Design of Benzyl-triazolopyrimidine-Based NADPH Oxidase Inhibitors Leads to the Discovery of a Potent Dual Covalent NOX2/MAOB Inhibitor حسب Beatrice Noce (16540800)

"…We found that <b>9a</b>, bearing a pargyline moiety, is also able to selectively inhibit MAOB over MAOA (465-fold) with an IC₅₀ of 0.182 μM, being the first-in-class dual NOX2/MAOB covalent inhibitor. …"

Development of (2-(Benzyloxy)phenyl)methanamine Derivatives as Potent and Selective Inhibitors of CARM1 for the Treatment of Melanoma حسب Zhihao Liu (419349)

"…In our previous study, we have identified a series of type I PRMT inhibitors, among which ZL-28-6 (<b>6</b>) exhibited increased activity against CARM1 while displaying decreased potency against other type I PRMTs. …"

Development of (2-(Benzyloxy)phenyl)methanamine Derivatives as Potent and Selective Inhibitors of CARM1 for the Treatment of Melanoma حسب Zhihao Liu (419349)

"…In our previous study, we have identified a series of type I PRMT inhibitors, among which ZL-28-6 (<b>6</b>) exhibited increased activity against CARM1 while displaying decreased potency against other type I PRMTs. …"

Development of (2-(Benzyloxy)phenyl)methanamine Derivatives as Potent and Selective Inhibitors of CARM1 for the Treatment of Melanoma حسب Zhihao Liu (419349)

"…In our previous study, we have identified a series of type I PRMT inhibitors, among which ZL-28-6 (<b>6</b>) exhibited increased activity against CARM1 while displaying decreased potency against other type I PRMTs. …"

First-in-Class Hydrazide-Based HDAC6 Selective Inhibitor with Potent Oral Anti-Inflammatory Activity by Attenuating NLRP3 Inflammasome Activation حسب Kairui Yue (11874403)

"…In this study, we report the first highly selective HDAC6 inhibitor with hydrazide as the zinc-binding group (ZBG), which displays superior pharmacokinetic properties to the current hydroxamic acid inhibitors. …"

First-in-Class Hydrazide-Based HDAC6 Selective Inhibitor with Potent Oral Anti-Inflammatory Activity by Attenuating NLRP3 Inflammasome Activation حسب Kairui Yue (11874403)

"…In this study, we report the first highly selective HDAC6 inhibitor with hydrazide as the zinc-binding group (ZBG), which displays superior pharmacokinetic properties to the current hydroxamic acid inhibitors. …"

Discovery of Triazolyl Derivatives of Cucurbitacin B Targeting IGF2BP1 against Non-Small Cell Lung Cancer حسب Fan-Fan Shang (16953264)

"…Cucurbitacin B (CuB) is a potent but toxic anticancer natural product. Herein, we designed and synthesized 2-OH- and 16-OH-modified CuB derivatives to improve their antitumor efficacy and reduce toxicity. …"

Measurement of ATP production in HL-1 cells exposed for 12 or 72h to LG, NG, HG or IHG. حسب Patrick Mordel (17020879)

PCR-RFLP detection results of the three new SNPs (g.-1293C>G, g.56T>C, g.7017C>T) in bovine <i>C3</i> gene. حسب Yonghui Wang (287491)

الموضوعات:

Host population bottlenecks decrease microbiome diversity. حسب Michael Ørsted (5926028)

2‑Aminobenzoxazole Derivatives as Potent Inhibitors of the Sphingosine-1-Phosphate Transporter Spinster Homolog 2 (Spns2) حسب Ariel L. Burgio (15069256)

"…To develop more potent compounds, we initiated a structure–activity relationship study that identified 2-aminobenzoxazole as a viable scaffold. …"

Design and Synthesis of Novel Spiro Derivatives as Potent and Reversible Monoacylglycerol Lipase (MAGL) Inhibitors: Bioisosteric Transformation from 3‑Oxo-3,4-dihydro‑2<i>H</i>‑ben... حسب Shuhei Ikeda (2380180)

"…Optimization of the left hand side afforded <b>4f</b> as a promising reversible MAGL inhibitor, which showed potent in vitro MAGL inhibitory activity (IC₅₀ 6.2 nM), good oral absorption, blood–brain barrier penetration, and significant pharmacodynamic changes (2-arachidonoylglycerol increase and arachidonic acid decrease) at 0.3–10 mg/kg, po. in mice.…"

Original full-length gel image related to Fig 5. Full, non-adjusted gel image corresponding to the Western blot data shown in Fig 5. Molecular weight markers are indicated in kilod... حسب Jin-Hwa Kim (101817)

الموضوعات:

E₅₀ values. حسب Junxia Zhou (14381598)

Data_Sheet_1_Microclimatic Warming Leads to a Decrease in Species and Growth Form Diversity: Insights From a Tropical Alpine Grassland.PDF حسب Sisimac A. Duchicela (11503918)

"…After 7 years of warming, we found significant increases in mean monthly (+0.24°C), daily (+0.16°C), and night air temperatures (+0.33°C) inside the OTCs, and the OTCs intensified microclimatic conditions during the dry season. …"

Retinoic acid decreases intracellular K⁺ in pectoral fin buds via transcriptional activation of the calcineurin inhibitor <i>rcan2</i>. حسب Xiaowen Jiang (8291814)

Emerging Disinfection Byproduct 2,6-Dichlorobenzoquinone-Induced Cardiovascular Developmental Toxicity of Embryonic Zebrafish and Larvae: Imaging and Transcriptome Analysis حسب Xue Yang (144876)

"…Aromatic DBPs represent a significant portion of total DBPs, but their effects on cardiovascular development are unclear. In this study, we examined the effects of an aromatic DBP, 2,6-dichlorobenzoquinone (DCBQ), on the cardiovascular development of zebrafish embryos. …"

Effect of seed priming on anti-oxidants and lipid peroxidation in pearl millet at 50 DAS. حسب N. K. Gupta (11211399)

The fraction of predicted heterozygotes that are set to “No Call” by RHA decreases as the size of the heterozygote cluster increases. حسب Orna Mizrahi-Man (42539)

DataSheet_1_Hemizygous nonsense variant in the moesin gene (MSN) leads to a new autoimmune phenotype of Immunodeficiency 50.pdf حسب András L. Kovács (13565251)

"…We present a putative new autoimmune phenotype of Immunodeficiency 50 (MIM300988) characterized by antiphospholipid syndrome, Hashimoto’s thyroiditis, leg ulcers, and juvenile tooth loss, associated with W217X mutation of the MSN gene.…"