Thomas Bohnacker相关文献与解析，生知库 | 链接生命科学的每一步

Lukas Bissegger, Theodora A Constantin, Erhan Keles, Luka Raguž, Isobel Barlow-Busch, Clara Orbegozo, Thorsten Schaefer, Valentina Borlandelli, Thomas Bohnacker, Rohitha Sriramaratnam, Alexander Schäfer, Matthias Gstaiger, John E Burke, Chiara Borsari, Matthias P Wymann

信号转导

PI3K/Akt

PK3CA

发表日期：2024

文献求助收藏

4-(Difluoromethyl)-5-(4-((3 R,5 S)-3,5-dimethylmorpholino)-6-((R)-3-methylmorpholino)-1,3,5-triazin-2-yl)pyridin-2-amine (PQR626), a Potent, Orally Available, and Brain-Penetrant mTOR Inhibitor for the Treatment of Neurological Disorders

4-(二氟甲基)-5-(4-((3 R,5 S)-3,5-二甲基吗啉)-6-((R)-3-甲基吗啉)-1,3,5-三嗪-2-基)吡啶-2-胺 (PQR626)，一种强效、口服、脑渗透性 mTOR 抑制剂，用于治疗神经系统疾病

期刊:Journal of Medicinal Chemistry

影响因子:6.8

doi:10.1021/acs.jmedchem.0c00620

Chiara Borsari, Erhan Keles, Denise Rageot, Andrea Treyer, Thomas Bohnacker, Lukas Bissegger, Martina De Pascale, Anna Melone, Rohitha Sriramaratnam, Florent Beaufils, Matthias Hamburger, Paul Hebeisen, Wolfgang Löscher, Doriano Fabbro, Petra Hillmann, Matthias P Wymann

PI3K γ Regulatory Protein p84 Determines Mast Cell Sensitivity to Ras Inhibition-Moving Towards Cell Specific PI3K Targeting?

PI3Kγ调节蛋白p84决定肥大细胞对Ras抑制的敏感性 - 朝着细胞特异性PI3K靶向发展？

期刊:Frontiers in Immunology

影响因子:5.7

doi:10.3389/fimmu.2020.585070

Julie R Jin, Elena Gogvadze, Ana R Xavier, Thomas Bohnacker, Jan Voelzmann, Matthias P Wymann

A Conformational Restriction Strategy for the Identification of a Highly Selective Pyrimido-pyrrolo-oxazine mTOR Inhibitor

构象限制策略用于鉴定高选择性嘧啶并吡咯并恶嗪 mTOR 抑制剂

期刊:Journal of Medicinal Chemistry

影响因子:6.8

doi:10.1021/acs.jmedchem.9b00972

Chiara Borsari, Denise Rageot, Alix Dall'Asen, Thomas Bohnacker, Anna Melone, Alexander M Sele, Eileen Jackson, Jean-Baptiste Langlois, Florent Beaufils, Paul Hebeisen, Doriano Fabbro, Petra Hillmann, Matthias P Wymann

Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders

5-[4,6-双({3-氧杂-8-氮杂双环[3.2.1]辛-8-基})-1,3,5-三嗪-2-基]-4-(二氟甲基)吡啶-2-胺 (PQR620) 的发现和临床前表征，这是一种用于治疗癌症和神经系统疾病的高效选择性 mTORC1/2 抑制剂

期刊:Journal of Medicinal Chemistry

影响因子:6.8

doi:10.1021/acs.jmedchem.8b01262

Denise Rageot, Thomas Bohnacker, Anna Melone, Jean-Baptiste Langlois, Chiara Borsari, Petra Hillmann, Alexander M Sele, Florent Beaufils, Marketa Zvelebil, Paul Hebeisen, Wolfgang Löscher, John Burke, Doriano Fabbro, Matthias P Wymann

Deconvolution of Buparlisib's mechanism of action defines specific PI3K and tubulin inhibitors for therapeutic intervention

对布帕利西布作用机制的解析，确定了可用于治疗干预的特定PI3K和微管蛋白抑制剂。

期刊:Nature Communications

影响因子:14.7

doi:10.1038/ncomms14683

Thomas Bohnacker ，Andrea E Prota ，Florent Beaufils ，John E Burke ，Anna Melone ，Alison J Inglis ，Denise Rageot ，Alexander M Sele ，Vladimir Cmiljanovic ，Natasa Cmiljanovic ，Katja Bargsten ，Amol Aher ，Anna Akhmanova ，J Fernando Díaz ，Doriano Fabbro ，Marketa Zvelebil ，Roger L Williams ，Michel O Steinmetz ，Matthias P Wymann

发表日期：2017

文献求助收藏

5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology

5-(4,6-二吗啉-1,3,5-三嗪-2-基)-4-(三氟甲基)吡啶-2-胺 (PQR309) 是一种强效、脑渗透性、口服生物利用度高的泛 I 类 PI3K/mTOR 抑制剂，可作为肿瘤学临床候选药物

期刊:Journal of Medicinal Chemistry

影响因子:6.8

doi:10.1021/acs.jmedchem.7b00930

Florent Beaufils, Natasa Cmiljanovic, Vladimir Cmiljanovic, Thomas Bohnacker, Anna Melone, Romina Marone, Eileen Jackson, Xuxiao Zhang, Alexander Sele, Chiara Borsari, Jürgen Mestan, Paul Hebeisen, Petra Hillmann, Bernd Giese, Marketa Zvelebil, Doriano Fabbro, Roger L Williams, Denise Rageot, Matthi

Fluid-phase pinocytosis of native low density lipoprotein promotes murine M-CSF differentiated macrophage foam cell formation

天然低密度脂蛋白的液相胞饮作用促进小鼠 M-CSF 分化的巨噬细胞泡沫细胞形成

期刊:PLoS One

影响因子:2.9

doi:10.1371/journal.pone.0058054

Manoj K Barthwal, Joshua J Anzinger, Qing Xu, Thomas Bohnacker, Matthias P Wymann, Howard S Kruth

Murine bone marrow-derived macrophages differentiated with GM-CSF become foam cells by PI3Kγ-dependent fluid-phase pinocytosis of native LDL

小鼠骨髓来源的巨噬细胞通过 GM-CSF 分化，通过 PI3Kγ 依赖的天然 LDL 液相胞饮作用变成泡沫细胞

期刊:Journal of Lipid Research

影响因子:5

doi:10.1194/jlr.M018887

Joshua J Anzinger, Janet Chang, Qing Xu, Manoj K Barthwal, Thomas Bohnacker, Matthias P Wymann, Howard S Kruth

Rapid, potent, and persistent covalent chemical probes to deconvolute PI3Kα signaling

快速、有效且持久的共价化学探针用于解卷积 PI3Kα 信号

4-(Difluoromethyl)-5-(4-((3 R,5 S)-3,5-dimethylmorpholino)-6-((R)-3-methylmorpholino)-1,3,5-triazin-2-yl)pyridin-2-amine (PQR626), a Potent, Orally Available, and Brain-Penetrant mTOR Inhibitor for the Treatment of Neurological Disorders

4-(二氟甲基)-5-(4-((3 R,5 S)-3,5-二甲基吗啉)-6-((R)-3-甲基吗啉)-1,3,5-三嗪-2-基)吡啶-2-胺 (PQR626)，一种强效、口服、脑渗透性 mTOR 抑制剂，用于治疗神经系统疾病

PI3K γ Regulatory Protein p84 Determines Mast Cell Sensitivity to Ras Inhibition-Moving Towards Cell Specific PI3K Targeting?

PI3Kγ调节蛋白p84决定肥大细胞对Ras抑制的敏感性 - 朝着细胞特异性PI3K靶向发展？

A Conformational Restriction Strategy for the Identification of a Highly Selective Pyrimido-pyrrolo-oxazine mTOR Inhibitor

构象限制策略用于鉴定高选择性嘧啶并吡咯并恶嗪 mTOR 抑制剂

Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders

5-[4,6-双({3-氧杂-8-氮杂双环[3.2.1]辛-8-基})-1,3,5-三嗪-2-基]-4-(二氟甲基)吡啶-2-胺 (PQR620) 的发现和临床前表征，这是一种用于治疗癌症和神经系统疾病的高效选择性 mTORC1/2 抑制剂

Deconvolution of Buparlisib's mechanism of action defines specific PI3K and tubulin inhibitors for therapeutic intervention

对布帕利西布作用机制的解析，确定了可用于治疗干预的特定PI3K和微管蛋白抑制剂。

5-(4,6-Dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine (PQR309), a Potent, Brain-Penetrant, Orally Bioavailable, Pan-Class I PI3K/mTOR Inhibitor as Clinical Candidate in Oncology

5-(4,6-二吗啉-1,3,5-三嗪-2-基)-4-(三氟甲基)吡啶-2-胺 (PQR309) 是一种强效、脑渗透性、口服生物利用度高的泛 I 类 PI3K/mTOR 抑制剂，可作为肿瘤学临床候选药物

Fluid-phase pinocytosis of native low density lipoprotein promotes murine M-CSF differentiated macrophage foam cell formation

天然低密度脂蛋白的液相胞饮作用促进小鼠 M-CSF 分化的巨噬细胞泡沫细胞形成

Murine bone marrow-derived macrophages differentiated with GM-CSF become foam cells by PI3Kγ-dependent fluid-phase pinocytosis of native LDL

小鼠骨髓来源的巨噬细胞通过 GM-CSF 分化，通过 PI3Kγ 依赖的天然 LDL 液相胞饮作用变成泡沫细胞