Guangdong Pharmaceutical University

ElectrochemiluminescenceMicroscopy

Abstract Electrochemiluminescence (ECL) microscopy is an emerging imaging technology that combines electrochemistry with optical microscopy. It operates without external light excitation, effectively eliminating photobleaching, phototoxicity, and scattered light noise, and thus e...

Body Composition–Driven Phenotyping Reveals Obesity and Cardiometabolic Heterogeneity in Children Using a Tree-Like Representation

Traditional measures such as BMI do not fully capture obesity-related metabolic risks. Here, we examined DXA-derived body composition patterns in children (n = 11,238) using the discriminative dimensionality reduction tree algorithm, which was validated in an independent cohort (...

HomocamptothecinPayloads with Enhanced Potency forAntibody-Drug Conjugates

Abstract Camptothecin derivatives, exemplified by DXd, are a dominant class of payloads for antibody-drug conjugates (ADCs). Herein, we describe the design and synthesis of H2, a novel homocamptothecin featuring a simplified hydroxybutyl structure that circumvents the complex ass...

Modification GeneKnockout Diversifies Piericidinsfrom the Marine-Derived Streptomyces psammoticus SCSIO NS126

Abstract Piericidins are α-pyridone agricultural antibiotics produced by actinomycetes. To improve their yield and structural diversity from marine-derived Streptomyces psammoticus SCSIO NS126, this study employed homologous recombination to achieve large-fragment knockout of mod...

Radical 1,3-Difunctionalizationof β,γ-UnsaturatedKetones via Synergistic LMCT and RLT Photocatalysis

Abstract We report herein a simple and general photoinduced iron-catalyzed method that combines 1,2-functional group migration (1,2-FGM) with ligand-to-metal charge transfer (LMCT) and radical ligand transfer (RLT) to broaden the reaction profiles of alkene 1,3-difunctionalizatio...

Optimizationof a Second-Generation, Highly SelectivePolθ/PARP1 Dual Inhibitor with Improved Pharmacokinetics andPotent Activity against HR-Deficient Tumors

Abstract Dual inhibition of Polθ and PARP1 represents a promising precision therapy strategy for HR-deficient tumors. While our first-generation Polθ/PARP1 dual inhibitor 4 provided proof-of-concept, its further development was hampered by poor selectivity over PARP2 and metaboli...

Photocatalyzed RegioselectivityTrifluoromethylationand Sulfuration of Unactivated Alkenes with S -ArylTrifluoromethanesulfonothioates (TTSA)

Abstract Under photocatalytic conditions, a novel and highly reactive trifluoromethylthiolation reagent, S-aryl trifluoromethanesulfonothioate (TTSA), reacted with various unactivated alkenes to produce sulfurized and trifluoromethylated derivatives in high yields. Furthermore, a...

Composite Hydrogel Loading Polysaccharides Derived from Coptis chinensis Franch. for Promoting Diabetic Wound Healing

Efficient treatment of diabetic wounds (DW) remains a major clinical challenge worldwide owing to vascular insufficiency, multiple bacterial infections, and overactivation of pro-inflammatory M1 macrophages caused by hyperglycemia. The development of novel pharmaceutical agents w...

NIR-Activated Enteric Prodrug Microparticles for Bioimaging-Guided Chemotherapy of Colorectal Cancer

Colorectal cancer (CRC) remains a leading cause of cancer mortality worldwide. 5-Fluorouracil (5-FU) is a first-line chemotherapeutic widely used in CRC treatment, but its systemic administration often causes severe toxicity due to uncontrolled biodistribution. Herein, we present...

Temperature-Dependent Crystallization Pathways ofthe Curcumin-Magnolol Coamorphous System: A Mechanistic Study IntegratingThermodynamics and Kinetics

Abstract Coamorphous drug systems have received increasing interest owing to their potential to improve the solubility, dissolution, and bioavailability of insoluble drugs. However, coamorphous systems exist in a high-energy state, making them prone to crystallization into stable...

Senkyunolide I Inhibits mtDNA‐cGAS‐STING Signaling in Macrophages via Targeting VDAC1 Oligomerization to Attenuate Ulcerative Colitis

Ulcerative colitis (UC) is a chronic inflammatory bowel disease with limited therapeutic options. The cyclic GMP-AMP synthase (cGAS)-stimulator of interferon genes (STING) pathway, activated by cytosolic mitochondrial DNA (mtDNA), has been increasingly implicated in UC. Through p...

Ultrafiltered Mulberry (Morus alba L.) Leaf Albumin-Type Protein Attenuates High-Fat Diet-Induced Obesity in Mice by Remodeling Gut Microbiota and Metabolic Homeostasis

Obesity is a chronic metabolic disorder closely associated with dyslipidemia, insulin resistance, low-grade inflammation, and gut microbiota dysbiosis. Mulberry leaves are rich in bioactive proteins, but whether mulberry leaf albumin-type protein can improve diet-induced obesity...

A Multi-Modal Pre-training Framework-Driven Active Learning System for Enhanced Protein Evolution of Cs CE

Abstract Protein language models have shown strong potential in modeling fitness landscapes for directed evolution; however, their predictive accuracy and generalization to unexplored sequence space remain limited under few-shot learning conditions. Here, we present MmALS (Multi-...

Thyroid function and hypertensive disorders of pregnancy: Insights from a sex‐specific cohort study, Mendelian randomization, and experimental validation

OBJECTIVE: To investigate the association of a history of hypertensive disorders of pregnancy (HDP) and a higher risk of cardiovascular disease using a sex-specific cohort study, bidirectional two-sample Mendelian randomization (MR), and in vitro experiments. METHODS: Multivariab...