drug targeting: G-proteins or protein kinases? - (Jun/25/2008 )
at the moment I think still the most prominent target in small-molecular therapy are G-coupled receptors;
receptor tyrosine kinases are becoming more and more important in drug therapy;
what about direct targeting of G-proteins and non-receptor protein kinases? what is more promissing as a drug target?
heterotrimeric G-protein are linked to various receptors and transduce the signal into the cell by f.i. releasing second messengers which activate among others protein kinases; in my point of view protein kinases have a more subtil regulation mechanism, and therefore should offer a more advanced regulation by small molecules;
or G-proteins are better targets in drug therapy? what is the future perspective of each target, G-protein and non-receptor protein kinase?
receptor tyrosine kinases are becoming more and more important in drug therapy;
what about direct targeting of G-proteins and non-receptor protein kinases? what is more promissing as a drug target?
heterotrimeric G-protein are linked to various receptors and transduce the signal into the cell by f.i. releasing second messengers which activate among others protein kinases; in my point of view protein kinases have a more subtil regulation mechanism, and therefore should offer a more advanced regulation by small molecules;
or G-proteins are better targets in drug therapy? what is the future perspective of each target, G-protein and non-receptor protein kinase?
I don't think this can be generalized as yet. All of them are elusive fellas.
Some lectures here: http://search.vadlo.com/b/q?sn=158621799&a...eting&rel=2