Gpcrs: A solid view of GPCRs

  title={Gpcrs: A solid view of GPCRs},
  author={Suzanne J. Farley},
  journal={Nature Reviews Drug Discovery},
  • S. Farley
  • Published 1 November 2003
  • Biology
  • Nature Reviews Drug Discovery
Inhibitors of heat-shock protein 90 (Hsp90) — which regulates the function and stability of key signalling proteins — have been shown to selectively kill cancer cells, despite the fact that Hsp90 is highly expressed in most cells. Kamal et al. now provide an explanation for this selectivity: Hsp90 in tumour cells exists in a functionally distinct molecular form that has a 100-fold higher affinity for the Hsp90 inhibitor 17-allylaminogeldanamycin (17-AAG; now in Phase I clinical trials) than… 

The therapeutic potential of NS3 protease inhibitors in HCV infection

The impressive reduction of HCV RNA plasma levels observed with two of these inhibitors in clinical trials has undoubtedly illustrated the potential of this viral enzyme-targeted drug discovery approach.

Construction of an in vitro trans-sialylation system: surface display of Corynebacterium diphtheriae sialidase on Saccharomyces cerevisiae

An in vitro trans-sialylation system is constructed by reconstructing the exogenous sialoglycoconjugate synthesis system of pathogens on the surfaces of yeast cells and shows its potential as a useful whole cell biocatalyst for the transfer of sialic acid as well as the hydrolysis of N-glycans containing α(2,3)- and α( 2,6)-linked sIALic acids for glycoprotein remodeling.

Consolidation of molecular testing in clinical virology

The history and development of virology diagnostic methods are described, dedicating particular emphasis on the gradual evolution and recent advances toward the introduction of multiparametric platforms for the syndromic diagnosis.



The conformation of neurotensin bound to its G protein-coupled receptor

  • S. LucaJim F. White M. Baldus
  • Biology, Chemistry
    Proceedings of the National Academy of Sciences of the United States of America
  • 2003
The conformation of a high-affinity peptide agonist (neurotensin, NT) bound to its GPCR NTS-1, determined by direct structural methods is presented, providing a viable structural template for further pharmacological investigations.

High-resolution solid-state NMR applied to polypeptides and membrane proteins.

Solid-state NMR methods that make use of experimental improvements and allow for the study of multiply or uniformly [(13)C,(15)N]-labeled polypeptides and proteins are discussed.