日期:
2020 年 — 2026 年
2020
2021
2022
2023
2024
2025
2026
影响因子:

Drug Repurposing: Conversion of the Peripherally Restricted HIV Protease Inhibitor Amprenavir to Potent, Selective, and CNS-Penetrant Agonists for the Cannabinoid Receptor 2

药物再利用:将外周限制性 HIV 蛋白酶抑制剂安普那韦转化为强效、选择性强且能穿透血脑屏障的大麻素受体 2 激动剂

Haymer, Daniel H; Duncan, Renn A; Rodriguez, Alice L; Han, Allie; Lindsay, Richard J; Wijesiri, N Kithmini; Thompson Gray, Analisa; Krishnan, Srinivasan; Qi, Aidong; Brown, Benjamin P; Boutaud, Olivier; Engers, Darren W; Jones, Carrie K; Niswender, Colleen M; Lindsley, Craig W; Bender, Aaron M

Discovery of VU6025733 (AG06827): A Highly Selective, Orally Bioavailable, and Structurally Distinct M(4) Muscarinic Acetylcholine Receptor Positive Allosteric Modulator (PAM) with Robust In Vivo Efficacy

VU6025733 (AG06827) 的发现:一种高选择性、口服生物利用度高、结构独特的 M(4) 毒蕈碱乙酰胆碱受体正向变构调节剂 (PAM),具有强大的体内疗效

Gregro, Alison R; Park, Charlotte; Long, Madeline F; Baker, Logan A; Bollinger, Katrina A; Ringuette, Anna E; Peng, Li; Luscombe, Vincent B; Billard, Natasha B; Rodriguez, Alice L; Niswender, Colleen M; Peng, Weimin; Dickerson, Jonathan W; Rook, Jerri M; O'Neill, Jordan; Chang, Sichen; Boonen, Harrie C M; Jensen, Thomas; Thomsen, Morten S; Bridges, Thomas M; Boutaud, Olivier; Conn, P Jeffrey; Engers, Darren W; Lindsley, Craig W; Temple, Kayla J

Discovery of VU6083859, a TAOK1 Selective Inhibitor, and VU6080195, a pan-TAOK Activator

发现 VU6083859(一种 TAOK1 选择性抑制剂)和 VU6080195(一种泛 TAOK 激活剂)

Schultz, Daniel C; Parr, Lauren C; Sweet, Hunter; Lamb, Sean; Engers, Julie L; Napier, Nathaniel C; McKinnie, Hallie G; Whomble, David; Kramlinger, Valerie; Boutaud, Olivier; Lindsley, Craig W

Optimization of Selective and CNS Penetrant Alkyne-Based TREK Inhibitors: The Discovery and Characterization of ONO-9517601 (VU6022856) and ONO-7927846 (VU6024391)

选择性和中枢神经系统渗透性炔基TREK抑制剂的优化:ONO-9517601 (VU6022856) 和 ONO-7927846 (VU6024391) 的发现和表征

Tanaka, Motoyuki; Sekioka, Yoko; Hashimoto, Gakuji; Mori, Takahiro; Shono, Tomoyuki; Isaji, Yuuki; Hisaichi, Katsuya; Childress, Elizabeth S; Bollinger, Sean; Schmitt, Joza A; Chopko, Trevor C; Garrison, Aaron T; Perry, Charles K; Chronister, Keagan; Kramer, Meghan; Chang, Sichen; Watson, Katherine J; Dickerson, Jonathan W; Bubser, Michael; Rook, Jerri M; Jones, Carrie K; Boutaud, Olivier; Bridges, Thomas M; Denton, Jerod S; Engers, Darren W; Kurata, Haruto; Lindsley, Craig W

Evaluation of antiseizure medication concentration ranges in blood samples using an automated big data approach

利用自动化大数据方法评估血液样本中抗癫痫药物浓度范围

Nersesjan, Mariam; Hoffmann-Lücke, Elke; Greibe, Eva; Aaslo, Per Hersom; Bak, Lasse Kristoffer; Pedersen, Lars Engers; Fruekilde, Palle Bach Nielsen; Stark, Anette; Christensen, Jakob; Brønden, Andreas; Larsen, Jens Borggaard

Silver Nanoparticles from Hermetia illucens Biomass Are Antibacterial Against Pseudomonas aeruginosa Infection in Caenorhabditis elegans

来自黑水螅生物质的银纳米颗粒对秀丽隐杆线虫中的铜绿假单胞菌感染具有抗菌作用

Ayech, Alinne; Hollmann, Gabriela; Gomes, Robson M Marreiro; Rodrigues, Belisa A; Engers, Vanessa K; Gonçalves, Rafael S; Nornberg, Sandro Daniel; Ramos, Daniela F; Zimmer, Karine Rigon; Monserrat, José M

Discovery of Thieno[3,2-b]pyridine-5-carboxamide and 2,3-Difluorobenzamide Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5

噻吩并[3,2-b]吡啶-5-甲酰胺和2,3-二氟苯甲酰胺作为代谢型谷氨酸受体5亚型的负变构调节剂的发现

Crocker, Katherine E; Henderson, Scott H; Capstick, Rory A; Whomble, David L; Bender, Aaron M; Felts, Andrew S; Han, Changho; Engers, Julie L; Billard, Natasha B; Maurer, Mallory A; Cho, Hyekyung P; Rodriguez, Alice L; Niswender, Colleen M; O'Neill, Jordan; Watson, Katherine J; Chang, Sichen; Blobaum, Anna L; Boutaud, Olivier; Peng, Weimin; Rook, Jerri M; Conn, P Jeffrey; Lindsley, Craig W; Temple, Kayla J

Discovery of a Novel sp(3)‑Rich M(1) Positive Allosteric Modulators (PAMs) Chemotype via Scaffold Hopping

通过骨架跃迁发现一种新型富含sp(3)杂环的M(1)正变构调节剂(PAM)化学类型

Bungard, Joseph D; Spearing, Paul; Nishio, Yu; Rathnayake, Upendra; Presley, Chris C; Chang, Sichen; Kling, Haley E; Thompson, Analisa D; Cho, Hyekyung P; Peng, Li; Rodriguez, Alice L; Niswender, Colleen M; Boutaud, Olivier; Kramlinger, Valerie; Jones, Carrie K; Conn, P Jeffrey; Engers, Julie L; Engers, Darren W; Lindsley, Craig W; Han, Changho

Characterization of Next-Generation Inhibitors for the Inward-Rectifier Potassium Channel K(ir)2.1: Discovery of VU6080824

内向整流钾通道 K(ir)2.1 的下一代抑制剂的特性研究:VU6080824 的发现

Duncan, Renn A; Haymer, Daniel H; Lazarenko, Roman M; Li, Liangping; Blackwell, Yvette; Days, Emily L; Krishnan, Srinivasan; Gray, Analisa Thompson; Boutaud, Olivier; Engers, Darren W; Lindsley, Craig W; Denton, Jerod S; Bender, Aaron M

Discovery of ONO-TR-772 (VU6018042): A Highly Selective and CNS Penetrant TREK Inhibitor in Vivo Tool Compound

ONO-TR-772 (VU6018042) 的发现:一种高选择性且能穿透中枢神经系统的 TREK 抑制剂体内工具化合物

Tanaka, Motoyuki; Mori, Takahiro; Hashimoto, Gakuji; Mitsui, Katsukuni; Kishi, Akihiro; Childress, Elizabeth S; Bollinger, Sean R; Chopko, Trevor C; Bridges, Thomas M; Stafford, Douglas G; Huang, Zhonping; Wolf, Mark A; Engers, Darren W; Denton, Jerod S; Kurata, Haruto; Lindsley, Craig W