Gregory Craven

[Gregory Craven @GregoryCraven13]

This has been my main postdoctoral project and has only been possible because of all the support I had from Jack, Ying and Hao in the Taunton lab, as well as everyone at Terremoto Biosciences! It's been a lot of fun and I hope this will inspire new E17K-targeted therapeutics.

[Gregory Craven @GregoryCraven13]

Our work addressing E17K-mutant AKT1 using lysine-targeted inhibitors was published today https://t.co/74RZx4tkOW. AKT1(E17K) is a recurrent mutation in a range of solid tumors but is clinically challenging to target because panAKT inhibitors have severe side-effects.

[Gregory Craven @GregoryCraven13]

There's a twist: the salicylimine adduct with E17K recruits Zn2+ to form a tetrahedral chelate, completed by two cysteine residues. I discovered this inhibition mode serendipitously using X-ray crystallography and found that it actually forms in cells to enhance residence-time.

[Gregory Craven @GregoryCraven13]

Check out the latest publication from the Taunton lab on Reversible lysine-targeted probes. Huge congrats to Tangpo and everyone else involved. Salicylaldehydes showing real promise for in vivo lysine targeting. https://t.co/HBwuGiuvpF

[Keely Oltion @keely_oltion]

Incredibly excited to share my graduate work, and the latest from the Taunton lab @UCSF! We think this will open a new dimension of surveillance pathways for elongating ribosomes.

https://t.co/C58yX9pYtk

[Bull Group Chemistry @jamesabull]

Our latest work on transient directing groups for C-H functionalization, now using copper, is out as a preprint on @ChemRxiv. Congrats to Joe @jhigham96! https://t.co/M1ah09mbTg

[Gregory Craven @GregoryCraven13]

Bored of acrylamides? check out our new routes to chiral S(VI) alkenes: https://t.co/BZgfLO21gF. Cool molecules and probes in the making. Watch this space for our follow-up chemical biology study. Thanks to everyone involved @alanarmstrong13 @jamesabull @REACHSEPARATION

[Gregory Craven @GregoryCraven13]

@jhigham96 @jamesabull This looks great Joe. Well done.

[Adam Nelson @Adam_S_Nelson]

Interested in high-throughput molecular discovery? Postdoctoral position available in Leeds, closing date 6th Dec! Happy to answer any questions about the post! https://t.co/KNLQGVfzgq

[Gregory Craven @GregoryCraven13]

Well done to all authors involved especially @Cuisheng2017 and his group for persevering with the crystallography.

[Gregory Craven @GregoryCraven13]

This project went in a unforeseen direction. From a screen against EV71 3Cpro we identified acrylamide fragments that bind an interesting cryptic site. Repurposing these against SARS-CoV-2 Mpro we found an unexpected result: allosteric dimer disruption. https://t.co/2vQcp20Pac

[Gregory Craven @GregoryCraven13]

Fragment merging is so satisfying to see in action and this is a really nice approach. The jumps in LE are wicked. All done without a structure!

[Practical_Fragments @PracticalFrag]

No structure, no problem. Researchers built a fragment library around a privileged pharmacophore to facilitate merging and found potent, selective inhibitors of protein kinase C ζ: https://t.co/THn7vHUDJR
@JMedChem @QuantumTessera