Targeted protein degradation: expanding the toolbox

M Schapira, MF Calabrese, AN Bullock… - Nature reviews Drug …, 2019 - nature.com
Proteolysis-targeting chimeras (PROTACs) and related molecules that induce targeted
protein degradation by the ubiquitin–proteasome system represent a new therapeutic …

E3 ligase ligands for PROTACs: how they were found and how to discover new ones

T Ishida, A Ciulli - … Advancing the Science of Drug Discovery, 2021 - journals.sagepub.com
Bifunctional degrader molecules, also called proteolysis-targeting chimeras (PROTACs), are
a new modality of chemical tools and potential therapeutics to understand and treat human …

The CRL5–SPSB3 ubiquitin ligase targets nuclear cGAS for degradation

P Xu, Y Liu, C Liu, B Guey, L Li, P Melenec, J Ricci… - Nature, 2024 - nature.com
Abstract Cyclic GMP-AMP synthase (cGAS) senses aberrant DNA during infection, cancer
and inflammatory disease, and initiates potent innate immune responses through the …

Glucocorticoids, genes and brain function

GR Juszczak, AM Stankiewicz - Progress in Neuro-Psychopharmacology …, 2018 - Elsevier
The identification of key genes in transcriptomic data constitutes a huge challenge. Our
review of microarray reports revealed 88 genes whose transcription is consistently regulated …

Applications of isothermal titration calorimetry in pure and applied research—survey of the literature from 2010

R Ghai, RJ Falconer, BM Collins - Journal of Molecular …, 2012 - Wiley Online Library
Isothermal titration calorimetry (ITC) is a biophysical technique for measuring the formation
and dissociation of molecular complexes and has become an invaluable tool in many …

Butyrophilin 3A1 plays an essential role in prenyl pyrophosphate stimulation of human Vγ2Vδ2 T cells

H Wang, O Henry, MD Distefano, YC Wang… - The Journal of …, 2013 - journals.aai.org
Most human γδ T cells express Vγ2Vδ2 TCRs and play important roles in microbial and
tumor immunity. Vγ2Vδ2 T cells are stimulated by self-and foreign prenyl pyrophosphate …

Structure and function of the SPRY/B30. 2 domain proteins involved in innate immunity

AA D'Cruz, JJ Babon, RS Norton, NA Nicola… - Protein …, 2013 - Wiley Online Library
The SPRY domain is a protein interaction module found in 77 murine and∼ 100 human
proteins, and is implicated in important biological pathways, including those that regulate …

[HTML][HTML] Applications of 19F-NMR in Fragment-Based Drug Discovery

RS Norton, EWW Leung, IR Chandrashekaran… - Molecules, 2016 - mdpi.com
19F-NMR has proved to be a valuable tool in fragment-based drug discovery. Its
applications include screening libraries of fluorinated fragments, assessing competition …

Structural and biochemical insights into MLL1 core complex assembly

V Avdic, P Zhang, S Lanouette, A Groulx, V Tremblay… - Structure, 2011 - cell.com
Histone H3 Lys-4 methylation is predominantly catalyzed by a family of methyltransferases
whose enzymatic activity depends on their interaction with a three-subunit complex …

Sensor function for butyrophilin 3A1 in prenyl pyrophosphate stimulation of human Vγ2Vδ2 T cells

H Wang, CT Morita - The Journal of Immunology, 2015 - journals.aai.org
Abstract Vγ2Vδ2 T cells play important roles in human immunity to pathogens and in cancer
immunotherapy by responding to isoprenoid metabolites, such as (E)-4-hydroxy-3-methyl …