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Showing results 1 to 6 of 6

Journal article

A two-point IC50 method for evaluating the biochemical potency of irreversible enzyme inhibitors

Authors : Kuzmič, Petr (2023)

Irreversible (covalent) enzyme inhibitors cannot be unambiguously ranked for biochemical potency by using IC50 values determined at a single point in time, because the same IC50 value could originate either from relatively low initial binding affinity accompanied by high chemical reactivity, or the other way around. To disambiguate the potency ranking of covalent inhibitors, here we describe a data-analytic procedure relying on two separate IC50...

Ebooks (Sách điện tử)

Allosteric activation or inhibition of PI3Kγ mediated through conformational changes in the p110γ helical domain

Authors : Harris, Noah J (2023)

PI3Kγ is a critical immune signaling enzym 31 e activated downstream of diverse cell 32 surface molecules, including Ras, PKCβ activated by the IgE receptor, and Gβγ 33 subunits released from activated GPCRs. PI3Kγ can form two distinct complexes, with 34 the p110γ catalytic subunit binding to either a p101 or p84 regulatory subunit, with these 35 complexes being differentially activated by upstream stimuli. Here using a combinati...

Journal article

G protein βγ subunits bind to and inhibit the function of multiple Qa- and Qb,c-SNARE isoforms

Authors : Zurawski, Zack (2023)

While the ability of G protein βγ subunits (Gβγ) to bind to and functionally inhibit the neuronal SNARE proteins Stx1A, SNAP25, and synaptobrevin in the presence of the calcium sensor synaptotagmin I is well documented, these three SNARE proteins, which form the core SNARE complex for synchronous evoked release in neurons, are but a subset of the larger family of SNARE proteins, which participate in many other exocytic proces...

Journal article

PH Domain-Mediated Autoinhibition and Oncogenic Activation of Akt

Authors : Bae, Hwan (2023)

Previously, we reported that the conformation of autoinhibited Akt, a Ser/Thr protein kinase that plays a central role in metabolism and cancer, may be shifted by small molecule allosteric inhibitors limiting the mechanistic insights from existing X-ray structures that have relied on such compounds (Chu, Viennet, et al, 2020). Here we discover unexpectedly that a single mutation, R86A, in Akt’s PH domain exhibits intensified autoinhibitory&...

Journal article

Pyroptosis inhibiting nanobodies block Gasdermin D pore formation

Authors : Kopp, Anja (2023)

Gasdermin D (GSDMD) is a key mediator of pyroptosis, a pro-inflammatory form of cell death 10 occurring downstream of inflammasome activation as part of the innate immune defence. Upon cleavage by inflammatory caspases, the N-terminal domain of GSDMD forms pores in the plasma membrane resulting in cytokine release and eventually cell death. Targeting GSDMD is an attractive way to dampen inflammation. In this study, six GSDMD targeting nanobodies wer...

Journal article

Towards Novel Herbicide Modes of Action by Inhibiting Lysine Biosynthesis in Plants

Authors : Soares da Costa, Tatiana P. (2021)

Weeds are becoming increasingly resistant to our current herbicides, posing a significant threat to agricultural production. Therefore, new herbicides are urgently needed. In this study, we exploited a novel herbicide target, dihydrodipicolinate synthase (DHDPS), which catalyses the first and rate-limiting step in lysine biosynthesis. Using a high throughput chemical screen, we identified the first class of plant DHDPS inhibitors that have micromolar potency against Ar...