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Covalent drugs are a thing these days: as long as you can get selectivity, theres nothing like a covalent bond to juice up affinity for a target. Screening for covalent fragments is thus a reasonable approach, and multiple researchers have assembled libraries...
Last year we highlighted work out of Ben Cravatts group at Scripps on screening covalent fragments in cells. Now, in a new Cell paper, his group and collaborators at the cole Polytechnique Fdrale de Lausanne, Bristol-Myers Squibb, and the Salk Institute...
This year is finally coming to an end, and as we've done for the past four years, Practical Fragmentswill highlight some of the reviews that we didn't cover previously.In terms of what we didcover, there were several excellent events, including the eleventh...
Last December the first-ever Pacifichem symposium on FBLD was held in Honolulu. Two of the organizers, Martin Scanlon and Ray Norton, invited participants to submit manuscripts to a special issue of Molecules, which has now published.The...
FBLD started early at AstraZeneca (AZ). The first conference Practical Fragmentscovered was held at their erstwhile Alderley Park site; Pete Kenny is an AZ alum, and the company has put at least four fragment-derived drugs into the clinic. Clearly their scientists...
What happens when you expose a reactive, covalent-bond-forming compound to cell extracts (or to living cells)? The answer is complicated. You might expect the compound to go around grabbing every reactive group it sees, shotgunning across the proteins it encounters...