未登录 Cephalosporins are potent SARS-CoV-2 main protease inhibitors 头孢菌素是SARS-CoV-2主蛋白酶的有效抑制剂 Muntean, Dorian-Gabriel; Treyde, Wojtek; Laczi, Dora; Laidlaw, Stephen M.; Salah, Eidarus; Choudhry, Hani; Carroll, Miles W.; Duarte, Fernanda; Schofield, Christopher J.; Brewitz, Lennart 分享 收藏
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Silaproline-bearing nirmatrelvir derivatives are potent inhibitors of the SARS-CoV-2 main protease highlighting the value of silicon-derivatives in structure-activity-relationship studies 含Silaproline的Nirmatrelvir衍生物是SARS-CoV-2主要蛋白酶的强效抑制剂，突显了硅衍生物在构效关系研究中的价值。 Laczi, Dora; Huaman, Sofia Schonbauer; Andrews-Clark, Taylah; Laidlaw, Stephen M.; Salah, Eidarus; Dumjahn, Leo; Lukacik, Petra; Choudhry, Hani; Walsh, Martin A.; Carroll, Miles W.; Schofield, Christopher J.; Brewitz, Lennart 分享 收藏
Derivatives of the Clinically Used HIF Prolyl Hydroxylase Inhibitor Desidustat Are Efficient Inhibitors of Human γ-Butyrobetaine Hydroxylase 临床使用的HIF脯氨酰羟化酶抑制剂Desidustat的衍生物是高效的人γ-丁基丁二酸羟化酶抑制剂 Corner, Thomas P.; Tumber, Anthony; Salah, Eidarus; Jabbary, Mohammadparsa; Nakashima, Yu; Schnaubelt, Lara I.; Basak, Shyam; Alshref, Faisal M.; Brewitz, Lennart; Schofield, Christopher J. 分享 收藏
RaPID discovery of cell-permeable helical peptide inhibitors con-taining cyclic β-amino acids against SARS-CoV-2 main protease 快速发现靶向SARS-CoV-2主蛋白酶的含环β-氨基酸的细胞渗透性螺旋肽抑制剂 Kawai, Marina; Malla, Tika R.; Chan, H. T. Henry; Tumber, Anthony; Brewitz, Lennart; Salah, Eidarus; Katoh, Takayuki; Kawamura, Akane; Schofield, Christopher J.; Duarte, Fernanda; Suga, Hiroaki 分享 收藏
JmjC catalysed histone H2a N-methyl arginine demethylation and C4-arginine hydroxylation reveals importance of sequence-reactivity relationships Bonnici, Joanna; Oueini, Razanne; Salah, Eidarus; Johansson, Catrine; Pires, Elisabete; Abboud, Martine; Dawber, Robert S.; Tumber, Anthony; Rabe, Patrick; Sarac, Hilal; Schofield, Christopher J.; Kawamura, Akane 分享 收藏
Crystallographic and Selectivity Studies on the Approved HIF Prolyl Hydroxylase Inhibitors Desidustat and Enarodustat 批准的HIF脯氨酰羟化酶抑制剂Desidustat和Enarodustat的晶体学和选择性研究 Corner, Thomas P.; Salah, Eidarus; Tumber, Anthony; Kaur, Samanpreet; Nakashima, Yu; Allen, Mark D.; Schnaubelt, Lara I.; Fiorini, Giorgia; Brewitz, Lennart; Schofield, Christopher J. 分享 收藏
A Small-Molecule Inhibitor of Factor Inhibiting HIF Binding to a Tyrosine-Flip Pocket for the Treatment of Obesity Wu, Yue; Chen, Yafen; Corner, Thomas P.; Nakashima, Yu; Salah, Eidarus; Li, Zhihong; Zhang, Linjian; Yang, Le; Tumber, Anthony; Sun, Zhuoli; Wen, Yukang; Zhong, Ailin; Yang, Fulai; Li, Xiang; Zhang, Zhihong; Schofield, Christopher J.; Zhang, Xiaojin 分享 收藏
The selective prolyl hydroxylase inhibitor IOX5 stabilizes HIF-1α and compromises development and progression of acute myeloid leukemia Lawson, Hannah; Holt-Martyn, James P.; Dembitz, Vilma; Kabayama, Yuka; Wang, Lydia M.; Bellani, Aarushi; Atwal, Samanpreet; Saffoon, Nadia; Durko, Jozef; van de Lagemaat, Louie N.; De Pace, Azzura L.; Tumber, Anthony; Corner, Thomas; Salah, Eidarus; Arndt, Christine; Brewitz, Lennart; Bowen, Matthew; Dubusse, Louis; George, Derek; Allen, Lewis; Guitart, Amelie V.; Fung, Tsz Kan; So, Chi Wai Eric; Schwaller, Juerg; Gallipoli, Paolo; O'Carroll, Donal; Schofield, Christopher J.; Kranc, Kamil R. 分享 收藏
Cyclic β2,3-amino acids improve the serum stability of macrocyclic peptide inhibitors targeting the SARS-CoV-2 main protease Miura, Takashi; Malla, Tika R.; Brewitz, Lennart; Tumber, Anthony; Salah, Eidarus; Lee, Kang Ju; Terasaka, Naohiro; Owen, C. David; Strain-Damerell, Claire; Lukacik, Petra; Walsh, Martin A.; Kawamura, Akane; Schofield, Christopher J.; Katoh, Takayuki; Suga, Hiroaki 分享 收藏
Selective targeting of human TET1 by cyclic peptide inhibitors: Insights from biochemical profiling Simelis, Klemensas; Sarac, Hilal; Salah, Eidarus; Nishio, Kosuke; McAllister, Tom E.; Corner, Thomas P.; Tumber, Anthony; Belle, Roman; Schofield, Christopher J.; Suga, Hiroaki; Kawamura, Akane 分享 收藏
Focused Screening Identifies Different Sensitivities of Human TET Oxygenases to the Oncometabolite 2-Hydroxyglutarate 聚焦筛选确定了人类TET加氧酶对单代谢物2-羟基戊二酸的不同敏感性 Belle, Roman; Sarac, Hilal; Salah, Eidarus; Bhushan, Bhaskar; Szykowska, Aleksandra; Roper, Grace; Tumber, Anthony; Kriaucionis, Skirmantas; Burgess-Brown, Nicola; Schofield, Christopher J.; Brown, Tom; Kawamura, Akane 分享 收藏
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5-Substituted Pyridine-2,4-dicarboxylate Derivatives Have Potential for Selective Inhibition of Human Jumonji-C Domain-Containing Protein 5 Brewitz, Lennart; Nakashima, Yu; Piasecka, Sonia K.; Salah, Eidarus; Fletcher, Sally C.; Tumber, Anthony; Corner, Thomas P.; Kennedy, Tristan J.; Fiorini, Giorgia; Thalhammer, Armin; Christensen, Kirsten E.; Coleman, Mathew L.; Schofield, Christopher J. 分享 收藏
In vitro selection of macrocyclic peptide inhibitors containing cyclic ?2,4-amino acids targeting the SARS-CoV-2 main protease Miura, Takashi; Malla, Tika R. R.; Owen, C. David; Tumber, Anthony; Brewitz, Lennart; McDonough, Michael A. A.; Salah, Eidarus; Terasaka, Naohiro; Katoh, Takayuki; Lukacik, Petra; Strain-Damerell, Claire; Mikolajek, Halina; Walsh, Martin A. A.; Kawamura, Akane; Schofield, Christopher J. J.; Suga, Hiroaki 分享 收藏
Alkyne Derivatives of SARS-CoV-2 Main Protease Inhibitors Including Nirmatrelvir Inhibit by Reacting Covalently with the Nucleophilic Cysteine Brewitz, Lennart; Dumjahn, Leo; Zhao, Yilin; Owen, C. David; Laidlaw, Stephen M.; Malla, Tika R.; Nguyen, Dung; Lukacik, Petra; Salah, Eidarus; Crawshaw, Adam D.; Warren, Anna J.; Trincao, Jose; Strain-Damerell, Claire; Carroll, Miles W.; Walsh, Martin A.; Schofield, Christopher J. 分享 收藏
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