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Identification of interaction regions for protein-protein and antibody-antigen interactions
Identification of interaction regions for protein-protein and antibody-antigen interactions A profound understanding of protein structure and its interactions is crucial for revealing their biological functions. However, due to the complexity and diversity in the field of proteins, a single research technique often struggles to fully elucidate their mysteries. Therefore, biologists typically adopt a strategy of integrating multiple technical approaches to collectively explore the three-dimens... -
Identification of Protein-Protein Interaction Networks in Cells
Identification of Protein-Protein Interaction Networks in Cells Protein-protein interactions (PPIs) constitute an indispensable core component of cellular life activities, spanning multiple temporal and spatial dimensions and profoundly influencing crucial cellular processes such as cell cycle regulation, protein synthesis and secretion, signal transduction, and metabolism. Therefore, a deep investigation into protein interactions plays a pivotal role in uncovering the mysteries of molecular ... -
Protein-Protein Interactions
Protein-Protein Interactions Protein-protein interactions (PPIs) serve as the cornerstone of cellular life activities, playing crucial roles in cell signaling, structural assembly, and key life processes such as pathogen-host recognition. However, many pathological processes are also caused by abnormalities in PPIs. Therefore, intervening and regulating PPIs has shown tremendous potential as a means to treat related diseases. ChomiX integrates a series of cutting-edge technology platform... -
Identification and Selectivity Analysis of Protein Degrader Targets
Identification and Selectivity Analysis of Protein Degrader Targets In recent years, targeted protein degradation (TPD) has emerged as an innovative therapeutic strategy aiming to modulate disease by intervening in protein expression using drug molecules. Among these approaches, proteolysis targeting chimeras (PROTACs) have garnered significant attention. The concept of PROTAC was first proposed by Crews et al. in 2001, with the core idea being to leverage the endogenous ubiquitin-proteasome ... -
Quantitative Analysis of Occupancy and Selectivity of Covalent Small Molecule Drug Targets
Quantitative Analysis of Occupancy and Selectivity of Covalent Small Molecule Drug Targets Covalent drugs primarily exert their effects by forming covalent bonds with specific amino acid residues on target proteins, including cysteine, lysine, serine, among others. Aspirin was the first covalent drug molecule discovered, and several representative covalent drugs with anti-inflammatory bioactivity exist in natural products, such as artemisinin. In recent years, covalent targeted drugs have gai... -
Identification of Binding Pockets for Non-covalent Small Molecule Drugs
Identification of Binding Pockets for Non-covalent Small Molecule Drugs In the process of small molecule drug development, understanding the binding mode between drugs and target proteins is crucial for elucidating drug mechanisms and guiding subsequent structural optimization. Structural biology techniques such as X-ray crystallography, cryo-electron microscopy (cryo-EM), and nuclear magnetic resonance (NMR) have become key tools for determining drug binding models. Particularly, high-resolu... -
Identification of Direct Targets for Non-covalent Small Molecule Drugs
Identification of Direct Targets for Non-covalent Small Molecule Drugs In the field of drug development for diseases, small molecule drugs undoubtedly play a crucial role. According to recent statistics, among the 854 human protein targets targeted by FDA-approved drugs, a staggering 84% correspond to small molecule drugs. Notably, only 665 of these targets have been successfully developed with small molecule drugs (source: https://www.proteinatlas.org/humanproteome/tissue/druggable). Small m... -
Small Molecule-Protein Interactions
Small Molecule-Protein Interactions Proteins, as the direct participants and executors of life activities, represent crucial targets for disease therapy. Small molecule drugs (organic compounds typically with a molecular weight less than 1000 Da) exert effective therapeutic effects by finely modulating protein activities, abundances, and interactions. Common small molecule drugs include natural products and their derivatives (e.g., herbal monomers) as well as chemically synthesized drugs. Upo... -
Target Discovery Platform: Unraveling the Mechanisms of Natural Products
The active ingredient within Chinese medicine is a series of compounds that have therapeutic or physiological activities. Chinese medicines are rich in variety, complex in composition, and have a wide range of active ingredients, constituting an important avenue for acquiring active ingredients, lead compounds, and making medicines.
Our chemoproteomics platform excels in discovering protein targets for natural products in Chinese medicine. It ingeniously transforms these natural products into multifunctional chemical probes, mirroring their bioactivities. These probes, when applied within live cells or diseased tissues, can directly capture natural product-binding proteins. With the aid of bioorthogonal coupling reactions, we precisely isolate and enrich these target proteins. Utilizing high resolution mass spectrometry, we achieve pinpoint accuracy down to the binding pockets. It equips us with more comprehensive and accurate information, poised to unveil the intricate mechanism underlying the active ingredients in Chinese medicine.
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Identification of Non-covalent Small Molecule Binding Pockets in Cells
Identification of Non-covalent Small Molecule Binding Pockets in Cells Platform Technical Features It is critical to determine the binding mode between small molecule drugs and their protein targets for drug R&D. A comprehensive analysis of these interactions at both structural and physico-chemical levels could significantly deepen our understanding of protein functions and facilitate drug design & optimization. Structural biology techniques, including X-ray, cryo-electron microscopy ... -
Proteome-wide profiling for Targeted Protein Degradation (TPD) drugs
The Proteolysis Targeting Chimeras (PROTAC) drug is a bifunctional molecule that can bind to the targeted protein and recruit the ubiquitin E3 ligase for degradation. Therefore, novel modalities such as PROTAC and molecular glue have the ability to inadvertently alter the abundance of endogenous proteins, which provides a new therapeutic method for protein targets, especially the undruggable proteins. Comprehensively quantifying the abundance of on and off-target proteins has been one of the standard experiments for TPD drugs R&D.
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Protein targets identification by differential proteomics
Protein Targets Identification by Differential Proteomics Platform Technical Features Differential proteomics studies the changes of proteome under different physiological or pathological states, such as drug treatments or gene regulation, by comparing two or more samples. This approach sheds light on important life processes or major diseases in order to figure out the key different proteins that are regarded as markers for qualitative and functional analysis. Thousands of proteins can be id...
