📅 2026년 6월 6일 | PubMed 수집 논문
★ 주요 논문 — 이번 수집의 하이라이트
HDAC inhibition reprograms stem cell fate to suppress infantile hemangioma vasculogenesis.
Infantile hemangioma (IH), the most common vascular tumor of infancy, relies on hemangioma stem cells (HemSCs) to drive pathological vasculogenesis during the proliferating phase. While beta-blockers are currently first-line treatment for IH, resistance and rebound growth necessitates novel strategi…
Bioactive treatments against chronic myeloid leukemia from Hypericum lancasteri targeting p53 pathway.
The discovery of biologically active compounds from plants is an emerging challenge in natural pharmaceutical development. Here, we report the comprehensive strategy for undescribed compounds discovery targeting p53 pathway from Hypericum lancasteri against chronic myeloid leukemia (CML). The UHPLC-…
Discovery of novel ULK1 inhibitors by virtual screening, synthesis, in vitro assay and molecular dynamics simulations.
The serine/threonine kinase UNC-51-like autophagy-activating kinase 1 (ULK1) has emerged as a promising target for cancer treatment. This study utilized an integrative approach combining computational and experimental methods to discover novel ULK1 inhibitors. Through molecular fingerprint similarit…
A natural product-hybridization approach toward anticancer drug discovery: synthesis and antitumor evaluation of CTBC6, designed from sulforaphane and magnolol.
Natural products, with their promising drug-like profiles, inherent pharmacological potential, and a vast reservoir of privileged structures, have long been recognized as a rich source of hit compounds in anticancer drug discovery. Building upon our group’s prior work, this study delves into the med…
Clonal lineage tracing of innate immune cells in human cancer.
Innate immune cells constitute the majority of the tumor microenvironment (TME) and mediate anti-tumor immunity and immunotherapy responses. While single-cell T and B cell receptor sequencing have revealed insights into the clonal dynamics of adaptive immunity, the lack of analogous tools has preclu…
Discovery and characterization of Z1: an imipridone-based ClpP agonist with potent anti-staphylococcal activity.
To identify novel antibacterial agents targeting Staphylococcus aureus ClpP (SaClpP), a target-based screening model was established using the fluorogenic substrate Suc-LY-AMC, leading to the identification of a potent hit, Z1, from a proprietary compound library. SDS-PAGE-based protein degradation …
Hyperuricemia aggravates acute pancreatitis through CNR1-mediated inflammatory signaling and gut-pancreas axis dysregulation: a multi-omics and clinical study.
Hyperuricemia (HUA) is implicated in various metabolic and inflammatory diseases. Its role in the pathogenesis of acute pancreatitis (AP), particularly in gut-pancreas crosstalk and the underlying molecular mechanisms, remains poorly understood. This study integrates clinical epidemiology (UK Bioban…
Patient-derived lymphoma spheroids reveal predictive markers of glofitamab resistance in relapsed/refractory B-NHL.
Bispecific antibodies (bsAbs) such as glofitamab represent a promising therapeutic approach for relapsed/refractory B-cell non-Hodgkin lymphoma (R/R B-NHL), but resistance mechanisms remain poorly understood. This study aimed to identify predictive markers of bsAb resistance based on the response of…
Antioxidant lipid nanoparticles enhance mRNA stability for regeneration therapy and gene editing.
The success of mRNA vaccines has motivated the development of mRNA therapeutics to treat a wide range of diseases, as well as applications in regenerative medicine. However, the inherent instability of mRNA under conditions of oxidative stress renders these applications challenging. Here we report a…
Comprehensive multi-omics analysis identifies cancer subtypes and prognostic signatures of hepatitis B virus-associated hepatocellular carcinoma.
Hepatitis B virus-associated hepatocellular carcinoma (HBV-HCC) is a heterogeneous malignancy with poor prognosis, necessitating refined classification and novel therapeutics. Leveraging multi-omics data, we utilized the MOVICS package to identify two robust cancer subtypes (CSs) from the TCGA-LIHC …
Pathogenesis of diffuse large B cell lymphoma proteogenotypes.
The clinical and molecular heterogeneity of diffuse large B cell lymphoma (DLBCL) is incompletely understood. By integrating proteomic, transcriptomic, and genomic data from 478 DLBCL tumors, we identify seven DLBCL proteogenotypes (PGs) reflecting specific pathophysiological features that span know…
Peptide modified lipid nanoparticles Co-Delivering IL-12 mRNA and PD-L1 siRNA for glioblastoma immunotherapy.
Lipid nanoparticles (LNPs) have emerged as the most advanced nucleic acid delivery vehicles in clinical applications, achieving successful targeting of major organs such as the liver, spleen, and lungs. However, efficient penetration of the blood-brain barrier (BBB) continues to be a key obstacle fo…
Multi-target pyrazolopyrimidine-coumarin derivatives as potent CA IX/XII and tubulin polymerization inhibitors: Design, synthesis, and biological evaluation.
In the current medical era, developing multi-target anticancer agents that simultaneously engage complementary cellular vulnerabilities represents a promising strategy to overcome the inherent limitations of single-target therapeutics. Building on insights from our previous investigation, we synthes…
Design and synthesis of novel 1,2,4-triazolobenzene sulfonamide derivatives as selective CDK1 inhibitors with potent in vivo anticancer efficacy.
Cyclin-dependent kinase 1 (CDK1) is a key regulator of cell cycle progression and a potential therapeutic target for invasive malignancies. However, developing selective CDK1 inhibitors with manageable toxicity remains a significant challenge. In this study, a novel series of 1,2,4-triazolobenzene s…
Discovery of quinoxaline-chalcone derivatives as covalent colchicine binding site inhibitors for breast and fibrosarcoma treatment.
Targeting the colchicine binding site is an attractive pharmacological strategy to overcome the multidrug resistance microtubule-targeting agents are faced with. Herein, a series of novel covalent quinoxaline-chalcone derivatives were rationally designed using pharmacophore fusion with S-Ⅳ-25…
Design, synthesis, and optimization of Honokiol-Piperazine derivatives as lung-enriched agents against MRSA pneumonia infection.
Methicillin-resistant Staphylococcus aureus (MRSA) causes severe bacterial pneumonia; current therapies (e.g., vancomycin) suffer from poor pulmonary bioavailability and dose-limiting safety concerns, demanding precision lung-enriched agents. However, small-molecule lung-enriched antibacterials are …
High-throughput screening for the discovery of antidepressants targeting adenosine A2A receptors.
The adenosine A2A receptor (A2AR) is a promising therapeutic target for depression, as evidenced by the notable antidepressant-like efficacy of its antagonists. However, conventional screening methods for A2AR ligands are hampered by low throughput and operational complexity. To address this, we dev…
Discovery of small-sized tris-aryl imidazoles as bifunctional ligands for c-Myc and KRAS G-quadruplexes.
Tumor growth promotion is achieved by overlapping intrinsic pathways of c-Myc and KRAS, and dual-targeting therapies emerge as an encouraging approach for drug discovery. G-quadruplexes (G4s) exist in the promoter regions of c-Myc and KRAS genes, rendering the transcriptional repression. G4 ligands …
Rapid discovery of repurposed drugs targeting SARS-CoV-2 spike HR1 by DNA-encoded library screening.
The membrane fusion process mediated by the SARS-CoV-2 spike protein is a key therapeutic target. Its heptad repeat 1 (HR1) domain forms a conserved trimeric groove critical for forming the fusion-competent six-helix bundle with HR2. We used DNA-encoded library screening to identify small molecules …
Regioselectivity enhancement of UDP-glycosyltransferase via tunnel-block engineering for the exclusive synthesis of icariside D2.
Glycosylation is a common modification in natural products that enhances their pharmacological value. Icariside D2, derived from the O-glycosylation of tyrosol, exerts significant antitumor and cardiovascular protective effects; however, biosynthesis is limited by poor UDP-glycosyltransferase (UGT) …
Hydroxyl radical from iridium(III)-based photosensitizer triggers PANoptosis and ferroptosis for hypoxia-tolerant photodynamic immunotherapy.
Exploring photosensitizers that efficiently generate oxygen-independent hydroxyl radical (•OH) and activate highly immunogenic PANoptosis and ferroptosis shows promise in addressing the limited efficacy of photodynamic immunotherapy (PDI) in the hypoxic and immunosuppressive tumor microenviro…
PET imaging of XPO1 engagement with [18F]selinexor: A pharmacodynamic theranostic strategy for multiple myeloma.
Exportin 1 (XPO1), a nuclear export protein frequently overexpressed in multiple myeloma (MM), represents a validated therapeutic target. However, noninvasive imaging approaches capable of assessing XPO1 engagement and pharmacodynamic modulation during therapy remain limited. Here, we present the ra…
Novel staurosporine-type indolocarbazole glycoalkaloids as potent and selective FLT3-ITD inhibitors for acute myeloid leukemia.
Aberrant activation of the FMS-like tyrosine kinase 3 (FLT3) caused by internal tandem duplication (ITD) mutations is a major driver of acute myeloid leukemia (AML). To identify novel FLT3 inhibitors, two structurally distinct series of indolocarbazole glycoalkaloids, rebeccamycin-type and staurospo…
Novel platinum(IV) complexes trigger apoptosis and ferroptosis to conquer cisplatin resistance in triple-negative breast cancer.
Platinum (II)-based agents are commonly used for the cancer treatment, but are limited by drug resistance and severe systemic toxicity. To address these limitations, sulfasalazine derivatives were employed as ligands to construct four platinum(IV) complexes, which exhibited superior anticancer activ…
Injectable pre-vascularized alginate-collagen hydrogel with sustained delivery of miR-133a-loaded lipid nanoparticles for myocardial repair.
Myocardial infarction (MI) remains a leading cause of heart failure, and current therapies fail to prevent cardiomyocyte loss or support effective tissue regeneration. Injectable hydrogels (HGs) have emerged as promising platforms for delivering therapeutic cues and structural support; however, few …
Novel benzophenones from the fibrous roots of Anemarrhena asphodeloides Bunge inhibit hepatocellular carcinoma activity by targeting ALDH3A1.
Hepatocellular carcinoma (HCC) represents a formidable clinical challenge due to limited treatment options. Plant-derived natural products, in particular, represent a promising source for such discoveries. The fibrous roots of Anemarrhena asphodeloides Bunge (FRA) were subjected to investigation. Si…
Integrative multi-omics identifies lyn-mediated microglial activation as a key driver of central post-stroke pain.
Central post-stroke pain (CPSP) is a neuropathic pain condition that severely impairs patients’ quality of life and recovery, yet its pathogenesis remains poorly understood. This study employed a multi-omics approach to investigate CPSP mechanisms in a mouse model generated by stereotaxic injection …
Stereoselective AChE/BChE/BACE1 inhibition by enantiomeric norsesquiterpenoids with an unprecedented oxatricyclo[7.2.1.01,9]dodecane scaffold from the soft coral Sclerophytum humesi.
Chemical investigation of the soft coral Sclerophytum humesi led to the discovery of (±)-norsclerohumin A (1), a pair of enantiomeric norsesquiterpenoids possessing an unprecedented oxatricyclo[7.2.1.01,9]dodecane scaffold with a rare C5-O-C8 intramolecular ether-bridge. Their structures were e…
Discovery, structural characterization, chemical synthesis, anti-migraine effect, and pharmacological mechanism of ligualkaloid B: an alkaloid from Ligusticum chuanxiong.
Migraine is a common neurological disorder and imposes a heavy burden on individuals and society. The rhizomes of Ligusticum chuanxiong Hort. are known as an excellent medicine for headache. Our previous study demonstrated that its total alkaloids possess significant anti-migraine effects. However, …
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HDAC inhibition reprograms stem cell fate to suppress infantile hemangioma vasculogenesis.
Infantile hemangioma (IH), the most common vascular tumor of infancy, relies on hemangioma stem cells (HemSCs) to drive pathological vasculogenesis during the proliferating phase. While beta-blockers are currently first-line treatment for IH, resistance and rebound growth necessitates novel strategi…
전임상 마우스 모델에서 infantile hemangioma 억제 기전을 제시한 연구다. 임상 근거는 아직 없지만, 기존 propranolol과의 병용 가능성과 새로운 표적성 때문에 후속 연구 가치가 있다.
Bioactive treatments against chronic myeloid leukemia from Hypericum lancasteri targeting p53 pathway.
The discovery of biologically active compounds from plants is an emerging challenge in natural pharmaceutical development. Here, we report the comprehensive strategy for undescribed compounds discovery targeting p53 pathway from Hypericum lancasteri against chronic myeloid leukemia (CML). The UHPLC-…
천연물에서 신규 화합물을 발굴하고 CML에 대한 활성과 기전을 함께 제시한 연구다. 다만 임상 근거는 세포 및 동물 수준에 머물러 있어 직접적인 환자 적용 가능성은 아직 낮다. 그럼에도 p53/MDM2 표적 가능성과 in vivo 효능이 있어 후속 최적화 가치가 있다.
Discovery of novel ULK1 inhibitors by virtual screening, synthesis, in vitro assay and molecular dynamics simulations.
The serine/threonine kinase UNC-51-like autophagy-activating kinase 1 (ULK1) has emerged as a promising target for cancer treatment. This study utilized an integrative approach combining computational and experimental methods to discover novel ULK1 inhibitors. Through molecular fingerprint similarit…
새로운 ULK1 저해제 후보를 발굴한 초기 약물발굴 연구다. 효소 수준에서는 매우 강한 활성을 보였지만, 세포 효능과 인체 근거는 제한적이다. 따라서 발견 가치와 후속 개발 가능성은 있으나 임상적 의미는 아직 초기 단계다.
A natural product-hybridization approach toward anticancer drug discovery: synthesis and antitumor evaluation of CTBC6, designed from sulforaphane and magnolol.
Natural products, with their promising drug-like profiles, inherent pharmacological potential, and a vast reservoir of privileged structures, have long been recognized as a rich source of hit compounds in anticancer drug discovery. Building upon our group’s prior work, this study delves into the med…
이 연구는 천연물 기반 하이브리드 화합물 CTBC6의 항유방암 활성을 제시한 전임상 연구다. 동물과 세포 수준에서 효능과 기전을 함께 보여주어 후속 개발 가치는 있으나, 임상적 근거는 아직 제한적이다. 상업적으로는 리드 최적화와 독성·약동학 검증이 필요한 초기 단계다.
Clonal lineage tracing of innate immune cells in human cancer.
Innate immune cells constitute the majority of the tumor microenvironment (TME) and mediate anti-tumor immunity and immunotherapy responses. While single-cell T and B cell receptor sequencing have revealed insights into the clonal dynamics of adaptive immunity, the lack of analogous tools has preclu…
인간 종양 조직에서 선천면역세포의 계통을 추적할 수 있는 새로운 분석법을 제시한 연구다. 임상적 직접성은 낮지만, 인간 데이터 기반의 방법론적 혁신과 후속 면역종양학 연구 활용 가능성이 크다.
Discovery and characterization of Z1: an imipridone-based ClpP agonist with potent anti-staphylococcal activity.
To identify novel antibacterial agents targeting Staphylococcus aureus ClpP (SaClpP), a target-based screening model was established using the fluorogenic substrate Suc-LY-AMC, leading to the identification of a potent hit, Z1, from a proprietary compound library. SDS-PAGE-based protein degradation …
사람 대상 임상 근거는 없지만, MRSA에 대한 강한 항균 활성과 마우스 감염모델 효능이 있어 전임상 가치가 높다. ClpP 표적 항생제 후보로서 차별성이 있고, PK와 내성 빈도 데이터도 있어 후속 개발 가능성이 보인다.
Hyperuricemia aggravates acute pancreatitis through CNR1-mediated inflammatory signaling and gut-pancreas axis dysregulation: a multi-omics and clinical study.
Hyperuricemia (HUA) is implicated in various metabolic and inflammatory diseases. Its role in the pathogenesis of acute pancreatitis (AP), particularly in gut-pancreas crosstalk and the underlying molecular mechanisms, remains poorly understood. This study integrates clinical epidemiology (UK Bioban…
임상 코호트와 동물·세포 실험을 함께 사용해 고요산혈증이 급성췌장염을 악화시킨다는 연관성과 기전을 제시한 연구다. 진단 보조 지표 가능성은 있으나 아직 관찰연구와 전임상 근거 수준이라 즉시 임상 적용 단계는 아니다. 기전적 새로움은 있으나 상업화는 추가 검증이 많이 필요하다.
Patient-derived lymphoma spheroids reveal predictive markers of glofitamab resistance in relapsed/refractory B-NHL.
Bispecific antibodies (bsAbs) such as glofitamab represent a promising therapeutic approach for relapsed/refractory B-cell non-Hodgkin lymphoma (R/R B-NHL), but resistance mechanisms remain poorly understood. This study aimed to identify predictive markers of bsAb resistance based on the response of…
환자 유래 3차원 모델과 실제 환자 코호트 분석을 함께 사용해 glofitamab 저항성의 후보 바이오마커를 제시한 연구다. 임상적 근거는 아직 전임상·전향적 검증 전 단계이지만, 병용전략과 환자선별로 이어질 가능성이 있어 의미가 있다.
Antioxidant lipid nanoparticles enhance mRNA stability for regeneration therapy and gene editing.
The success of mRNA vaccines has motivated the development of mRNA therapeutics to treat a wide range of diseases, as well as applications in regenerative medicine. However, the inherent instability of mRNA under conditions of oxidative stress renders these applications challenging. Here we report a…
산화 스트레스 환경에서 mRNA 안정성을 높이는 새로운 LNP 설계를 제시한 연구다. 임상 근거는 전임상 수준이지만, 재생의학과 유전자 편집 전달체로서 확장성이 있어 의미가 있다.
Comprehensive multi-omics analysis identifies cancer subtypes and prognostic signatures of hepatitis B virus-associated hepatocellular carcinoma.
Hepatitis B virus-associated hepatocellular carcinoma (HBV-HCC) is a heterogeneous malignancy with poor prognosis, necessitating refined classification and novel therapeutics. Leveraging multi-omics data, we utilized the MOVICS package to identify two robust cancer subtypes (CSs) from the TCGA-LIHC …
이 연구는 HBV-HCC의 분류와 예후 예측을 정교화한 점에서 의미가 있다. 다만 임상 근거는 아직 전임상 수준이며, 실제 환자 적용까지는 추가 검증이 필요하다. 약물 재창출 후보와 기전 제시는 흥미롭지만 상용화 가능성은 초기 단계다.
Pathogenesis of diffuse large B cell lymphoma proteogenotypes.
The clinical and molecular heterogeneity of diffuse large B cell lymphoma (DLBCL) is incompletely understood. By integrating proteomic, transcriptomic, and genomic data from 478 DLBCL tumors, we identify seven DLBCL proteogenotypes (PGs) reflecting specific pathophysiological features that span know…
DLBCL의 이질성을 다중오믹스로 정교하게 분류한 연구다. 임상적으로는 즉시 치료를 바꾸는 수준은 아니지만, 고위험군 예측과 향후 진단·치료 표적 발굴에 의미가 있다. 상업적으로도 직접 제품화 단계는 아니나 바이오마커 개발 가능성은 있다.
Aptamer-targeted biomimetic gold nanostar core with mesoporous organosilica layer for NIR-triggered chemo-photothermal therapy and CT imaging of melanoma.
Chemo-photothermal therapy (chemo-PTT), which integrates chemotherapy with photothermal ablation, has emerged as a promising strategy for enhancing antitumor efficacy compared with single-modality treatments. However, aggressive malignancies such as melanoma still demand more efficient targeted and …
Patients in-use stability and safety of repacked delayed-release capsules of sodium divalproex.
Divalproex Sodium (DVS) is an antiseizure narrow therapeutic index drug. Despite its effectiveness, the primary reason for reduced compliance and/or treatment discontinuation is intolerance to its gastric side effects. Delayed-release forms to alleviate gastric side effects are available as enteric …
Covalent JAK3 inhibitors based on 2-arylamino and 7H-pyrrolo[2,3-d]pyrimidine scaffold: design, synthesis, and biological evaluation for the potential treatment of bortezomib-resistant multiple myeloma.
Bortezomib, as a first-generation proteasome inhibitor, is one of the cornerstone drugs in the treatment of multiple myeloma. However, its long-term clinical efficacy is severely limited by both primary and acquired resistance. Studies have shown that the Janus kinase 3/Signal transducer and activat…
Multivariate feature analysis of early-stage laryngeal cancer serum components using surface-enhanced Raman spectroscopy.
Laryngeal cancer is a common head-and-neck malignant tumor with geographically variable incidence. Its lack of specific early clinical symptoms often causes missed diagnosis, leading to most cases being identified at intermediate/advanced stages and thus poor treatment efficacy and prognosis. Early,…
Solvent-induced phase separation enhances the drug loading and encapsulation efficiency of a highly hydrophilic low-molecular-weight S-propargyl-cysteine in injectable PLGA microspheres.
Efficient encapsulating of highly hydrophilic low-molecular-weight compound within poly (D, L-lactic-co-glycolic acid) (PLGA) to obtain microspheres with both excellent drug loading capacity (DL) and encapsulation efficiency (EE) was substantially challenging. This study specifically aimed to enhanc…
Peptide modified lipid nanoparticles Co-Delivering IL-12 mRNA and PD-L1 siRNA for glioblastoma immunotherapy.
Lipid nanoparticles (LNPs) have emerged as the most advanced nucleic acid delivery vehicles in clinical applications, achieving successful targeting of major organs such as the liver, spleen, and lungs. However, efficient penetration of the blood-brain barrier (BBB) continues to be a key obstacle fo…
전임상 in vivo 연구로, 교모세포종 치료용 뇌표적 전달 플랫폼의 가능성을 보여준다. 임상적 근거는 아직 부족하지만 BBB 장벽 극복과 병용 면역치료라는 점에서 후속 연구 가치가 있다.
On-site loading of powder-attached microneedles enables quantitative and reproducible intradermal vaccine delivery.
Conventional vaccination relies on liquid formulations that require cold-chain storage and administration by trained healthcare personnel, creating logistical barriers in resource-limited settings. Microneedle-based intradermal delivery enables solid vaccine administration; however, most microneedle…
Nanostructured lipid carrier enabled delivery of levofloxacin and clove essential oil to overcome Pseudomonas aeruginosa biofilm infection in burn wounds- a synergistic approach.
Conventional antibiotics struggle to completely eradicate the infection because of their ineffective penetration of biofilms. New multimodal strategy integrating antibiofilm agent with antimicrobials delivered as nanomedicine could be a powerful approach to overcome biofilm resistance. Bioactive ess…
Multi-target pyrazolopyrimidine-coumarin derivatives as potent CA IX/XII and tubulin polymerization inhibitors: Design, synthesis, and biological evaluation.
In the current medical era, developing multi-target anticancer agents that simultaneously engage complementary cellular vulnerabilities represents a promising strategy to overcome the inherent limitations of single-target therapeutics. Building on insights from our previous investigation, we synthes…
전임상 항암 후보물질을 제시한 연구다. 기전적 설계와 세포 수준 효능은 인상적이지만, 동물 효능과 안전성 데이터가 없어 임상적 의미는 제한적이다. 다만 다중표적 항암 리드로서 후속 최적화 가치는 있다.
Design and synthesis of novel 1,2,4-triazolobenzene sulfonamide derivatives as selective CDK1 inhibitors with potent in vivo anticancer efficacy.
Cyclin-dependent kinase 1 (CDK1) is a key regulator of cell cycle progression and a potential therapeutic target for invasive malignancies. However, developing selective CDK1 inhibitors with manageable toxicity remains a significant challenge. In this study, a novel series of 1,2,4-triazolobenzene s…
전임상 항암 후보물질을 제시한 연구다. CDK1 선택성과 in vivo 효능은 의미가 있으나, 아직 인간 데이터가 없어 임상적 영향은 제한적이다. 기전과 약효가 비교적 선명해 후속 최적화 가치가 있다.
Discovery of quinoxaline-chalcone derivatives as covalent colchicine binding site inhibitors for breast and fibrosarcoma treatment.
Targeting the colchicine binding site is an attractive pharmacological strategy to overcome the multidrug resistance microtubule-targeting agents are faced with. Herein, a series of novel covalent quinoxaline-chalcone derivatives were rationally designed using pharmacophore fusion with S-Ⅳ-25…
이 연구는 신규 covalent tubulin inhibitor 후보를 제시한 전임상 연구다. 세포 및 동물 수준에서 효능과 기전이 확인되어 발견적 가치는 높지만, 임상적 근거는 아직 제한적이다. 상업적 가능성은 있으나 독성, 선택성, 개발 난이도 검증이 더 필요하다.
Design and optimization of potent, selective, and peripherally acting JNK3 inhibitors for chronic kidney disease.
Chronic kidney disease (CKD) is characterized by progressive fibrosis and podocyte injury driven in part by TGF-β-dependent MAPK signaling. Although pan-JNK inhibition has shown antifibrotic efficacy, isoform selectivity and safety remain major challenges. Herein, we report the design, synthes…
Design, synthesis, and optimization of Honokiol-Piperazine derivatives as lung-enriched agents against MRSA pneumonia infection.
Methicillin-resistant Staphylococcus aureus (MRSA) causes severe bacterial pneumonia; current therapies (e.g., vancomycin) suffer from poor pulmonary bioavailability and dose-limiting safety concerns, demanding precision lung-enriched agents. However, small-molecule lung-enriched antibacterials are …
전임상 단계의 항MRSA 후보물질을 제시한 연구다. 폐 표적화와 항균 효능을 함께 보여 의미가 있으나, 사람 대상 근거는 없다. 상용화 가능성은 있으나 추가 독성·약동학·효능 검증이 필요하다.
High-throughput screening for the discovery of antidepressants targeting adenosine A2A receptors.
The adenosine A2A receptor (A2AR) is a promising therapeutic target for depression, as evidenced by the notable antidepressant-like efficacy of its antagonists. However, conventional screening methods for A2AR ligands are hampered by low throughput and operational complexity. To address this, we dev…
이 연구는 인간 임상 근거가 아니라 동물모델 기반의 전임상 연구다. 그러나 A2A 수용체 표적 항우울제 후보를 빠르게 발굴할 수 있는 스크리닝 플랫폼을 제시했다는 점에서 발견 가치가 높다. 상업적 가치는 초기 단계이지만, 후속 최적화와 독성·약동학 검증이 진행되면 의미가 커질 수 있다.
Design, synthesis and biological evaluation of novel fluoroquinolone-uracil hybrids against methicillin-resistant Staphylococcus Epidermidis (MRSE) infections.
A series of 24 novel fluoroquinolone-uracil hybrids via various lengths linkers were designed, synthesized and evaluated for their antibacterial activities against both Gram-negative and Gram-positive bacteria, including resistant strains. All target compounds were fully characterized by 1H NMR, 13C…
Discovery of small-sized tris-aryl imidazoles as bifunctional ligands for c-Myc and KRAS G-quadruplexes.
Tumor growth promotion is achieved by overlapping intrinsic pathways of c-Myc and KRAS, and dual-targeting therapies emerge as an encouraging approach for drug discovery. G-quadruplexes (G4s) exist in the promoter regions of c-Myc and KRAS genes, rendering the transcriptional repression. G4 ligands …
이 연구는 신규 G-quadruplex 이중 표적 리간드를 제시한 점에서 발견적 가치가 있다. 다만 임상 근거는 세포와 마우스 수준에 머물러 있어 직접적인 임상 영향은 제한적이다. 상업적 가능성은 있으나 전임상 단계라 개발 리스크가 크다.
Rapid discovery of repurposed drugs targeting SARS-CoV-2 spike HR1 by DNA-encoded library screening.
The membrane fusion process mediated by the SARS-CoV-2 spike protein is a key therapeutic target. Its heptad repeat 1 (HR1) domain forms a conserved trimeric groove critical for forming the fusion-competent six-helix bundle with HR2. We used DNA-encoded library screening to identify small molecules …
이 연구는 HR1 표적 소분자를 재창출 방식으로 발굴해 융합 억제 가능성을 보였다. 다만 세포 수준 결과 중심이라 임상적 근거는 아직 제한적이다. 기전적 새로움은 있으나 상용화까지는 추가 검증이 필요하다.
Regioselectivity enhancement of UDP-glycosyltransferase via tunnel-block engineering for the exclusive synthesis of icariside D2.
Glycosylation is a common modification in natural products that enhances their pharmacological value. Icariside D2, derived from the O-glycosylation of tyrosol, exerts significant antitumor and cardiovascular protective effects; however, biosynthesis is limited by poor UDP-glycosyltransferase (UGT) …
인간 대상 임상 근거는 없고 효소 공학 기반의 전임상 연구다. 그러나 선택성 향상과 활성 유지라는 실용적 문제를 동시에 해결해 발견 가치가 높다. 산업적 응용 가능성은 있으나 아직 공정 개발과 스케일업 검증이 필요하다.
Hydroxyl radical from iridium(III)-based photosensitizer triggers PANoptosis and ferroptosis for hypoxia-tolerant photodynamic immunotherapy.
Exploring photosensitizers that efficiently generate oxygen-independent hydroxyl radical (•OH) and activate highly immunogenic PANoptosis and ferroptosis shows promise in addressing the limited efficacy of photodynamic immunotherapy (PDI) in the hypoxic and immunosuppressive tumor microenviro…
전임상 연구로서 임상적 직접성은 낮다. 다만 저산소 종양 미세환경에서 작동하는 광감작제라는 점과 면역활성화 효과는 의미가 있다. 상용화 가능성은 있으나 아직 동물 수준이라 개발 리스크가 크다.
Rational β-turn engineering of a disulfide-free β-hairpin-like antimicrobial peptide W2PG with enhanced stability, selectivity, and in vivo efficacy.
Antimicrobial resistance (AMR) is an increasing global concern, while the development of new antibiotics remains limited. Antimicrobial peptides (AMPs) offer an alternative due to their broad-spectrum and membrane-targeting features, but their translation is restricted by instability and cytotoxicit…
PET imaging of XPO1 engagement with [18F]selinexor: A pharmacodynamic theranostic strategy for multiple myeloma.
Exportin 1 (XPO1), a nuclear export protein frequently overexpressed in multiple myeloma (MM), represents a validated therapeutic target. However, noninvasive imaging approaches capable of assessing XPO1 engagement and pharmacodynamic modulation during therapy remain limited. Here, we present the ra…
전임상 단계의 theranostic PET tracer 연구다. XPO1 결합과 약물 반응을 비침습적으로 추적할 수 있다는 점은 의미가 크지만, 임상 검증과 구조 최적화가 아직 필요하다. 상업적 가치는 있으나 개발 리스크가 높다.
Cell-Mimetic Antifouling Poly(ethylene glycol) Interface Enables Selective Capture and Viable Release of Circulating Tumor Cells.
Circulating tumor cells (CTCs) hold great promise as biomarkers for cancer diagnosis, metastasis assessment, and therapeutic monitoring. However, their extremely low abundance and interference from complex blood components make their efficient and specific isolation highly challenging. Herein, we de…
Novel staurosporine-type indolocarbazole glycoalkaloids as potent and selective FLT3-ITD inhibitors for acute myeloid leukemia.
Aberrant activation of the FMS-like tyrosine kinase 3 (FLT3) caused by internal tandem duplication (ITD) mutations is a major driver of acute myeloid leukemia (AML). To identify novel FLT3 inhibitors, two structurally distinct series of indolocarbazole glycoalkaloids, rebeccamycin-type and staurospo…
임상 근거는 아직 전임상 수준이라 직접적 환자 효용은 제한적이다. 그러나 FLT3-ITD에 대한 선택성과 기전 검증이 좋아 후속 최적화 가치가 높다. 상업성은 초기 단계지만 AML 표적치료제 후보로서 잠재력은 있다.
Novel platinum(IV) complexes trigger apoptosis and ferroptosis to conquer cisplatin resistance in triple-negative breast cancer.
Platinum (II)-based agents are commonly used for the cancer treatment, but are limited by drug resistance and severe systemic toxicity. To address these limitations, sulfasalazine derivatives were employed as ligands to construct four platinum(IV) complexes, which exhibited superior anticancer activ…
전임상 연구로서 임상적 근거는 제한적이다. 그러나 시스플라틴 저항성 TNBC에서 이중 세포사멸 기전을 보인 점은 발견적 가치가 높다. 상업적 관점에서는 후보물질 단계로서 가능성은 있으나 개발 리스크가 크다.
Robotic vs thoracoscopic vs open lobectomy and segmentectomy for lung cancer: a multicenter cohort study in the ATS of Milan.
The study aimed at comparing the effectiveness of open thoracotomy (OT), video-assisted thoracoscopic surgery (VATS), and robot-assisted thoracic surgery (RATS) for anatomical lung resection in early-stage non-small cell lung cancer. We conducted a multicenter cohort study across eight hospitals in …
Clinical and geriatric factors associated with fracture risk in older adults with bone metastases: A prospective observational study.
Bone metastases frequently lead to fractures, causing substantial morbidity, impaired quality of life, and poor prognosis in older adults with cancer. This study aimed to evaluate fracture risk by integrating geriatric parameters with clinical and oncological factors in older patients with bone meta…
Tirzepatide for Recurrent Weight Gain after Bariatric Procedures: Real-World Evidence of Efficacy and Safety.
Recurrent weight gain after bariatric surgery (BS) or endoscopic bariatric therapy (EBT) remains a long-term clinical challenge, potentially undermining long-term treatment success. Tirzepatide, a dual agonist of the glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP…
Syntaphilin inhibits glioma invasion via modulating mitochondria redistribution and shapes the immune microenvironment: A potential prognostic biomarker.
Glioma remains a lethal brain malignancy with a dismal prognosis. Syntaphilin (SNPH), a mitochondrial anchoring protein, shows emerging relevance in cancer biology. This study investigates the diagnostic and prognostic potential of SNPH, while elucidatingits functional mechanisms in glioma progressi…
A transformer and 3D CNN-based feature fusion network with interpretable ability for Raman spectra analysis: improving the diagnosis of thyroid cancer.
Accurate differentiation of benign and malignant thyroid lesions continues to pose a significant clinical challenge. Raman spectroscopy offers label-free molecular fingerprints of cells, yet the identification of diagnostic spectral patterns remains challenging. While artificial intelligence has bee…
Maximizing drug loading in cavity microneedles through precision cavity engineering and centrifugal techniques.
Cavity microneedles achieve powder drug loading through the cavity structure within the needle, reducing drug loading limitations related to solubility and stability, and effectively increasing drug loading capacity. However, the unclear mechanisms for cavity formation, the compromised mechanical pe…
Plant-based diet quality and risk of age-related eye diseases: evidence from multi-cohorts with multi-omics insights.
Plant-based diets may influence age-related eye diseases (AREDs), but whether ocular benefits depend on diet quality remains unclear. We examined associations of a healthy plant-based diet index (PDI-H) and an unhealthy plant-based diet index (PDI-U) with age-related macular degeneration (AMD), cata…
Digital therapeutics for negative symptoms of psychosis: Where do we go from here?
Some of the most pressing unmet needs in the treatment of psychosis spectrum disorders are negative symptoms. Digital therapeutics (DTx) have been touted as a transformative approach to advancing mental health treatment, including for negative symptoms. Although existing trials demonstrate that DTx …
Injectable pre-vascularized alginate-collagen hydrogel with sustained delivery of miR-133a-loaded lipid nanoparticles for myocardial repair.
Myocardial infarction (MI) remains a leading cause of heart failure, and current therapies fail to prevent cardiomyocyte loss or support effective tissue regeneration. Injectable hydrogels (HGs) have emerged as promising platforms for delivering therapeutic cues and structural support; however, few …
심근경색 치료를 위한 복합 재생 플랫폼을 제시한 전임상 연구다. 혈관화와 miRNA 전달을 결합한 점은 새롭지만, 아직 인간 임상 근거는 없다. 상용화 가능성은 있으나 제조·안전성·효능 검증이 더 필요하다.
Establishment of the first nationwide registry for inherited hemoglobin and blood-related disorders (IHBD) in Saudi Arabia: design and clinical evaluation.
Inherited hemoglobinopathies, particularly sickle cell disease (SCD) and thalassemia, represent a major public health burden in Saudi Arabia. However, comprehensive nationwide real-world data have historically been fragmented across healthcare facilities. This study describes the development, govern…
Engineering β-amino acid antimicrobial peptides with enhanced stability and potential efficacy against gram-negative bacterial infections.
Antibiotics revolutionized bacterial infection treatment, but misuse has led to the rise of antimicrobial resistance, which threatens global health. In this study, a series of new antimicrobial peptides containing β-amino acid were developed, and some of them showed potent antibacterial activi…
Amphiphilic xanthotoxin derivatives with phosphatidylglycerol-targeting membrane disruption for potent anti-methicillin-resistant Staphylococcus aureus (MRSA) activity.
With the escalating threat posed by methicillin-resistant Staphylococcus aureus (MRSA) infections, the development of novel and potent antibacterial agents is an urgent priority. Based on this rationale, xanthotoxin was employed as the lead structure, a series of derivatives were designed and synthe…
Effects of Cytochrome P450 enzymes and drug-drug interaction on donafenib metabolism: in vivo, in vitro and in silico.
This study systematically elucidated the metabolic characteristics of the hepatocellular carcinoma (HCC) therapeutic drug donafenib and its drug-drug interaction (DDI) with the antiviral agent arbidol. In vitro phenotyping assays using chemical inhibitors and recombinant CYP enzymes identified CYP3A…
Oleoyl-hyaluronate nanoparticles for enhanced stability and bioactivity of encapsulated coenzyme Q10.
This study presents the successful encapsulation of coenzyme Q10 (CoQ10) within sodium oleoyl hyaluronate (O-HA; Mw ∼12,000 Da) nanoparticles, creating a concentrated, liquid colloidal dispersion. The nanoprecipitation process achieved high encapsulation efficiency (up to 96%) and a…
Real-world effectiveness and safety of apremilast in psoriatic arthritis: results from the multicenter Italian MAPSI II study.
To assess the effectiveness and safety of apremilast in the treatment of psoriatic arthritis (PsA) in a real-world setting across multiple rheumatology centers in Italy….
Hook plate fixation and the importance of anatomical reduction in periprosthetic hip fractures: a retrospective single-centre study at a United Kingdom District General Hospital.
Periprosthetic hip fractures are an increasingly common consequence of the expanding arthroplasty population and are associated with substantial morbidity, mortality, and technical operative complexity. Evidence evaluating hook plate fixation in routine district general hospital practice remains lim…