A growing team of groundbreaking scientists around the world are now sharing their lab notebooks online
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 …
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 …
Updates on the huntingtin PAR binding story can be found on the Truant lab website.
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 …
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 …
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 …
Proteolysis Targeting Chimeras (PROTACs) are small molecules that induce the degradation of their target and have shown considerable promise as a novel therapeutic modality.1-3 PROTACs are heterobifunctional compounds containing one chemical moiety that binds to the target protein of interest and a chemical handle that binds to an E3 ubiquitin ligase (Figure 1). Recruitment of Read More …
It has now been almost 2 years since I set out to try and make fragments of the huntingtin protein which might be amenable to structural analysis with X-ray crystallography. X-ray crystallography is a fantastic method and allows us to see the molecules in very fine atomic detail which is important if we are to Read More …
Special thanks to: David Drewry – Helped with designing the nanoBRET tracers M4K pharma OICR chemist team – Synthesised the M4K1046-linker derivatives Carrow Wells (UNC) – Conjugated the M4K1046 to nanoBRET fluorophore Background: I have always wanted to establish nanoBRET target engagement assay for ALK5. Relative to dual luciferase promoter assay and immunofluorescent staining, nanoBRET Read More …
One goal of the CaMKK2 project is to explore the chemistry and biology of novel hinge binders. Various hinge binders showing CaMKK2 inhibition have been identified in the literature and through testing of compounds synthesized in the SGC. Of note in this search was a recent publication by Price et al. (Bioorg. Med. Chem. Lett., Read More …
