GTPases have long been considered key examples of undruggable proteins. While this has been overcome for K-Ras using #CovalentInhibitors, for many other family member #DrugDevelopment has not been shown.

Congratulations to Johannes Morstein on winning one of the @GDCh_BioChem Young Scientist Awards for his work addressing this challenge by identifying druggable, allosteric pockets in several GTPases.

https://www.cell.com/cell/fulltext/S0092-8674(24)00908-5
#Biochemistry #ChemBio #GTP #GTPases #Chemistry
CC: @gdch

The structure of the GDP-bound state of the signal recognition particle-type GTPase FlhF allows comparison with GTP-loaded FlhF and elucidation of the conformational changes associated with GTP hydrolysis @IUCr #FlagellarAssembly #SRPGTPases #GTPases https://doi.org/10.1107/S2053230X24000979
Structure of the GDP-bound state of the SRP GTPase FlhF

This study presents the X-ray structure of FlhF in its GDP-bound state at a resolution of 2.28 Å, exhibiting the classical N- and G-domain fold. Comparative analysis with GTP-loaded FlhF elucidates the conformational changes associated with GTP hydrolysis.

Acta Crystallographica Section F

#alt4u
Excerpted from figure legend:

Phylogenetic tree of the McrB #GTPases
The major clades in the #phylogenetic tree of the McrB GTPases are distinguished by the distinct versions of the Nx(xx)D signature motif. Each of the differently colored groups is characterized by distinct conserved genomic associations that are abundant within but not completely confined to the respective groups. This tree was built from the representatives of 90% identity clusters of all validated homologs.

@alexcc

Math determines the dynamically coordinated regulation of edge velocity by Rho GTPases

Rho GTPases have a crucial role in the orchestration of cell movements. Cells use Rho GTPases to coordinate cytoskeletal reorganization in dynamically changing environments. Among these RhoGTPases, Cdc42 and Rac1 promote cytoskeletal formation, whereas RhoA is involved in myosin II-mediated cytoskeletal retraction and formation.

Phys.org
A bit of #cellbiology history. I was going through a box of inherited column hardware and found this, which would have been used in the Glomset lab as they were discovering and characterizing prenylation of #Rab #GTPases in the early 1990s.
Twitter (and #mastodon) #cellbio #membrane community! Membrane seminars are back this Thu 5 pm (Berlin/Barcelona time). This week a bit of #neuron and #endocytosis with @DomenicoAzTe from @VolkerHaucke's lab and #Rab #GTPases #mitosis with Stéphanie Miserey @institut_curie!