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 7-(Pyridin-3-yl)thieno[3,2-b]pyridine-5-carboxamides as Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5

发现 7-(吡啶-3-基)噻吩并[3,2-b]吡啶-5-甲酰胺类化合物作为代谢型谷氨酸受体5亚型的负变构调节剂

Henderson, Scott H; Ringuette, Anna E; Whomble, David L; Capstick, Rory A; Richardson, Alexa E; Maurer, Mallory A; Billard, Natasha B; Lei, Xia; Wilkinson, Joshua C; Kethanapalli, Sri H; Cho, Hyekyung P; Rodriguez, Alice L; Niswender, Colleen M; Peng, Weimin; Rook, Jerri M; Chang, Sichen; Blobaum, Anna L; Boutaud, Olivier; Felts, Andrew S; Conn, P Jeffrey; Lindsley, Craig W; Temple, Kayla J

Characterization of Novel and Known Activators of Cannabinoid Receptor Subtype 2 Reveals Mixed Pharmacology That Differentiates Mycophenolate Mofetil and GW-842,166X from MDA7

对新型和已知大麻素受体亚型 2 激活剂的表征揭示了混合药理学特性,该特性使吗替麦考酚酯和 GW-842,166X 与 MDA7 有所区别。

Rodriguez, Alice L; Qi, Aidong; Han, Allie; Kling, Haley E; Quitalig, Marc C; Bender, Aaron M; Barbaro, Lisa; Whomble, David; Lindsley, Craig W; Niswender, Colleen M

Overexpression of mGlu(7B) in Mice: Implications for Neurodevelopmental Disorders.

小鼠中 mGlu(7B) 的过度表达:对神经发育障碍的影响。

Freitas Geanne A, Weiss Kelly, Bavadekar Vaishnavi, Vermudez Sheryl Anne D, Fisher Nicole M, Buch Aditi, Dogra Shalini, Xiang Zixiu, Gogliotti Rocco G, Niswender Colleen 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

Discovery of VU0467319: an M(1) Positive Allosteric Modulator Candidate That Advanced into Clinical Trials

VU0467319 的发现:一种进入临床试验的 M(1) 正向变构调节剂候选药物

Poslunsey, Michael S; Wood, Michael R; Han, Changho; Stauffer, Shaun R; Panarese, Joseph D; Melancon, Bruce J; Engers, Julie L; Dickerson, Jonathan W; Peng, Weimin; Noetzel, Meredith J; Cho, Hyekyung P; Rodriguez, Alice L; Hopkins, Corey R; Morrison, Ryan; Crouch, Rachel D; Bridges, Thomas M; Blobaum, Anna L; Boutaud, Olivier; Daniels, J Scott; Kates, Michael J; Castelhano, Arlindo; Rook, Jerri M; Niswender, Colleen M; Jones, Carrie K; Conn, P Jeffrey; Lindsley, Craig W

Further Optimization of the mGlu(1) PAM VU6024578/BI02982816: Discovery and Characterization of VU6033685

mGlu(1) PAM VU6024578/BI02982816 的进一步优化:VU6033685 的发现和表征

Reed, Carson W; Kalbfleisch, Jacob F; Turkett, Jeremy A; Trombley, Trevor A; Spearing, Paul K; Haymer, Daniel H; Quitalig, Marc; Dickerson, Jonathan W; Foster, Daniel J; Blobaum, Annie L; Boutaud, Olivier; Cho, Hyekyung P; Niswender, Colleen M; Rook, Jerri M; Priepke, Henning; Sommer, Heiko; Scheuerer, Stefan; Ursu, Daniel; Conn, P Jeffrey; Melancon, Bruce J; Lindsley, Craig W

Application of Deuterium in an M(1) Positive Allosteric Modulator Back-Up Program: The Discovery of VU6045422

氘在M(1)正变构调节剂备用方案中的应用:VU6045422的发现

Engers, Julie L; Li, Jinming; Han, Changho; Long, Madeline F; Gregro, Alison R; Presley, Christopher C; Dickerson, Jonathan W; Peng, Weimin; Cho, Hyekyung P; Rodriguez, Alice L; Xiang, Zixiu; Boutaud, Olivier; O'Carroll, Colin; Dey, P Markus; Burstein, Ethan S; Niswender, Colleen M; Rook, Jerri M; Conn, P Jeffrey; Engers, Darren W; Lindsley, Craig W