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N4BP1 functions as a dimerization-dependent linear ubiquitin reader which regulates TNF signalling
Signalling through TNFR1 modulates proinflammatory gene transcription and programmed cell death, and its impairment causes autoimmune diseases and...
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Inhibiting ERK dimerization ameliorates BRAF-driven anaplastic thyroid cancer
BackgroundRAS-to-ERK signaling is crucial for the onset and progression of advanced thyroid carcinoma, and blocking ERK dimerization provides a...
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The N-terminal dimerization domains of human and Drosophila CTCF have similar functionality
BackgroundCTCF is highly likely to be the ancestor of proteins that contain large clusters of C2H2 zinc finger domains, and its conservation is...
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Structural insights into dimerization and activation of the mGlu2–mGlu3 and mGlu2–mGlu4 heterodimers
Heterodimerization of the metabotropic glutamate receptors (mGlus) has shown importance in the functional modulation of the receptors and offers...
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Resistance mechanisms of SARS-CoV-2 3CLpro to the non-covalent inhibitor WU-04
Drug resistance poses a significant challenge in the development of effective therapies against SARS-CoV-2. Here, we identified two double mutations,...
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Mechanistic insights into HuR inhibitor MS-444 arresting embryonic development revealed by low-input RNA-seq and STORM
With improvements in the survival rate of patients with cancer, fertility maintenance has become a major concern in terms of cancer treatment for...
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Acetylation-dependent SAGA complex dimerization promotes nucleosome acetylation and gene transcription
Cells reprogram their transcriptomes to adapt to external conditions. The SAGA (Spt-Ada-Gcn5 acetyltransferase) complex is a highly conserved...
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Crystal structure of rice APIP6 reveals a new dimerization mode of RING-type E3 ligases that facilities the construction of its working model
Ubiquitination is an important modification process in eukaryotic organisms, and ubiquitin ligase (E3) is the most diversified component of this...
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Phosphorylation-dependent BRD4 dimerization and implications for therapeutic inhibition of BET family proteins
Bromodomain-containing protein 4 (BRD4) is an epigenetic reader and oncology drug target that regulates gene transcription through binding to...
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Phosphatidylinositol 4,5-bisphosphate (PIP2) facilitates norepinephrine transporter dimerization and modulates substrate efflux
The plasmalemmal norepinephrine transporter (NET) regulates cardiovascular sympathetic activity by clearing extracellular norepinephrine in the...
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Regulation of cadherin dimerization by chemical fragments as a trigger to inhibit cell adhesion
Many cadherin family proteins are associated with diseases such as cancer. Since cell adhesion requires homodimerization of cadherin molecules, a...
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A fluorogenic chemically induced dimerization technology for controlling, imaging and sensing protein proximity
Molecular tools enabling the control and observation of the proximity of proteins are essential for studying the functional role of physical distance...
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The MLKL kinase-like domain dimerization is an indispensable step of mammalian MLKL activation in necroptosis signaling
MLKL phosphorylation by RIP3 is the commitment step of necroptosis execution, which could induce MLKL activation featured as MLKL monomer-oligomer...
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Rational optimization of a transcription factor activation domain inhibitor
Transcription factors are among the most attractive therapeutic targets but are considered largely ‘undruggable’ in part due to the intrinsically...
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Targeting Enterococcus faecalis HMG-CoA reductase with a non-statin inhibitor
HMG-CoA reductase (HMGR), a rate-limiting enzyme of the mevalonate pathway in Gram-positive pathogenic bacteria, is an attractive target for...
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Discovery of an OTUD3 inhibitor for the treatment of non-small cell lung cancer
The ubiquitin-proteasome system (UPS) controls protein turnover, and its dysfunction contributes to human diseases including cancer. Deubiquitinating...
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Stability of Oligopeptides in Solution. Proteolytic Digestion and Potential Dimerization Process
The specificity of peptide activity depends on the sequence of amino acids and structure, so it is easy to understand the great degree of...
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PD-L1 induction via the MEK-JNK-AP1 axis by a neddylation inhibitor promotes cancer-associated immunosuppression
MLN4924 is a first-in-class small molecule inhibitor of NEDD8-activating enzyme (NAE), which is currently in several clinical trials for anti-cancer...
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Identification of marine natural product Pretrichodermamide B as a STAT3 inhibitor for efficient anticancer therapy
The Janus kinase (JAK)/signal transducer and activator of transcription 3 (STAT3) regulates the expression of various critical mediators of cancer...
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Making ERRFI1-Derived Peptides ‘Bindable’ to the Allosteric Dimerization Interface of Breast Cancer ERBB3 Kinase by Adding a Nonbonded Interaction System
The ERBB3 is a member of human receptor tyrosine kinase ErbB family involved in various cellular processes, which has been recognized as a new and...
