New ways to target old receptors.
Numerous important drugs target cytokines and growth factors or their receptors. Our understanding of the molecular mechanisms governing receptor activation and signaling has lagged in key areas, however, limiting drug discovery efforts to relatively few basic strategies. Recently, substantial progress has been made on several aspects of this problem. These include improved methods for establishing the mechanism of receptor activation, a clearer understanding of the biochemical basis for differential signaling by ligands that act through a common receptor, new methods for measuring the affinities of steps in receptor activation on live cells, and progress toward a systems level understanding of receptor signaling. These advances are providing a new understanding of the function of these receptors that presents opportunities for the development of improved drugs.
Whitty
Adrian
A
Department of Chemistry, Boston University, Metcalf Center for Science and Engineering, 590 Commonwealth Avenue, Boston, MA 02215-2521, USA. whitty@bu.edu
Riera
Thomas V
TV
D000818:Animals; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D006801:Humans; D008024:Ligands; D018121:Receptors, Cytokine / Q000819:agonists* / Q000037:antagonists & inhibitors* / Q000378:metabolism; D017978:Receptors, Growth Factor / Q000819:agonists* / Q000037:antagonists & inhibitors* / Q000378:metabolism
D008024:Ligands; D018121:Receptors, Cytokine; D017978:Receptors, Growth Factor