Current Opinion in Drug Discovery & Development
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Small-molecule modulation of cellular chaperones to treat protein misfolding disorders.
The correct folding of proteins is a fundamental process in the normal physiological functioning of cells, and is mediated by cellular chaperones including members of the Hsp70 family. Many diseases are caused by a failure of cellular chaperones to adequately maintain correct protein folding, and ha...
Recent developments in allene-based synthetic methods.
Presented is a review of the advances in synthetic methodology that make use of the allene functional group, with emphasis on catalytic asymmetric transformations and new mechanistic insights. The review covers the period from January 2007 to May 2008 and focuses on intra- and intermolecular cycload...
Applications of chiral allylmetallating agents toward the synthesis of oxygen heterocyles.
Oxygen heterocycles represent an important structural feature in many biologically active natural products. Consequently, new methods for the stereoselective synthesis of these units are continuously being sought. Allylmetal reagents have emerged as powerful tools in these efforts. This review summa...
Lead optimization via high-throughput molecular docking.
Structure-based lead optimization approaches are increasingly playing a role in the drug-discovery process. Recent advances in 'high-throughput' molecular docking methods and examples of their successful use in lead optimization are reviewed. Measures of docking accuracy, scoring function comparison...
Embracing complexity in drug discovery.
Automated synthesis of heterocycles on solid supports.
The creation of novel diverse heterocycle libraries is an indispensable requirement of modern drug discovery processes. Currently, library sizes of over 10,000 discrete compounds are viable using programmed synthesis on solid supports. This review discusses the recent advances in the automated solid...
The continuing contribution of biodiversity to drug discovery.
Orthosteric- and allosteric-induced ligand-directed trafficking at GPCRs.
Many orthosteric agonists differentially activate downstream effectors of GPCRs. Such defined induction of signaling has strongly supported the hypothesis termed 'ligand-directed trafficking of receptor signaling' (LDTRS). More recently, subtype-selective GPCR activators, such as allosteric agonists...
Hsp90 inhibitors: clinical development and future opportunities in oncology therapy.
The development of small molecular mass Hsp90 inhibitors has become an increasingly competitive field of research in recent years. Progress in preclinical and clinical research has provided increasing evidence that Hsp90 represents a promising molecular target for the treatment of cancer and other d...
Roles of CD44 in chemical-induced liver injury.
CD44 has been identified as one of the adhesion molecules that regulate cell migration in inflamed tissue. The principal ligand of CD44 is hyaluronan, and CD44 is involved in the metabolism of this compound. Furthermore, an increasing quantity of evidence suggests that CD44 has various functions rel...