A5070504126- Cell Image Analysis Techniques
- Cancer-related gene regulation
- Protein Degradation and Inhibitors
- Cancer Mechanisms and Therapy
- Connexins and lens biology
- Peptidase Inhibition and Analysis
- Histone Deacetylase Inhibitors Research
- Ion channel regulation and function
- Nicotinic Acetylcholine Receptors Study
- Epigenetics and DNA Methylation
- bioluminescence and chemiluminescence research
- AI in cancer detection
- Genetics, Bioinformatics, and Biomedical Research
- Ubiquitin and proteasome pathways
- Chemical Synthesis and Analysis
- Chromosomal and Genetic Variations
- Cardiomyopathy and Myosin Studies
- Gene Regulatory Network Analysis
- Heat shock proteins research
- Scientific Computing and Data Management
- Insect and Pesticide Research
- Biomedical and Engineering Education
- Computational Drug Discovery Methods
- Force Microscopy Techniques and Applications
- Advanced Fluorescence Microscopy Techniques
Centre for Genomic Regulation
2023-2024
University of Oxford
2018-2019
Genomics (United Kingdom)
2018-2019
Harvard University Press
2012
École Polytechnique Fédérale de Lausanne
2009-2012
YEATS domain (YD) containing proteins are an emerging class of epigenetic targets in drug discovery. Dysregulation these modified lysine-binding has been linked to the onset and progression cancers. We herein report discovery characterisation first small-molecule chemical probe, SGC-iMLLT, for YD MLLT1 (ENL/YEATS1) MLLT3 (AF9/YEATS3). SGC-iMLLT is a potent selective inhibitor MLLT1/3-histone interactions. Excellent selectivity over other human (YEATS2/4) bromodomains was observed....
Modifications of histone tails, including lysine/arginine methylation, provide the basis a "chromatin or code". Proteins that contain "reader" domains can bind to these modifications and form specific effector complexes, which ultimately mediate chromatin function. The spindlin1 (SPIN1) protein contains three Tudor methyllysine/arginine reader was identified as putative oncogene transcriptional coactivator. Here we report SPIN1 chemical probe inhibitor with low nanomolar in vitro activity,...
Modern life science research is a collaborative effort. Few groups can single-handedly support the necessary equipment, expertise and personnel needed for ever-expanding portfolio of technologies that are required across multiple disciplines in today's endeavours. Thus, institutes increasingly setting up scientific core facilities to provide access specialised cutting-edge technologies. Maintaining momentum carry out leading while ensuring high-quality daily operations an ongoing challenge,...
Images document scientific discoveries and are prevalent in modern biomedical research. Microscopy imaging particular is currently undergoing rapid technological advancements. However for scientists wishing to publish the obtained images image analyses results, there date no unified guidelines. Consequently, microscopy data publications may be unclear or difficult interpret. Here we present community-developed checklists preparing light analysis publications. These offer authors, readers,...
Intercellular Ca2 + wave propagation between vascular smooth muscle cells (SMCs) is associated with the of contraction along vessel. Here, we characterize involvement gap junctions (GJs) in SMCs at cellular level. Gap junctional communication was assessed by intercellular waves and transfer Lucifer Yellow A7r5 cells, primary rat mesenteric (pSMCs), 6B5N a clone expressing higher connexin43 (Cx43) to Cx40 ratio. Mechanical stimulation induced an intracellular pSMC that propagated neighboring...
<p>YEATS domain (YD) containing proteins are an emerging</p> <p>class of epigenetic targets in drug discovery. Dysregulation these modified lysine binding has been linked to the onset and progression cancers. We herein report discovery characterisation first small molecule chemical probe, SGC-iMLLT, for YD MLLT1 (ENL/YEATS1) MLLT3 (AF9/YEATS3). SGC-iMLLT is a potent selective inhibitor MLLT1/3 -histone interactions. Excellent selectivity over other human (YEATS2/4)...
Abstract Translocations have largely been implicated in tumor development. However, beyond the consequences of aberrant gene expression near breakpoint, their effects remain unexplored. In this work, we characterize interplay between translocations, chromatin organization and using mantle cell lymphoma (MCL) as a model. We show that vitro induced MCL-associated translocations can drive transcriptional changes at entire chromosome arms affecting multiple genes regulon-like fashion....
Abstract YEATS‐Domänen(YD)‐enthaltende Proteine sind eine neue Klasse epigenetischer Zielstrukturen für die Wirkstoffentwicklung. Die YD‐enthaltenden MLLT1 (ENL/YEATS1) und MLLT3 (AF9/MLLT3) oft in Krebs dereguliert wurden daher als potentielle Therapieansätze diskutiert. Wir berichten hier Entwicklung Charakterisierung des ersten niedermolekularen Inhibitors der YD MLLT3, SGC‐iMLLT . Er ist ein potenter selektiver Inhibitor MLLT1/3‐Histon‐Interaktion zeichnet sich durch exzellente...
YEATS domain (YD) containing proteins are an emerging class of epigenetic targets in drug discovery. Dysregulation these modified lysine binding has been linked to the onset and progression cancers. We herein report discovery characterisation first small molecule chemical probe, SGC-iMLLT, for YD MLLT1 (ENL/YEATS1) MLLT3 (AF9/YEATS3). SGC-iMLLT is a potent selective inhibitor MLLT1/3 -histone interactions. Excellent selectivity over other human (YEATS2/4) bromodomains was observed....
Modifications of histone tails, including lysine/arginine methylation, provide the basis a 'chromatin or code'. Proteins that contain 'reader' domains can bind to these modifications and form specific effector complexes, which ultimately mediate chromatin function. The spindlin1 (SPIN1) protein contains three Tudor methyllysine/arginine reader was identified as putative oncogene transcriptional co-activator. Here we report SPIN1 chemical probe inhibitor with low nanomolar in vitro activity,...
Tissue blood flow is controlled by changes in the diameter of arteries and arterioles through coordinated contraction relaxation smooth muscle cells (SMCs) within vascular wall. The SMCs primarily regulated intracellular Ca2+ concentration ([Ca2+]i). An increase [Ca2+]i, response to stimuli, can propagate from cell cell, as an intercellular wave along vessel wall activate process contraction. aim this thesis elucidate mechanisms underlying propagation between SMCs. In first part thesis, we...
Modifications of histone tails, including lysine/arginine methylation, provide the basis a 'chromatin or code'. Proteins that contain 'reader' domains can bind to these modifications and form specific effector complexes, which ultimately mediate chromatin function. The spindlin1 (SPIN1) protein contains three Tudor methyllysine/arginine reader was identified as putative oncogene transcriptional co-activator. Here we report SPIN1 chemical probe inhibitor with low nanomolar in vitro activity,...
Lysine and arginine methylation are amongst the most frequent modifications on unstructured histone tails incombination with other provide basis for a combinatorial 'chromatin or code'. Recognition of modifiedhistone residues is accomplished in specific manner by 'reader' domains that recognize chromatin modifications, allowing forassociation effector complexes mediate functions. The methyl-lysine methyl-arginine reader domainprotein SPINDLIN1 (SPIN1) belongs to family 5 human genes, has...