Category Archives: Reviews

MDM2-p53 protein-protein interaction inhibitors


The successful development of inhibitors of protein-protein interactions remains a formidable challenge for medicinal chemists. An excellent review highlights some successes in this field and ascribes the low tractability of these targets to: The large contact surfaces between proteins (~1,500–3,000 … Continue reading

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More physicochemical musings & ChEMBL


Following on from his earlier papers (e.g. ADMET rules of thumb for candidate drug design), Gleeson’s most recent publication in Nature Reviews|Drug Discovery details a now familiar tale of physicochemical woe associated with the failure of many medicinal chemistry programmes to … Continue reading

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Review: Optimizing CNS access


Neurotherapeutic agents generally illicit their effects by acting on receptors in the central nervous system (CNS) and a short review in Expert Opin. Drug Discov. highlights the current best practices and recent developments in targeting molecules to the brain.  The … Continue reading

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Review: Bioisosteres in Drug Design


An excellent J.Med.Chem. perspective titled ‘Synopsis of Some Recent Tactical Applications of Bioisosteres in Drug Design‘ has just published (The article is based on a short course presented at an ACS Prospectives conference in 2009).  The author gives a brief … Continue reading

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Enhancing solubility by disrupting crystal packing


Drug candidates can be classified, according to the BCS system, into four groups on the basis of their permeability and aqueous solubility.  Molecules with lower solubility tend to be more difficult to develop and are subject to closer scrutiny by … Continue reading

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Reducing bioactivation potential by chemical design


Continuing the theme of an earlier post, an excellent article in Current Topics in Medicinal Chemistry looks at the issue of adverse drug events associated with the formation of reactive intermediates.  The authors (from Novartis) give some background to drug-related … Continue reading

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Review: Gamma-secretase modulators


An excellent review titled ‘γ-Secretase Modulators as Potential Disease Modifying Anti-Alzheimer’s Drugs’ has recently published in J.Med.Chem. The review gives some background to the disease and to the generally, although not universally, accepted hypothesis that amyloid plays a key role … Continue reading

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