel concepts are stimulating drug research, e.g. epigenetic therapy, but the molecular target of some approved drugs, such as paracetamol and imidazolines, still need to be identified." @default.
- W2029152175 created "2016-06-24" @default.
- W2029152175 creator A5068787947 @default.
- W2029152175 creator A5086644895 @default.
- W2029152175 date "2008-01-30" @default.
- W2029152175 modified "2023-10-14" @default.
- W2029152175 title "Drugs and their molecular targets: an updated overview" @default.
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- W2029152175 doi "https://doi.org/10.1111/j.1472-8206.2007.00548.x" @default.
- W2029152175 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/18251718" @default.
- W2029152175 hasPublicationYear "2008" @default.
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