Xiaoguang Chen
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View article: Deep Learning-Based Automated Body Composition Analysis Predicts Mortality in Peritoneal Dialysis Patients: A Retrospective Cohort Study
Deep Learning-Based Automated Body Composition Analysis Predicts Mortality in Peritoneal Dialysis Patients: A Retrospective Cohort Study Open
Background Patients undergoing peritoneal dialysis (PD) frequently experience a progressive loss of lean mass and an increase in fat mass. Quantitative body composition analysis is critical for predicting mortality; In this study, we devel…
View article: Thermal proteome profiling (TPP) reveals NAMPT as the anti-glioma target of phenanthroindolizidine alkaloid PF403
Thermal proteome profiling (TPP) reveals NAMPT as the anti-glioma target of phenanthroindolizidine alkaloid PF403 Open
Glioma is difficult to treat due to the unique tumor microenvironment and blood-brain barrier. (13aS)-3-Hydroxyl-6,7-dimethoxyphenanthro[9,10-b] indolizidine (PF403), a phenanthroindolizidine alkaloid, has been identified as …
View article: Impact of biomechanical properties of tongue muscles on accuracy of English vowel pronunciation
Impact of biomechanical properties of tongue muscles on accuracy of English vowel pronunciation Open
Pronunciation is a complex physiological process. Traditional research usually uses static pronunciation tests and fails to observe the dynamic changes of tongue muscles during pronunciation. This paper aims to comprehensively analyze the …
View article: Discovery of Bromobenzyl Phenyl Ether Derivative Ypd-29b: A Novel Pre-Clinical Compound Targeting the Programmed Cell Death-1/Programmed Cell Death-Ligand 1 (Pd-1/Pd-L1) Interaction
Discovery of Bromobenzyl Phenyl Ether Derivative Ypd-29b: A Novel Pre-Clinical Compound Targeting the Programmed Cell Death-1/Programmed Cell Death-Ligand 1 (Pd-1/Pd-L1) Interaction Open
View article: Synthesis and Biological Evaluation of Novel <i>Psidium</i> Meroterpenoid Derivatives against Cisplatin-Induced Acute Kidney Injury
Synthesis and Biological Evaluation of Novel <i>Psidium</i> Meroterpenoid Derivatives against Cisplatin-Induced Acute Kidney Injury Open
Cisplatin is a widely used drug for the clinical treatment of tumors. However, nephrotoxicity limits its widespread use. A series of compounds including eight analogs (G3-G10) and 40 simplifiers (G11-G50) were synthesized bas…
View article: Target fishing and mechanistic insights of the natural anticancer drug candidate chlorogenic acid
Target fishing and mechanistic insights of the natural anticancer drug candidate chlorogenic acid Open
Chlorogenic acid (CGA) is a natural product that effectively inhibits tumor growth, demonstrated in many preclinical models, and phase II clinical trials for patients with glioma. However, its direct proteomic targets and anticancer molecu…
View article: Design, Synthesis, and Bioevaluation of Novel Reversibly Photoswitchable PI3K Inhibitors Based on Phenylazopyridine Derivatives toward Light-Controlled Cancer Treatment
Design, Synthesis, and Bioevaluation of Novel Reversibly Photoswitchable PI3K Inhibitors Based on Phenylazopyridine Derivatives toward Light-Controlled Cancer Treatment Open
Photopharmacology is an emerging approach for achieving light-controlled drug activity. Herein, we design and synthesize a novel series of photoswitchable PI3K inhibitors by replacing a sulfonamide moiety with an azo group in a 4-methylqui…
View article: YPD-29B is an oral Small Molecular Targeting PD-L1 for Treating Human Cancers
YPD-29B is an oral Small Molecular Targeting PD-L1 for Treating Human Cancers Open
Background and Purpose: PD-1 and PD-L1 antibodies have brought extraordinary clinical beneficial for cancer patients and their indications are expanding incessantly. Currently, most PD-1/PD-L1 products are delivered intravenously which may…
View article: Discovery of Natural Ah Receptor Antagonists from <i>Salvia miltiorrhiza</i> Bunge and Synthesis of Analogs for Tumor Immunotherapy
Discovery of Natural Ah Receptor Antagonists from <i>Salvia miltiorrhiza</i> Bunge and Synthesis of Analogs for Tumor Immunotherapy Open
IDO/TDO/Kyn/AhR signaling plays a crucial role in regulating innate and adaptive immunity, and targeting Ah receptor (AhR) inhibition can potentially redirect immune cells toward an antitumoral phenotype. Therefore, AhR is an attractive dr…
View article: Dynamic gut microbiome-metabolome in cationic bovine serum albumin induced experimental immune-complex glomerulonephritis and effect of losartan and mycophenolate mofetil on microbiota modulation
Dynamic gut microbiome-metabolome in cationic bovine serum albumin induced experimental immune-complex glomerulonephritis and effect of losartan and mycophenolate mofetil on microbiota modulation Open
View article: Rational design and optimization of novel 4-methyl quinazoline derivatives as PI3K/HDAC dual inhibitors with benzamide as zinc binding moiety for the treatment of acute myeloid leukemia
Rational design and optimization of novel 4-methyl quinazoline derivatives as PI3K/HDAC dual inhibitors with benzamide as zinc binding moiety for the treatment of acute myeloid leukemia Open
View article: Discovery of Quinazoline-2,4(1<i>H</i>,3<i>H</i>)-dione Derivatives Containing a Piperizinone Moiety as Potent PARP-1/2 Inhibitors─Design, Synthesis, <i>In Vivo</i> Antitumor Activity, and X-ray Crystal Structure Analysis
Discovery of Quinazoline-2,4(1<i>H</i>,3<i>H</i>)-dione Derivatives Containing a Piperizinone Moiety as Potent PARP-1/2 Inhibitors─Design, Synthesis, <i>In Vivo</i> Antitumor Activity, and X-ray Crystal Structure Analysis Open
PARP-1/2 inhibitors have become an important therapeutic strategy for the treatment of HR-deficient tumors. However, discovery of new inhibitors with an improved and distinct pharmacological file still need enormous explorations. Herein, a…
View article: Targeting the Subpocket Enables the Discovery of Thiadiazole–Pyridazine Derivatives as Glutaminase C Inhibitors
Targeting the Subpocket Enables the Discovery of Thiadiazole–Pyridazine Derivatives as Glutaminase C Inhibitors Open
As glutaminase C (GAC) has become an attractive target for cancer treatment by regulating glutaminolysis, thus, interest in GAC inhibitors has risen in recent years. Herein, a potential binding subpocket comprising basic residues was ident…
View article: Discovery, Optimization, and Evaluation of Novel <i>N</i>-(Benzimidazol-5-yl)-1,3,4-thiadiazol-2-amine Analogues as Potent STAT3 Inhibitors for Cancer Treatment
Discovery, Optimization, and Evaluation of Novel <i>N</i>-(Benzimidazol-5-yl)-1,3,4-thiadiazol-2-amine Analogues as Potent STAT3 Inhibitors for Cancer Treatment Open
Signal transducer and activator of transcription 3 (STAT3) is an attractive target for cancer therapy. However, identifying potent and selective STAT3 small-molecule inhibitors with drug-like properties remains challenging. Based on a scaf…
View article: Discovery of a Novel Photocaged PI3K Inhibitor Capable of Real-Time Reporting of Drug Release
Discovery of a Novel Photocaged PI3K Inhibitor Capable of Real-Time Reporting of Drug Release Open
A novel photocaged PI3K inhibitor 2 was designed and synthesized by introducing a cascade photocaging group to block its key interaction with the kinase. Upon UV light irradiation, the photocaged compound released a highly potent PI…
View article: Chlorogenic Acid Induced Neuroblastoma Cells Differentiation via the ACAT1-TPK1-PDH Pathway
Chlorogenic Acid Induced Neuroblastoma Cells Differentiation via the ACAT1-TPK1-PDH Pathway Open
Background: Chlorogenic acid (CHA) has been shown to have substantial biological activities, including anti-inflammatory, antioxidant, and antitumor effects. However, the pharmacological role of CHA in neuroblastoma has not yet been assess…
View article: S-72, a Novel Orally Available Tubulin Inhibitor, Overcomes Paclitaxel Resistance via Inactivation of the STING Pathway in Breast Cancer
S-72, a Novel Orally Available Tubulin Inhibitor, Overcomes Paclitaxel Resistance via Inactivation of the STING Pathway in Breast Cancer Open
Microtubule-targeting agents are widely used as active anticancer drugs. However, drug resistance always emerges after their long-term use, especially in the case of paclitaxel, which is the cornerstone of all subtypes of breast cancer tre…
View article: Author correction to “YPD-30, a prodrug of YPD-29B, is an oral small-molecule inhibitor targeting PD-L1 for the treatment of human cancer” [Acta Pharmaceutica Sinica B 12 (2022) 2845–2858]
Author correction to “YPD-30, a prodrug of YPD-29B, is an oral small-molecule inhibitor targeting PD-L1 for the treatment of human cancer” [Acta Pharmaceutica Sinica B 12 (2022) 2845–2858] Open
View article: SHMT2 Promotes Gastric Cancer Development through Regulation of HIF1α/VEGF/STAT3 Signaling
SHMT2 Promotes Gastric Cancer Development through Regulation of HIF1α/VEGF/STAT3 Signaling Open
The metabolic enzymes involved in one-carbon metabolism are closely associated with tumor progression and could be potential targets for cancer therapy. Recent studies showed that serine hydroxymethyltransferase 2 (SHMT2), a crucial enzyme…
View article: Rational Design and Optimization of Novel 4-Methyl Quinazoline Derivatives as Pi3k/Hdac Dual Inhibitors with Benzamide as Zinc Binding Moiety for the Treatment of Acute Myeloid Leukemia
Rational Design and Optimization of Novel 4-Methyl Quinazoline Derivatives as Pi3k/Hdac Dual Inhibitors with Benzamide as Zinc Binding Moiety for the Treatment of Acute Myeloid Leukemia Open
View article: Optimization of Benzamide Derivatives as Potent and Orally Active Tubulin Inhibitors Targeting the Colchicine Binding Site
Optimization of Benzamide Derivatives as Potent and Orally Active Tubulin Inhibitors Targeting the Colchicine Binding Site Open
Targeting the colchicine binding site on tubulin is a promising strategy to develop cancer therapeutics. Herein, we describe our systematic structure-activity relationship studies of benzamide derivatives that lead to an identification of …
View article: Structure-activity relationship study of amidobenzimidazole derivatives as stimulator of interferon genes (STING) agonists
Structure-activity relationship study of amidobenzimidazole derivatives as stimulator of interferon genes (STING) agonists Open
View article: Chlorogenic Acid Relieves the Lupus Erythematosus-like Skin Lesions and Arthritis in MRL/lpr Mice
Chlorogenic Acid Relieves the Lupus Erythematosus-like Skin Lesions and Arthritis in MRL/lpr Mice Open
Chlorogenic acid (CGA) is a phenylpropyl substance synthesized through the shikimic acid pathway. In addition to its anti-tumor, anti-inflammatory, and antioxidant abilities, CGA also has immunomodulatory effects. The aim of the present st…
View article: Gut Microbiota, the Potential Biological Medicine for Prevention, Intervention and Drug Sensitization to Fight Diseases
Gut Microbiota, the Potential Biological Medicine for Prevention, Intervention and Drug Sensitization to Fight Diseases Open
As the largest “immune organ” of human beings, the gut microbiota is symbiotic and mutually beneficial with the human host, playing multiple physiological functions. Studies have long shown that dysbiosis of gut microbiota is associated wi…
View article: [Corrigendum] The novel anti‑neuroblastoma agent PF403, inhibits proliferation and invasion <i>in vitro</i> and in brain xenografts
[Corrigendum] The novel anti‑neuroblastoma agent PF403, inhibits proliferation and invasion <i>in vitro</i> and in brain xenografts Open
Subsequently to the publication of the above article, the authors have realized that Fig. 5D on p. 183 was published containing an error; essentially, the images chosen for the data panels representing the Fig. 5D, CAT3 Low and …
View article: Discovery of a novel photoswitchable PI3K inhibitor toward optically-controlled anticancer activity
Discovery of a novel photoswitchable PI3K inhibitor toward optically-controlled anticancer activity Open
View article: Design, synthesis, and biological evaluation of pyrrolopyrimidine derivatives as novel Bruton's tyrosine kinase (BTK) inhibitors
Design, synthesis, and biological evaluation of pyrrolopyrimidine derivatives as novel Bruton's tyrosine kinase (BTK) inhibitors Open
View article: A Novel PARP Inhibitor YHP-836 For the Treatment of BRCA-Deficiency Cancers
A Novel PARP Inhibitor YHP-836 For the Treatment of BRCA-Deficiency Cancers Open
PARP inhibitors have clinically demonstrated good antitumor activity in patients with BRCA mutations. Here, we described YHP-836, a novel PARP inhibitor, YHP-836 demonstrated excellent inhibitory activity for both PARP1 and PARP2 enzymes. …
View article: Chlorogenic Acid Prevents UVA-Induced Skin Photoaging through Regulating Collagen Metabolism and Apoptosis in Human Dermal Fibroblasts
Chlorogenic Acid Prevents UVA-Induced Skin Photoaging through Regulating Collagen Metabolism and Apoptosis in Human Dermal Fibroblasts Open
Skin aging is categorized as chronological aging and photo-aging that affected by intrinsic and extrinsic factors. The present study aimed to investigate the anti-aging ability and its underlying mechanism of chlorogenic acid (CGA) on huma…
View article: Efficacy and adverse events of octreotide long-acting release in acromegaly: a real-world retrospective study
Efficacy and adverse events of octreotide long-acting release in acromegaly: a real-world retrospective study Open
Our findings revealed that octreotide LAR treatment is effective in normalizing GH and IGF-1 levels in Chinese patients with acromegaly. In addition, adverse events related to octreotide LAR use were moderate and well tolerated by the pati…