Challenges and approaches for assay development of membrane and membrane-associated proteins in drug discovery

Prog Mol Biol Transl Sci. 2010:91:209-39. doi: 10.1016/S1877-1173(10)91007-7.

Abstract

In addition to its role as a barrier between the cytoplasm and the extracellular milieu, the cell membrane is a scaffold for a diverse collection of receptors and enzymes. The organization afforded by this scaffold serves to ensure an efficient interaction between the components of the membrane. The desire to maintain this organization in solution is a challenge for the appropriate interrogation of these biochemical components. This chapter will discuss strategies that allow biochemical analysis of membrane-associated enzymes within standard biochemical reactions. The advantages of these screening strategies in identifying valuable compounds from compound libraries and in understanding the intricacies of complex multiprotein complexes (i.e., chemotaxis) will be discussed.

Publication types

  • Review

MeSH terms

  • Animals
  • Bacteria / drug effects
  • Bacteria / metabolism
  • Chemotaxis
  • Drug Discovery / methods*
  • ErbB Receptors / drug effects
  • ErbB Receptors / metabolism
  • Humans
  • Membrane Proteins / drug effects*
  • Membrane Proteins / metabolism*
  • Poliovirus / drug effects
  • Poliovirus / physiology
  • Signal Transduction
  • Thromboplastin / drug effects
  • Thromboplastin / metabolism
  • Virus Internalization / drug effects

Substances

  • Membrane Proteins
  • Thromboplastin
  • ErbB Receptors