Human body consist of around 90 tyrosine kinases. If one tries to target them selectively then what are the factors or measure he/she must be carefully employed?
For instance, if a inhibitor is designed then at the same time that inhibitor has 90 possiblities to target. Then how would, it be possible to get selectivity for only one tyrosine kinase at ONE TIME!!!!
Not sure what the intended purpose is but inhibitors would be the way to go :)
Hii Tamjeed !! Thanks for your answering
Ya it is obvious that the inhibitor may be one of the choice to target the tyrosine kinase but at the same time that inhibitor has 90 possible tyrosine kinase to target. Then how would it be possible to get selectivity for only one tyrosine kinase
Sorry, why would it have 90 possible targets? There is some cross-reactivity with some inhibitors but there are also a number of inhibitors that are very selective.
Tamjeed... thank you for your answering. However you are talking about some selective inhibitors. Now the question is, what they have, so special that they are only selective to particular tyrosine kinase?
The selectivity comes from the favorable energetics the kinase and the inhibitor can achieve when they bind. Kinases in the active form have similar structures but because of differences in sequences and the 'x' factor, they bind to inhibitors with different affinity.
P.S the x factor is anything from inherent flexibility of the protein/conformation changes etc etc
In order to understand the concepts of drug selectivity, e.g. in the field of tyrosine kinases, I highly recommend the following review:
Huggins DJ, Sherman W, Tidor B, J Med Chem. 2012 Feb 23;55(4):1424-44. Rational approaches to improving selectivity in drug design.
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