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Posts tagged with "Chemical Biology"

  • Chemical Biology

    Ignoring the Literature, Selectively

    Very little time for blogging today (travel), but I wanted to pass on some words of wisdom from Kevan Shokat, from a recent Perspectives piece in Nature Reviews Cancer. Talking about chemical probes, and how to know if they’re valid enough to work with, he suggests that you need to see dose-response data (for one… Read More
  • Cancer

    MTH1: From Hot Topic to Devalidation?

    Here’s an argument that’s been going on inside the oncology drug development world over the last few years: is the enzyme MTH1 a great cancer target or a complete waste of time? MTH1, also known as NUDT1, degrades phosphates of 8-oxoguanine, an oxidized form of the regular guanine that cells know and love. That enzymatic… Read More
  • Cancer

    How to Know When a New Target is Really a New Target

    This is an excellent article, and the title is self-recommending: “Common Pitfalls in Preclinical Cancer Target Validation”. The abstract speaketh the truth: An alarming number of papers from laboratories nominating new cancer drug targets contain findings that cannot be reproduced by others or are simply not robust enough to justify dr… Read More
  • Biological News

    Thinking About Genetics and Disease

    Robert Plenge has an excellent post here, drawing on this recent paper from authors at Stanford. It’s on the idea of polygenic traits and disease, a very worthwhile subject considering what’s going on in the drug industry these days. I say that because I’ve been making the joke, for some time now, that if you were… Read More
  • Biological News

    Making Sure of the Chemistry in Chemical Biology

    There are a lot of interesting and useful experiments you can do to test interactions with DNA in the living cell. Chromatin Immunoprecipitation Sequencing (ChIP-Seq) is a well-known one to spot protein-DNA interactions, and the graphic at right (from the Swiss Institute of Bioinformatics) will show you broadly how it works. Proteins that are inter… Read More
  • Cancer

    Palladium Couplings – Inside Living Cells

    I only have time for a short post this morning, but here’s a technique that I had never thought about: palladium-catalyzed drug synthesis inside the target cells. There have been a few reports of activation of prodrugs via intracellular Pd catalysis (such as this one), but it seems like a real challenge to get both… Read More
  • Biological News

    A Look at Antibody Therapies

    Since we were just talking about antibody therapies in immuno-oncology, here’s a timely column by Bruce Booth at LifeSciVC on antibody therapies in general. It’s well worth a read if, like many small-molecule drug discovery folks, you haven’t had to keep up with that area. I’ve written a few times over the years about how… Read More
  • Biological News

    Silently Affecting the Immune System?

    Here’s a new paper in Nature Chemical Biology that might be lifting the lid on a poorly-understood set of side effects. A multi-institution team (centered in Vienna) has taken peripheral blood mononuclear cells (PBMCs, basically the leukocytes and monocytes) from a single patient and looked for immunomodulatory effects of known drugs. (The si… Read More
  • Chemical Biology

    Protein Degradation Time

    I’ve written a couple of times about the technique for selectively targeting and destroying proteins by forcing them to be ubiquitinated and hauled off to the proteosome. Both the Bradner lab (at Harvard/Dana-Farber) and the Crews lab at Yale found ways to do this a couple of years ago through broadly similar methods. You create… Read More
  • Biological News

    Fragment Screening in Cells – It’s Great

    I’ve very much been enjoying this paper, on fragment-based chemogenomics in whole cells. That’s the sort of blurb, I admit, that’s probably going to make you immediately want to read the rest of the paper, or immediately go do something else (all the way up to “podiatrist appointment”). And I understand those impulses. Read More
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