Agnes C. L. Martin

TL;DR: It is shown that serine can bind to and activate human PKM2, and thatPKM2 activity in cells is reduced in response to serine deprivation, which shifts cells to a fuel-efficient mode in which more pyruvate is diverted to the mitochondria and more glucose-derived carbon is channelled into serine biosynthesis to support cell proliferation.

TL;DR: Two compounds are reported that inhibit ubiquitin-specific protease 7 with high affinity and specificity in vitro and within human cells, and co-crystal structures reveal that both compounds target a dynamic pocket near the catalytic centre of the auto-inhibited apo form of USP7, which differs from other USP deubiquitinases.

TL;DR: Together, the data indicate that Orai1 and STIM1 can be integral components of the cAMP and CCE microdomain associated with adenylyl cyclase type 8, and also indicate that AC8 is believed to be closely associated with the source of CCE.

TL;DR: Initial efforts to identify inhibitors of MMSET (aka NSD2 or WHSC1) using solution phase and crystal structural methods are presented and use of the close homologue SETD2 as a structural surrogate supported the design and characterization of N-alkyl sinefungin derivatives.

TL;DR: This study exploited the unique dependence of AC8 on CCE to determine whether the DAG analog, 1-oleyl-2-acetyl-sn-glycerol (OAG), activates the same subset of Ca2+ channels as store depletion, which triggers CCE.