Emma K. Grant

Fragment‐Based Screening of Heterocyclic Electrophiles Identified Acrylamide Bioisoteres for Covalent KRas G12C Inhibitors

Nikolett Péczka, Aaron Keeley, Péter Ábrányi‐Balogh, Zoltán Orgován et autres

ABSTRACT Covalent fragment approaches gained increasing attention in medicinal chemistry. Our covalent heterocyclic fragment library (Covalent MiniFrags) consisting of five and six membered heterocycles was screened against the oncogenic target KRas G12C . First, we detected the labeling of cysteine residues by …

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Table S2 from Novel WRN Helicase Inhibitors Selectively Target Microsatellite-Unstable Cancer Cells

Gabriele Picco, Yanhua Rao, Angham Al Saedi, Yang Lee et autres

This table lists the results from Base editing screen

Table S3 from Novel WRN Helicase Inhibitors Selectively Target Microsatellite-Unstable Cancer Cells

Gabriele Picco, Yanhua Rao, Angham Al Saedi, Yang Lee et autres

This file contain information on the Cell lines and organoids used in this study

Table S1 from Novel WRN Helicase Inhibitors Selectively Target Microsatellite-Unstable Cancer Cells

Gabriele Picco, Yanhua Rao, Angham Al Saedi, Yang Lee et autres

This file contains details of the BE sgRNA library

Druggability is not static

Harry Wilders, Emma K. Grant, Jacob T. Bush

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A chemical probe for prostate-specific membrane antigen for real-time Raman imaging of prostate cancer cells

William J. Tipping, Daniel J. Powell, Robert C. Wells, Emma K. Grant et autres

Intraoperative detection of localized prostate cancer is challenging with direct consequences for long-term, successful treatment of the disease. Optical imaging techniques have been incorporated into the surgical environment, often using theranostic agents to rapidly and accurately determine the tumor margin. Here, we …

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A Chemical Probe for Prostate-Specific Membrane Antigen for Real-Time Raman Imaging of Prostate Cancer Cells

William J. Tipping, Daniel J. Powell, Robert C. Wells, Emma K. Grant et autres

Intraoperative detection of localized prostate cancer is challenging with direct consequences for long-term, successful treatment of the disease. Optical imaging techniques have been incorporated into the surgical environment, often using theranostic agents to rapidly and accurately determine the tumor margin. Here, we …

gb (code pays fourni par la source)

Next Generation Sulfonyl Fluoride Electrophiles Expand the Scope of Covalent Drug Discovery

Alfred E. Doherty, Chloe Oxford, Ferdausi Mazumder, Katharine Gilbert et autres

Sulfonyl fluorides (SFs) are promising electrophiles for covalent drug discovery, enabling the targeting of diverse amino acids beyond cysteine. However, their widespread application has been hindered by limitations in stability and selectivity, often restricting their utility to early-stage tool development. We introduce …

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Author response for "Emerging applications of stimulated Raman scattering microscopy for medicinal chemistry and drug discovery"

Henry J. Braddick, William J. Tipping, Emma K. Grant, Nicholas C. O. Tomkinson et autres

Author response for "Emerging applications of stimulated Raman scattering microscopy for medicinal chemistry and drug discovery"

Henry J. Braddick, William J. Tipping, Emma K. Grant, Nicholas C. O. Tomkinson et autres

Deletion of Endocannabinoid Synthesizing Enzyme DAGLα in Pcp2-Positive Cerebellar Purkinje Cells Decreases Depolarization-Induced Short–Term Synaptic Plasticity, Reduces Social Preference, and Heightens Anxiety

Gabriella Smith, Kathleen McCoy, Gonzalo Viana Di Prisco, Alexander Kuklish et autres

The endocannabinoid (eCB) signaling system is robustly expressed in the cerebellum from embryonic developmental stages to adulthood. It plays a key role in regulating cerebellar synaptic plasticity and excitability, suggesting that impaired eCB signaling could lead to deficits in cerebellar adjustments of …

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‘Direct-to-biology’ drives optimisation of a cell-active covalent inhibitor of WRN helicase

Sam M. Rowe, Alan T. Price, Dennis J. Murphy, Jiarong Lin et autres

We report a ‘direct-to-biology’ (D2B) approach for optimising covalent acrylamide binders of protein targets and apply this to the identification of a selective and cell-active inhibitor of Werner (WRN) helicase. Inhibition of WRN helicase activity exhibits a synthetic lethal relationship with cancers …

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