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(S

(S)-atenolol (Atpure)

✓ Approved

Emcure Pharmaceuticals · ADRB1 · 小分子

什么是 (S)-atenolol?

(S)-atenolol 是一种小分子,由Emcure Pharmaceuticals研发。该药已获批,用于治疗相关适应症,给药途径:Oral (PO)。

药物档案

商品名Atpure
公司Emcure Pharmaceuticals
药物类别小分子
分子靶点ADRB1
给药途径Oral (PO)
状态Approved

作用机制

分子靶点

(S)-atenolol 作用于 1 个分子靶点:

ADRB1adrenoceptor beta 1 (B1AR, RHR)
需要更深入的分析?Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

(S)-atenolol 针对 2 个适应症,涉及 2 个治疗领域。

治疗领域疾病/病症分期
Cardiac disordersAngina pectoris✓ Approved
Vascular disordersHypertension✓ Approved

相关研究文献

PubMedACS chemical biology2026-09-10

ZDHHC13 Is a Catalytically Deficient Protein S-Acyltransferase That Functions via a Noncanonical Mechanism.

Petropavlovskiy Andrey A AA, Church Alysha M AM, Doerksen Amelia H AH, Raina Rahul R et al.

S-Acylation is the addition of fatty acids to cysteine residues to regulate protein function and localization. S-Acylation is catalyzed by ZDHHC (Asp-His-His-Cys) protein S-acyltransferases (PATs), which S-acylate protein substrates by first auto-S-acylating the catalytic cysteine of the DHHC active site followed by transfer to the substrate. ZDHHC13 and ZDHHC17 are related ankyrin repeat domain (ANK) PATs that S-acylate neuronal proteins, including Huntingtin (HTT), the protein mutated in Huntington disease. However, unlike ZDHHC17 and other human PATs, ZDHHC13 possesses a noncanonical DQHC active site. As the first histidine is essential for auto-S-acylation, it is unclear if ZDHHC13 is catalytically active. Our phylogenetic analysis of eukaryotic ANK PATs showed that while the DHHC of ZDHHC17 orthologues is highly conserved, the motif is variable among ZDHHC13 orthologues, suggesting evolution independent of catalytic activity. We found that the ZDHHC13 catalytic cysteine is indeed S-acylated in cells, albeit substantially less than ZDHHC17 or ZDHHC20. We also confirmed minimal autoacylation activity in vitro with purified ZDHHC13. While wild-type (WT) ZDHHC13 increased S-acylation of an HTT1-588 fragment in cells, surprisingly, catalytically dead DQHS ZDHHC13 facilitated HTT1-588 S-acylation equally. This suggests that the ZDHHC13 catalytic cysteine is not required for substrate S-acylation and instead ZDHHC13 contributes to S-acylation via an indirect mechanism. Furthermore, ZDHHC13 was identified in a high-molecular-weight complex, suggesting a scaffolding or accessory role in S-acylation. This work broadens our understanding of this noncanonical PAT and lays the foundation for future mechanistic and structural studies.

PMID 42717663
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PubMedJournal of ginseng research2026-09-10

Direct targeting of ORAI1 by ginsenoside Rg3 modulates calcium signaling and senescence-associated AMPK-NRF2 activation.

Lee Sooyeon S, Ko Minjeong M, Kwon Ho Jeong HJ

20(S)-ginsenoside Rg3 (Rg3(S)), a major saponin derived from red ginseng, exhibits diverse biological activities, including antioxidant and anti-senescence effects. However, the direct molecular targets through which Rg3(S) regulates calcium signaling and its role at membrane contact sites during cellular senescence remain largely unknown. Plasma membrane (PM)-endoplasmic reticulum (ER) contacts and related protein interactions were analyzed using proximity ligation assays and co-immunoprecipitation. Direct binding of Rg3(S) to ORAI1 was validated using cellular thermal shift assays and microscale thermophoresis. Molecular docking simulations followed by site-directed mutagenesis were used to define critical binding residues. Cytosolic calcium levels and cellular senescence were assessed using calcium imaging and senescence-associated β-galactosidase staining. Rg3(S) increased cytosolic calcium levels independently of ER calcium depletion and was accompanied by a reduction in PM-ER contacts. Rg3(S) directly bound to ORAI1 in a dose-dependent manner, identifying ORAI1 as a previously unrecognized molecular target of ginsenoside Rg3. Molecular docking revealed LYS204 and ILE229 within the extracellular loop of ORAI1 as key residues maintaining this interaction. Mutation of these residues abolished Rg3(S)-induced calcium influx, leading to impaired activation of the AMPK-NRF2 pathway and attenuation of the anti-senescence effect of Rg3(S). These findings identify ORAI1 as a key molecular mediator of ginsenoside Rg3(S)-induced calcium signaling linked to cellular senescence. By modulating PM-ER contact sites and cytosolic calcium dynamics, Rg3(S) attenuates senescence, providing new mechanistic insight into the anti-aging potential of ginseng-derived compounds beyond autophagy-centered pathways.

PMID 42718879
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PubMedJournal of biochemistry2026-09-10

Biochemical characterization of a homocysteine S-methyltransferase from Leuconostoc suionicum.

Oikawa Tadao T, Harada Nanami N, Hanafusa Sumire S, Yamanaka Kazuya K et al.

We identified and characterized a homocysteine S-methyltransferase (HMT) from the lactic acid bacterium Leuconostoc suionicum LT-38, representing the first characterization of an HMT from lactic acid bacteria. The enzyme exhibited a kcat/Km value of 15.7 mM-1 s-1 toward L-homocysteine. It showed optimal activity at 30 °C and pH 7.5 and remained stable over a broad range of temperatures (30-60 °C) and pH values (5-9). The enzyme accepted both L- and D-homocysteine as methyl acceptors but displayed markedly higher catalytic efficiency toward the L-form (~30-fold). In contrast, L- and D-cysteine were not utilized. Both S-methyl-L-methionine and S-methyl-D-methionine were consumed in reactions containing racemic S-methyl-DL-methionine, and S-adenosyl-L-methionine was also accepted, whereas betaine and related compounds were not utilized. Gel filtration analysis indicated a monomeric structure (~32 kDa). Phylogenetic analysis showed that Ls-HMT clustered with bacterial HMT homologs and was distinct from mammalian BHMT/BHMT2 proteins. Inductively coupled plasma-mass spectrometry revealed approximately one Zn atom per enzyme molecule, and the Zn-depleted apo enzyme showed no detectable activity. These findings support that Ls-HMT is a Zn-dependent HMT with relatively high activity and expand the functional diversity of microbial HMTs.

PMID 42720554
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PubMedTherapeutic advances in medical oncology2026-09-10

Adjuvant FOLFIRINOX versus S-1 monotherapy for resected PDAC: retrospective real-world data.

Tang Hui H, Li Zhengxia Z, You Tingting T, Ying Jinrong J et al.

Although modified FOLFIRINOX (mFOLFIRINOX) has improved survival in patients with resected pancreatic ductal adenocarcinoma (PDAC) in clinical studies, S-1 is also a treatment option with desirable efficacy and limited toxicity. We aimed to compare the efficacy and safety of adjuvant mFOLFIRINOX with those of S-1 monotherapy for PDAC. This study aimed to compare the efficacy and safety of adjuvant mFOLFIRINOX versus S-1 monotherapy in resected PDAC. A retrospective real-world study. Patients with resected PDAC who received adjuvant mFOLFIRINOX or S-1 chemotherapy at Peking Union Medical College Hospital were reviewed. A total of 223 patients were included, with 141 receiving S-1 and 82 receiving mFOLFIRINOX. Patients who received mFOLFIRINOX were younger (median age: 55.5 vs 66 years, p < 0.001) and had a significantly lower proportion of early-stage disease (stage I: 20.7% vs 46.1%, p < 0.001). The median disease-free survival (18.1 vs 12.5 months, p = 0.021) and overall survival (51.4 vs 24.7 months, p = 0.006) of the mFOLFIRINOX group were significantly longer, even after adjustment for bias. However, the incidence of grade 3 or 4 adverse events (65.0% vs 39.4%, p = 0.007), especially fatigue and gastrointestinal toxicity, was greater in the mFOLFIRINOX group than in the S-1 group. Furthermore, the molecular features of the included patients were also explored, and KMT2D alterations may be prognostic indicators of poor survival outcomes. No correlation between alterations in the homologous recombination repair-related genes and prognosis was observed in postoperative patients with PDAC. The mFOLFIRINOX regimen as an adjuvant chemotherapy for patients with resected PDAC demonstrated better efficacy than did S-1 monotherapy.

PMID 42719505
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PubMedFrontiers in cellular and infection microbiology2026-09-10

Epidemiological characteristics of bacterial lower respiratory tract infections in Jingzhou, Central China, 2020-2024.

Yang Yan Y, Wen Zihan Z, Qu Yue Y, Lei Yao Y et al.

Lower respiratory tract infections (LRTIs) represent a significant global public health issue and impose a substantial disease burden. However, regional epidemiological surveillance data on bacterial LRTIs in central China remain insufficient. This study aimed to systematically analyze the epidemiological characteristics of patients with bacterial LRTIs in Jingzhou, Hubei Province, China. This study included 5,442 hospitalized patients diagnosed with LRTIs between January 2020 and December 2024. Detection of respiratory pathogens was performed both using a chip-based loop-mediated isothermal amplification (LAMP) assay and the standard culture method (SCM). The LAMP assay kit simultaneously detects ten predefined bacterial respiratory pathogens, including Streptococcus pneumoniae (S. pneumoniae), Staphylococcus aureus (S. aureus), Klebsiella pneumoniae (K. pneumoniae), Pseudomonas aeruginosa (P. aeruginosa), Acinetobacter baumannii (A. baumannii), Stenotrophomonas maltophilia (S. maltophilia), Haemophilus influenzae (H. influenzae), Legionella pneumophila (L. pneumophila), Mycoplasma pneumoniae (M. pneumoniae), and Mycobacterium tuberculosis (M. tuberculosis). Among 5,442 samples, the overall positive rate of LAMP was 31.86%, with single-pathogen infections accounting for 26.17%. H. influenzae (8.18%) and S. pneumoniae (7.75%) were the most commonly detected pathogens. Dual-pathogen co-infections predominated among polymicrobial infections, with S. pneumoniae and H. influenzae representing the most frequent pathogen combination. The LAMP assay demonstrated a higher overall positive rate than SCM, with moderate agreement observed between the two methods for most pathogens. The overall pathogen positive rate exhibited seasonal variation, peaking from April to June. S. pneumoniae showed a bimodal distribution, with higher positive rate in May-June and November-December annually. During the COVID-19 pandemic era, S. pneumoniae and H. influenzae were predominant, while the positive rates of M. pneumoniae and M. tuberculosis notably increased in the post-pandemic era. School-aged children exhibited the highest positive rate, with M. pneumoniae as the predominant pathogen. Pathogen composition was more diverse among adults and older adults. These findings demonstrate significant age-related and temporal variations in the pathogen spectrum of bacterial LRTIs and provide epidemiological evidence to support empirical antibacterial decision-making and population-targeted prevention strategies. In addition, LAMP may serve as a practical molecular diagnostic tool for rapid bacterial pathogen detection, although its clinical utility in primary healthcare settings warrants further investigation.

PMID 42718465
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PubMedInternational journal of systematic and evolutionary microbiology2026-09-10

Genomic evidence that Shouchella miscanthi (Shin et al. 2020) Joshi et al. 2022 is a later heterotypic synonym of Shouchella hunanensis (Patel and Gupta 2020) Joshi et al. 2022.

Liu Qing Q, Yang Lei-Lei LL, Zhang Guo-Qing GQ, Xin Yu-Hua YH

Shouchella hunanensis DSM 23008T and Shouchella miscanthi AK13T were originally described from forest soil and the rhizosphere of Miscanthus sacchariflorus, respectively. The two strains share closely similar phenotypic properties, and their 16S rRNA gene sequences show 99.5% similarity. Phylogenetic analysis of all 16S rRNA gene copies revealed copy-dependent placements, whereas the phylogenomic analysis placed the two type strains and three additional genomes in a strongly supported, short-branched cluster. Eight 16S rRNA gene copies were identified in each genome, with detectable intragenomic heterogeneity, particularly in AK13ᵀ. Pairwise average nt identity among the two type-strain genomes and three additional publicly available genomes ranged from 99.0% to 99.3%, clearly above the accepted species boundary. The digital DNA-DNA hybridization value between strains S. hunanensis DSM 23008T and S. miscanthi AK13T was 92.5%. On the basis of the combined phylogenetic, genomic and phenotypic evidence, S. miscanthi (Shin et al. 2020) Joshi et al. 2022 is proposed as a later heterotypic synonym of S. hunanensis (Patel and Gupta 2020) Joshi et al. 2022.

PMID 42720666
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