A5049374801- Protein Degradation and Inhibitors
- Estrogen and related hormone effects
- Hydrology and Watershed Management Studies
- Nanoplatforms for cancer theranostics
- Metal and Thin Film Mechanics
- Advanced materials and composites
- HER2/EGFR in Cancer Research
- Synthesis and biological activity
- Histone Deacetylase Inhibitors Research
- Diamond and Carbon-based Materials Research
- Click Chemistry and Applications
- Cancer therapeutics and mechanisms
- Advancements in Solid Oxide Fuel Cells
- Hydrological Forecasting Using AI
- Environmental and Agricultural Sciences
- Integrated Circuits and Semiconductor Failure Analysis
- Biochemical and Molecular Research
- Fuel Cells and Related Materials
- Photoacoustic and Ultrasonic Imaging
- Flood Risk Assessment and Management
- Fish Ecology and Management Studies
- PARP inhibition in cancer therapy
- Ubiquitin and proteasome pathways
- Peptidase Inhibition and Analysis
- Cryospheric studies and observations
Guizhou University
2023-2025
Wuhan University of Science and Technology
2020-2024
Beijing Normal University
2022-2024
Henan Polytechnic University
2023
Yanshan University
2019-2022
Beihang University
2022
Beijing Academy of Agricultural and Forestry Sciences
2022
Ministry of Industry and Information Technology
2020
Harbin Institute of Technology
2020
Wuhan University
2015-2019
A strategy to develop chemotherapeutic agents by combining several active groups into a single molecule as conjugate that can modulate multiple cellular pathways may produce compounds having higher efficacy compared of single-target drugs. In this article, we describe the synthesis and evaluation an array dual-acting ER histone deacetylase inhibitors. These novel hybrid combine indirect antagonism structure motif (OBHS, oxabicycloheptene sulfonate) with HDAC inhibitor suberoylanilide...
Targeted protein degradation technologies (e.g., PROTACs) that can selectively degrade intracellular are an emerging class of promising therapeutic modalities. Herein, we describe the conjugation photosensitizers and ligands (PS-Degrons), as activable targeted platform. PS-Degrons capable degrading interest via light-triggered 1O2, which is orthogonal complementary to existing technologies. This generalizable platform allows controllable knockdown target with high spatiotemporal precision....
Chemodynamic therapy (CDT) is a cancer treatment that converts endogenous H2O2 into hydroxyl radicals (˙OH) through Fenton reaction to destroy cells. However, there are still some challenges in accelerating the of CDT and improving biodegradability nanocatalysts. Herein, multifunctional biomimetic BPQDs-Cu@GOD (BCG) nanocatalyst for boosting synergistically enhanced H2O2-guided photothermal reported. Cu2+ BCG can be reduced Cu+ by black phosphorus quantum dots (BPQDs), triggering...
Inhibition of methionine adenosyltransferase 2A (MAT2A) in cancers with a deletion methylthioadenosine phosphorylase (MTAP) gene leads to synthetic lethality, thus receiving significant interest the field precise cancer treatment. Herein, we report discovery tetrahydrobenzo[4,5]imidazo[1,2-a]pyrazine fragment which occupies MAT2A allosteric pocket. The lead compound 8 exhibited extremely high potency inhibit enzymatic activity (IC50 = 18 nM) and proliferation MTAP-null cells 52 nM). had...
The relentless pursuit of innovative hydrophobic tags remains a formidable challenge within the realm targeted protein degradation. Herein, we have uncovered remarkable potential D-ring-contracted artemisinin as potent tag that demonstrates exceptional degradation efficiency. We crafted series conjugates by fusing with raloxifene, and among these,
The interaction between son of sevenless 1 (SOS1) gene and Kirsten rat sarcoma viral oncogene (KRAS) is crucial for activating signals proliferation survival in a range cancers. We previously discovered compound 40a with tetracyclic quinazoline pharmacophore as potent orally bioavailable SOS1 inhibitor. Herein, we disclosed the discovery 13c, which substituted third ring seven-membered ring, clinical drug candidate suppressing KRAS-driven tumors. 13c strongly disrupted protein-protein KRAS...
In this work, we developed a small library of novel OBHS-RES hybrid compounds with dual inhibition activities targeting both the estrogen receptor α (ERα) and NF-κB by incorporating resveratrol (RES), known inhibitor NF-κB, into privileged indirect antagonism structural motif (OBHS, oxabicycloheptene sulfonate) (ER). The conjugates could bind well to ER showed remarkable ERα antagonistic activity, they also exhibited excellent NO in macrophage RAW 264.7 cells. Compared 4-hydroxytamoxifen,...
Abstract Vanillic acid, potentially derived from biosourced feedstocks, was used as starting material in the synthesis of novel polyesters. A diester obtained by esterification and etherification vanillic acid served first monomer, combination with resorcinol bis(2‐hydroxyethyl) ether, hydroquinone or aliphatic diols different carbon chain lengths second monomers, antimony trioxide catalyst to synthesize a series polyesters melt polymerization. The materials had polystyrene‐equivalent M n =...
The climate change impact on hydrology in China's Huang-Huai-Hai (H-H-H) region was assessed this study. Both variations mean monthly and annual runoff occurrences of extreme events including flood drought were examined for two future periods (2001–2030 2016–2045) the whole region. projected daily maximum minimum temperature precipitation from PRECIS (providing regional climates impacts studies) model used to drive variable infiltration capacity (VIC) model. Variable run over a domain 408...
Small molecules capable of modulating methionine adenosyltransferase 2A (MAT2A) are significant interest in precise cancer therapeutics. Herein, we raised the hole–electron Coulombic attraction as a reliable molecular descriptor for predicting reactive oxygen generation capacity MAT2A inhibitors, based on which discovered compound H3 sonically activated degrader MAT2A. Upon sonication, can generate species to specifically degrade cellular via rapid oxidative reactions. Combination and...
The complementary operation of hydropower and photovoltaic power, aimed at meeting real-time demand, has led to frequent adjustments in power generation, causing significant fluctuations hydrological systems adversely affecting fish reproduction. traditional regime alteration assessment index is based on hydrologic alternation (IHA) mostly focuses annual daily runoff alterations. This study proposes a new set indicators considering the characteristics subdaily alterations, including...
The importance of the heterocyclic core elements with peripheral phenolic and alkyl substituents as a dominant structural motif ligands for estrogen receptor (ER) has been well recognized. In this study we expanded diversity by preparing selenium-containing heterocycles exploring activities these selenophenes on two ERs, ERα ERβ. Careful structure-activity relationship (SAR) analysis their ER binding affinities showed that most are ERβ-selective, position phenol selenophene nature having...