#kobilka

[pharmtastic]

Noble prizes?

I'm spending the night at the lab to finish up some writing work but having done with it earlier than expected I thought why not add a new post. Yes, its been a while but hey I still remember the password to my tumblr account! 

I never got around to writing about the Nobel prize in chemistry this year which was awarded to the grandfather of GPCRs, Bob Leftkowitz sharing it with his protege Brian Kobilka. I will not dwell too much into whether they deserved it or what exactly won them the award, as a number of fellow bloggers and science journalists have dealt into this in great detail over the past few months. But I would like to make just one point that if you can spare about 50 mins, I would recommend watching their Nobel interview -  

http://www.nobelprize.org/mediaplayer/index.php?id=1860

The stark contrast in their demeanor during the interview is very interesting and is rather intriguing as to how they managed to get along over the years with such a massive difference in personalities (as pointed our by Bob himself). It is my belief that 'it' (it being this combined, massive undertaking of GPCRs that took over 40 years) would never have been such as success if Kobilka was the predecessor with Bob being his student. This is no offense to Kobilka's mentorship skills.

Anyway, lets move on to another monetary prize that has raised some eyebrows in the recent weeks - The Life science breakthrough prize!! The $3 million award to a select few scientists focusing on 'breakthrough' therapeutic strategies mainly targeting cancers and some neuro-degenerative diseases has elicited a rather bitter and unwarranted antipathy. I couldn't disagree more with this aversion towards awarding such large sums of money to a select few.

First and foremost, it is a privately funded award trying to encourage rapid development of therapeutic strategies for some diseases that could potentially wipe out the human race in the coming years unless they are conquered soon. Secondly, the wide (and rightly so) distribution of federal money although has given numerous breakthroughs over the years, have come along in far too few numbers and too far apart. This monetary push from these tech magnates with stuffed wallets may turn out be the push that has been missing in this field.  

[polishsocial]

Polish American Scientist wins Nobel Prize in Chemistry

Polish American Scientist and Stanford University Professor Brian Kobilka and his research partner Robert Lefkowitz won the 2012 Nobel Prize in chemistry Wednesday for studies of proteins that let body cells respond to signals from the outside.

The Royal Swedish Academy of Sciences said the two researchers had made groundbreaking discoveries on an important family of receptors, known as G-protein-coupled receptors.

To read more, click here.

[pharmtastic]

Why hasn't Struture-based drug design produced any blockbuster molecules yet?

For my Pharmacology class I am required to write a review paper this semester and I had decided to cover the use of x-ray structure of beta 2-adrenergic receptor to screen and design ligands. Obviously, I would be basing most of the paper on the work that has been done in Dr. Kobilka's lab at Stanford University. Their recent paper - "Structure-based discovery of Beta 2-adrenergic receptor ligands" in PNAS is what got me interested into this relatively new field of virtual screening. This paper deals with the use of virtual screening techniques to determine a list of probable targets using standard docking software programs.

My Prof. wants me to cover the clinical implications of these compounds obtained through virtual screening, and rightly so, considering my course is quite clinical-based. But unfortunately, I haven't found a single compound which has been obtained from these screens that has reached the market or even the clinical trials stage. Which makes me wonder as what might be stopping the Big Pharma from turning these into pharmaceuticals? Is it because that they comprise of no new therapeutic advantages (certainly may have some advantage) over the ligands previously obtained from traditional chemical synthesis and HTS? But I wouldn't think so considering the fact that this has never stopped them from developing such vast heaps of me-too drugs over the past 50 years. I guess they are still trying to get a feel of these compounds and its just too early for such questions.