Work at the turn of the last century summarized at - http://ow.ly/R8Hl led to the lock & key concept #receptor #pharmacology #science
Here's a modern version of the "lock and key concept" for the receptor response - http://ow.ly/R8KN #receptor #pharmacology #science
One problem is how does the binding of a small molecule alter the conformation of a much larger one? #receptor #pharmacology #science
Another problem is how do some binding molecules produce a partial or no response? #receptor #pharmacology #science
These problems & desensitization, fade or tachyphylaxis led to the two state theory - http://ow.ly/R8VQ #receptor #pharmacology
Two state mathematics only solved for the fractional or proportional change - http://ow.ly/R91A #receptor #pharmacology #science
Experiments showing an increased response with increased receptor expression didn't fit with 2 state theory #receptor #pharmacology #science
Also no consensus on what the two states of the receptor are -just active & inactive? #receptor #pharmacology #science
I suggested an alternative math to remove these problems with 2 state theory - http://ow.ly/R9jj #receptor #pharmacology #science
The idea was that the net shift could explain a binding molecule's preference - http://ow.ly/R9qX #receptor #pharmacology #science
The "net shift" (delta RH) could fit many classical dose-response curves - http://ow.ly/R9tj #receptor #pharmacology #science
We proposed that a free thiol produced the 2 (acid-base) receptor states - http://cogprints.org/4095/ #receptor #pharmacology
This was a mechanistic hypothesis of receptor function involving sulfhydryl modulation and redox regulation #receptor #pharmacology #science
This also fit nicely with the "net shift" producing the active state of the receptor #receptor #pharmacology #science
Subsequent work seems to support our observations - http://ow.ly/R9PR #receptor #pharmacology #science
Although much more work remains, it looks promising that a free thiol may explain many receptor responses #receptor #pharmacology #science
receptor activation thiol OR sulfhydryl "two state" - http://ow.ly/R9WI #receptor #pharmacology #science
@davidperrey Never seen a review by Twitter before! @rlanzara is trying it using these hashtags - check it out: #receptor #pharmacology #science
For my very mini (and biased) review of pharmacology - http://ow.ly/Rab6 #receptor #pharmacology #science
Bio Balance - Reference Library - http://www.bio-balance.com/Ref.htm
