/home/corante/public_html/pipeline/ en-us derek-lowe@sbcglobal.net 2008-07-16T07:52:08-05:00 hourly 1 2000-01-01T12:00+00:00 http://pipeline.corante.com/archives/2008/07/16/receptors_cant_live_with_em_cant_understand_em.php At various points in my drug discovery career, I’ve worked on G-protein-coupled receptor (GPCR) targets. Most everyone in the drug industry has at some point – a significant fraction of the known drugs work through them, even though we have... 73443@/home/corante/public_html/pipeline/ Biological News 2008-07-16T07:52:08-05:00 http://pipeline.corante.com/archives/2008/07/11/sharing_the_enlightenment.php Here's an interesting idea: Merck, Lilly, and Pfizer are bankrolling a startup company to look for new technologies for drug development. Enlight Biosciences will focus on the biggest bottlenecks and risk points in the process, including new imaging techniques for... 73433@/home/corante/public_html/pipeline/ Business and Markets 2008-07-11T07:37:23-05:00 http://pipeline.corante.com/archives/2008/06/03/oops.php We recently encountered a problem that’s (unfortunately) a rather common one. An enzyme assay turned up an interesting hit compound, with some characteristics that we were hoping to see for leads against our target. A re-test showed that yes, the... 73345@/home/corante/public_html/pipeline/ Life in the Drug Labs 2008-06-03T07:20:14-05:00 http://pipeline.corante.com/archives/2008/05/20/the_miracle_solvent.php For those who were wondering, my copper reactions the other day worked out just fine. They started out a beautiful blue (copper iodide and an amino acid in straight DMSO – if that’s not blue it’s maybe going to be... 73321@/home/corante/public_html/pipeline/ Life in the Drug Labs 2008-05-20T07:19:37-05:00 http://pipeline.corante.com/archives/2008/04/03/whose_guess_is_better.php I was having a discussion the other day about which therapeutic areas have the best predictive assays. That is, what diseases can you be reasonably sure of treating before your drug candidate gets into (costly) human trials? As we went... 73209@/home/corante/public_html/pipeline/ Animal Testing 2008-04-03T07:19:01-05:00 http://pipeline.corante.com/archives/2008/03/27/start_small_start_right.php There’s an excellent paper in the most recent issue of Chemistry and Biology that illustrates some of what fragment-based drug discovery is all about. The authors (the van Aalten group at Dundee) are looking at a known inhibitor of the... 73187@/home/corante/public_html/pipeline/ In Silico 2008-03-27T07:30:02-05:00 http://pipeline.corante.com/archives/2008/02/14/getting_real_with_real_cells.php I’ve been reading an interesting paper from JACS with the catchy title of “Optimization of Activity-Based Probes for Proteomic Profiling of Histone Deacetylase Complexes”. This is work from Benjamin Cravatt's lab at Scripps, and it says something about me, I... 73111@/home/corante/public_html/pipeline/ Biological News 2008-02-14T08:28:28-05:00 http://pipeline.corante.com/archives/2008/01/29/the_animal_testing_hierarchy.php I've had some questions about animal models and testing, so I thought I'd go over the general picture. As far as I can tell, my experience has been pretty representative. There are plenty of animal models used in my line... 73067@/home/corante/public_html/pipeline/ Animal Testing 2008-01-29T08:30:06-05:00 http://pipeline.corante.com/archives/2008/01/22/these_fragments_i_have_shored_against_my_ruins.php There’s been a big trend the last few years in the industry to try to build our molecules up from much smaller pieces than usual. “Fragment-based” drug discovery is the subject of many conferences and review articles these days, and... 73042@/home/corante/public_html/pipeline/ Drug Assays 2008-01-22T09:23:08-05:00 http://pipeline.corante.com/archives/2007/12/11/a_bad_assay_better_than_none.php Man, do we ever have a lot of assays in this business. Almost every drug development project has a long list of them, arranged in what we call a screening cascade. You check to make sure that your new molecule... 72929@/home/corante/public_html/pipeline/ Drug Development 2007-12-11T08:27:34-05:00 http://pipeline.corante.com/archives/2007/10/11/let_us_now_turn_to_the_example_of_yo_mama.php Now we open the sedate, learned pages of Nature Methods, a fine journal that specializes in new techniques in molecular and chemical biology. In the August issue, the correspondence section features. . .well, a testy response to a paper that... 72769@/home/corante/public_html/pipeline/ The Scientific Literature 2007-10-11T07:34:21-05:00 http://pipeline.corante.com/archives/2007/08/20/the_current_cancer_longjump_record.php As I've mentioned before, advances in molecular biology have continued to make all sorts of brute-force approachs possible - things that would have been laughed at (or, more likely, not even proposed at all) a few years ago. Another recent... 72611@/home/corante/public_html/pipeline/ Cancer 2007-08-20T06:38:47-05:00 http://pipeline.corante.com/archives/2007/07/10/travels_in_numerica_deserta.php There's a problem in the drug industry that people have recognized for some years, but we're not that much closer to dealing with it than we were then. We keep coming up with these technologies and techniques which seem as... 72481@/home/corante/public_html/pipeline/ Drug Assays 2007-07-10T18:09:56-05:00 http://pipeline.corante.com/archives/2007/04/26/less_than_zero.php When I wrote about lousy animal models of disease a few days ago, there was a general principle at the back of my mind. (There generally is - my wife, over the years, has become accustomed to the sudden dolly-back... 72260@/home/corante/public_html/pipeline/ Drug Assays 2007-04-26T19:27:33-05:00 http://pipeline.corante.com/archives/2007/03/12/no_shortcuts.php I wanted to link tonight to the "Milkshake Manifesto" over at OrgPrep Daily. It's a set of rules for med-chem, and looking them over, I agree with them pretty much across the board. There's a general theme in them of... 72116@/home/corante/public_html/pipeline/ Drug Assays 2007-03-12T20:01:51-05:00