/home/corante/public_html/pipeline/ en-us derek-lowe@sbcglobal.net 2010-03-15T07:22:13-05:00 hourly 1 2000-01-01T12:00+00:00 http://pipeline.corante.com/archives/2010/03/15/tricors_troubles.php It's easy to lose sight of what a drug is supposed to do. Many conditions come on so slowly that we have to use blood chemistry or other markers to see the progress of therapy in a realistic time. And... 74337@/home/corante/public_html/pipeline/ Cardiovascular Disease 2010-03-15T07:22:13-05:00 http://pipeline.corante.com/archives/2010/03/12/garage_biotech.php Freeman Dyson has written about his belief that molecular biology is becoming a field where even basement tinkerers can accomplish things. Whether we're ready for it or not, biohacking is on its way. The number of tools available (and the... 74333@/home/corante/public_html/pipeline/ Biological News 2010-03-12T07:22:25-05:00 http://pipeline.corante.com/archives/2010/03/02/why_you_dont_want_to_make_deathstarsized_drugs.php I was just talking about greasy compounds the other day, and reasons to avoid them. Right on cue, there's a review article in Expert Opinion in Drug Discovery on lipophilicity. It has some nice data in it, and I wanted... 74306@/home/corante/public_html/pipeline/ Pharma 101 2010-03-02T08:07:15-05:00 http://pipeline.corante.com/archives/2010/03/01/calorimetry_what_say_you.php I've been involved in a mailing list discussion that I wanted to open up to a wider audience in drug discovery, so here goes. We spend our time (well, a lot of it, when we're not filling out forms) trying... 74303@/home/corante/public_html/pipeline/ Drug Assays 2010-03-01T09:07:36-05:00 http://pipeline.corante.com/archives/2010/02/19/two_for_one_sale.php A double complaint this morning, and both from the same literature item - if I were charging anything for the blog, I'd say that it's delivering value for the money. At any rate, the first kvetch is something that I... 74290@/home/corante/public_html/pipeline/ The Scientific Literature 2010-02-19T10:01:06-05:00 http://pipeline.corante.com/archives/2010/02/08/polluting_the_literature_with_pains.php There's an article out from a group in Australia on the long-standing problem of "frequent hitter" compounds. Everyone who's had to work with high-throughput screening data has had to think about this issue, because it's clear that some compounds are... 74266@/home/corante/public_html/pipeline/ The Scientific Literature 2010-02-08T08:41:34-05:00 http://pipeline.corante.com/archives/2010/01/29/merck_and_sirna.php Xconomy has a look inside the Merck-Sirna acquisition, an interview with Merck's head of that area. As you'd guess, he emphasizes that one of the biggest challenges in the field is delivery, and he makes the pitch that this is... 74250@/home/corante/public_html/pipeline/ Business and Markets 2010-01-29T11:09:09-05:00 http://pipeline.corante.com/archives/2010/01/26/the_infinitely_active_impurity.php Yesterday's post touched on something that all experienced drug discovery people have been through: the compound that works - until a new batch is made. Then it doesn't work so well. What to do? You have a fork in the... 74238@/home/corante/public_html/pipeline/ Drug Assays 2010-01-26T08:29:04-05:00 http://pipeline.corante.com/archives/2010/01/25/gsk_and_sirtris_a_bit_more.php Nature has a short item on the Pfizer paper that questions the reproducibility of some key sirtuin work (covered here and here). There are some good points to temper the pessimism. Leonard Guarente of MIT, a key pioneer in the... 74235@/home/corante/public_html/pipeline/ Aging and Lifespan 2010-01-25T08:39:59-05:00 http://pipeline.corante.com/archives/2010/01/12/the_sirtris_compounds_worthless_really.php As followers of the drug industry know, GlaxoSmithKline famously paid $720 million to buy Sirtris Pharmaceuticals in 2008. Sirtris is the most high-profile shop working on sirtuins and resveratrol-like pharmacology, which subject has received a massive amount of press (some... 74213@/home/corante/public_html/pipeline/ Aging and Lifespan 2010-01-12T07:23:20-05:00 http://pipeline.corante.com/archives/2010/01/05/run_it_past_the_chemists.php I missed this paper when it came out back in October: "Reactome Array: Forging a Link Between Metabolome and Genome". I'd like to imagine that it was the ome-heavy title itself that drove me away, but I have to admit... 74199@/home/corante/public_html/pipeline/ The Scientific Literature 2010-01-05T07:27:52-05:00 http://pipeline.corante.com/archives/2009/12/10/selective_scaffolds.php We spend a lot of time in this business talking about molecular scaffolds - separate chemical cores that we elaborate into more advanced compounds. And there's no doubt that such things exist, but is part of the reason they exist... 74178@/home/corante/public_html/pipeline/ Drug Development 2009-12-10T08:40:12-05:00 http://pipeline.corante.com/archives/2009/12/07/why_dont_we_have_more_proteinprotein_drug_molecules.php Almost all of the drugs on the market target one or more small-molecule binding sites on proteins. But there's a lot more to the world than small-molecule binding sites. Proteins spend a vast amount of time interacting with other proteins,... 74171@/home/corante/public_html/pipeline/ Drug Industry History 2009-12-07T09:02:35-05:00 http://pipeline.corante.com/archives/2009/11/30/more_binding_site_weirdness.php Now here's an oddity: medicinal chemists are used to seeing the two enantiomers (mirror image compounds, for those outside the field) showing different activity. After all, proteins are chiral, and can recognize such things - in fact, it's a bit... 74164@/home/corante/public_html/pipeline/ Chemical News 2009-11-30T12:23:31-05:00 http://pipeline.corante.com/archives/2009/11/17/side_effects_predicted.php There's a new paper out in Nature that presents an intriguing way to look for off-target effects of drug candidates. The authors (a large multi-center team) looked at a large number of known drugs (or well-characterized clinical candidates) and their... 74146@/home/corante/public_html/pipeline/ In Silico 2009-11-17T12:14:57-05:00