Derek Lowe's commentary on drug discovery and the pharma industry. An editorially independent blog from the publishers of Science Translational Medicine. All content is Derek’s own, and he does not in any way speak for his employer.
In case you don’t know, there’s officially an effort to try to develop chemical probes for basically every protein in the human proteome. The “Target 2035” initiative has been looking through the literature and finding what you’d expect: power-law distributions that have most people working on proteins that other peopl… Read More
OK, today’s blog post is going to be even weirder than usual – we’re going to wander off into quantum mechanics. And into a particular borderland of it where have been a lot of interesting hypotheses and speculations, but plenty of hand-waving hoo-hah, so it’s important to realize the risks up front. But here we go. Read More
I wanted to note something today that won’t make many headlines outside of biopharma, but it’s just the sort of story that I wish more people knew about. Let’s start with this: there’s a terrible disease called IPF, idiopathic pulmonary fibrosis. Anyone with any medical background knows to beware the word “idiopathic&# Read More
When chemists have a wide range of reactants to choose from to make new compounds, how do they choose which ones to use? “Not randomly” is the answer, even when perhaps it should be. This effect has been noted in medicinal chemistry, where the choice of building blocks (not to mention reactions) for analog synthesis… Read More
Here’s more evidence of the power of the MicroED electron diffraction technique: this new paper reports the structure of two reactive organometallic species whose structures could not be determined by either NMR methods or conventional X-ray crystallography. One of them is the zirconium hydride species known as Schwartz’s reagent (zirco… Read More
I wrote here about a paper from Cold Spring Harbor labs that invalidated MELK as a cancer target. That was straightforward enough: knocking it out via CRISPR across a whole range of cancer cell lines had no effect on their growth at all, so it’s kind of hard to make the case that it’s an… Read More
The ways to mess around with the peer-review process are legion, but these schemes are getting a bit easier to catch. That’s what I take away from this paper, from two bibliographic scientists at Elsevier who set up a system to do just that. One hears tales of reviewers who will look more favorably on… Read More
Since I mentioned a new Mitsunobu-type reaction yesterday, I should note that a new route to hindered ethers has come out this summer from the Baran group at Scripps. Here’s the ChemRxiv version, and here’s the Nature paper that just appeared. And there are more details at the group’s blog here. It’s an electrochemical react… Read More
Well, people have been searching for a reaction like this one for quite a while now: that link describes a catalytic Mitsunobu-like reaction, and the original has always been a transformation that synthetic organic chemists groan about but use anyway. It’s a way of substituting an OH group in one pot with what should be… Read More
Here’s a topic that came up in my Twitter feed the other day – I fear it’s unanswerable, but I’d like to hear what people have to say about it. Drug discovery projects start, of course, from a selection of possible chemical matter and chemical series, and they eventually narrow down to a clinical candidate. Read More
