Knockouts model the 100 best-selling drugs—will they model the next 100?

By B. Zambrowicz, A. Sands. 2003

390 citations recorded by the source corpus.

Subfields: Computational Theory and Mathematics, Molecular Biology

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In Computational Theory and Mathematics

In Molecular Biology

Citations in the corpus

Fluorescence-detection size-exclusion chromatography for precrystallization screening of integral membrane proteins. (2006, background): “In particular, the structures of membrane proteins, including receptors, channels, and transporters, are especially important because these molecules are the targets of most drugs currently prescribed (Zambrowicz and Sands, 2003).”
Drugs, their targets and the nature and number of drug targets (2006, background): “For example, a lack of effect of a drug in mice lacking a particular target can provide strong support that the effects of the drug are mediated by that target (for a review on knockout mice in target validation, see Ref”
Molecular imaging in drug development (2008, background): “Moreover, despite dramatically increased investment, the rate of introduction of novel drugs has remained relatively constant over the past 30 years, with only two to three agents in new drug classes per year eventually making it to marke”
Chemical space and biology (2004, background): “For example, between 1994 and 2001, just 22 drugs that modulate new targets were approve”
Discovery and resupply of pharmacologically active plant-derived natural products: A review (2015, background): “Such genetically modified rodentmodels are successfully applied for the verification of in vivo efficacy prior to human trials, for the discovery of new pharmacological targets, as well as to assist the elucidation of pharmacological mechanisms of action (Foster et al., 2014; Zambrowicz and Sands, 2”
Evaluating drug targets through human loss-of-function genetic variation (2019, neutral): “Studying human gene inactivation can illuminate human biology and guide drug target selection, complementing mouse knockout studies 42 , but analysis of any one gene requires genome-wide context to set expectations and guide inferences.”
Network pharmacology: the next paradigm in drug discovery. (2008, background): “in the mouse genome and profile each knockout across a battery of phenotypic assays has revealed that as few as 10% of knockouts demonstrate phenotypes that may be of value for drug target validatio”