ACVR1 Crystals taken to the Diamond Light Source (Beamline I04.) – no data sets collected.

Following up on the crystals from my last post I sent them along on the last Diamond trip we had to beamline I04 but regrettably didn’t get any usable datasets. Perhaps fortunately there is a possible explanation for this that isn’t just ‘the crystals were a bit too rubbish’. We send our crystals to the Diamond Read More …

Testing Selectivity of USP5 Zf-UBD Analogues with SPR Assay

In a previous post, I tested hit analogues and found compound XSR00035795a (Figure 1) had increased potency and ligand efficiency; however, compound XSR00035795a was also found to bind to HDAC6 Zf-UBD, so it was not selective towards USP5. Figure 1. XSR00035795a We hypothesized that it was possible to extend the aliphatic group on the carboxylic Read More …

Growing co-crystallized fragments to ligands of the transcription factor brachyury (T)

In order to develop ligands addressing different possible binding sites of the transcription factor brachyury, fragments co-crystallized with this protein should be developed into ligands by using the program SparkTM (Cresset®). Brachyury (T, TBXT) is an essential regulator of the notochord development. Brachyury is primarily expressed in the embryo but not in the majority of normal Read More …

Re-Purification of ALK2 for crystallisation with different compounds from M4K.

I’ve been lucky enough to have a student (Mira) in the lab working with me for the past few weeks and so I’d like to write about the work that we’ve been doing together. We spent some time cleaning up an old sample of ALK2 that Ros had left over in the freezer to set Read More …

PhD position available in malaria parasite genomics and transcriptomics

Summary: –       3-year PhD funded by CNRS for genomics and transcriptomics data analysis of the Plasmodium falciparum malaria parasite. –       In a young dynamic team based in Montpellier, South of France, with many worldwide collaborators –       Keywords: population genetics & genomics, single-cell RNA-seq, molecular epidemiology, antigenic variation.   Our research Most malaria deaths are caused Read More …

Results from soaking follow-up compounds into preformed HAO1 crystals

In my last post, I told you I had soaked my follow-up compounds into HAO1 crystals to start developing structural explanations of how these compounds work. So far I have analysed four interesting protein-compound structures: 2 at the active site, 1 at the gating loop and 1 at the oligomeric interface. Full experimental details can Read More …

The Benefits of Conference attendance: BMP Signalling in Cancer II.

I’ve got a few things to catch up with on the blog – one of them is to talk about a conference I attended in Oxford recently. I attended the Biochemical Society BMP Signalling in Cancer II meeting which was held in St. Annes College, Oxford. At this meeting I presented a poster on the Read More …