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

Unhooking the Hook: Optimization of the Aurora A Targeting PROTAC JB170 to CCT400028, an In Vitro Degrader Chemical Probe

解开钩子：优化 Aurora A 靶向 PROTAC JB170 至 CCT400028，一种体外降解化学探针

期刊:Journal of Medicinal Chemistry
影响因子:6.8
doi:10.1021/acs.jmedchem.5c03024
O'Hanlon, Jack A; Gutsche, Katrin; Müller, Juliane Elisabeth; Ranjan Prusty, Nihar; Mirza, Amin; Roumeliotis, Theodoros I; Yang, Hengzhang; Stubbs, Mark; Hallett, Stephen T; Eing, Lorenz; McAndrew, Peter Craig; Choudhary, Jyoti Sharma; Le Bihan, Yann-Vaï; Caldwell, John; van Montfort, Rob L M; Workman, Paul; Wolf, Elmar; Newton, Gary K; Evans, Lindsay E
Aurora A
发表日期：2026
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Human DEAH-box helicase 8 regulates HSF1-mediated stress response and cancer-associated pre-mRNA splicing in tumour cells.

人类 DEAH 盒解旋酶 8 调节 HSF1 介导的应激反应和肿瘤细胞中与癌症相关的 pre-mRNA 剪接。

期刊:NAR Cancer
影响因子:3.2
doi:10.1093/narcan/zcag008
Tall Jennifer R, Te Poele Robert, Vasile Alexandra, Ramagiri Pradeep, Campbell James, Davies Caitlin R, Powers Marissa V, Roe Toby, Sankaran Deivendran, Wang Hannah, Mitsopoulos Konstantinos, Al-Lazikani Bissan, van Montfort Rob L M, de Billy Emmanuel, Workman Paul, Clarke Paul A
Human
细胞生物学
肿瘤细胞
HSF1
发表日期：2026
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Discovery of first-in-class inhibitors of the TRF1:TIN2 protein:protein interaction by fragment screening.

通过片段筛选发现TRF1:TIN2蛋白相互作用的首创抑制剂。

期刊:Scientific Reports
影响因子:3.9
doi:10.1038/s41598-025-23858-3
Casale Giacomo, Liu Manjuan, Le Bihan Yann-Vaï, Inian Oviya, Stammers Ellie, Caldwell John, van Montfort Rob L M, Collins Ian, Guettler Sebastian
发表日期：2025
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Specific radiation damage to halogenated inhibitors and ligands in protein-ligand crystal structures

蛋白质-配体晶体结构中卤代抑制剂和配体的特定辐射损伤

期刊:
影响因子:
doi:10.1107/S1600576724010549
Rodrigues, Matthew J; Cabry, Marc; Collie, Gavin; Carter, Michael; McAndrew, Craig; Owen, Robin L; Bellenie, Benjamin R; Le Bihan, Yann-Vaï; van Montfort, Rob L M
辐射损伤
毒理研究
发表日期：2024
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Discovery of an In Vivo Chemical Probe for BCL6 Inhibition by Optimization of Tricyclic Quinolinones

通过优化三环喹啉酮发现一种用于抑制BCL6的体内化学探针

期刊:Journal of Medicinal Chemistry
影响因子:6.8
doi:10.1021/acs.jmedchem.3c00155
Harnden, Alice C; Davis, Owen A; Box, Gary M; Hayes, Angela; Johnson, Louise D; Henley, Alan T; de Haven Brandon, Alexis K; Valenti, Melanie; Cheung, Kwai-Ming J; Brennan, Alfie; Huckvale, Rosemary; Pierrat, Olivier A; Talbot, Rachel; Bright, Michael D; Akpinar, Hafize Aysin; Miller, Daniel S J; Tarantino, Dalia; Gowan, Sharon; de Klerk, Selby; McAndrew, Peter Craig; Le Bihan, Yann-Vaï; Meniconi, Mirco; Burke, Rosemary; Kirkin, Vladimir; van Montfort, Rob L M; Raynaud, Florence I; Rossanese, Olivia W; Bellenie, Benjamin R; Hoelder, Swen
BCL6
发表日期：2023
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Determination of Ligand-Binding Affinity (K(d)) Using Transverse Relaxation Rate (R(2)) in the Ligand-Observed (1)H NMR Experiment and Applications to Fragment-Based Drug Discovery

利用配体观测的（1）H NMR实验中的横向弛豫速率（R（2））测定配体结合亲和力（K（d））及其在基于片段的药物发现中的应用

期刊:Journal of Medicinal Chemistry
影响因子:6.8
doi:10.1021/acs.jmedchem.3c00758
Liu, Manjuan; Mirza, Amin; McAndrew, P Craig; Thapaliya, Arjun; Pierrat, Olivier A; Stubbs, Mark; Hahner, Tamas; Chessum, Nicola E A; Innocenti, Paolo; Caldwell, John; Cheeseman, Matthew D; Bellenie, Benjamin R; van Montfort, Rob L M; Newton, Gary K; Burke, Rosemary; Collins, Ian; Hoelder, Swen
发表日期：2023
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Optimizing Shape Complementarity Enables the Discovery of Potent Tricyclic BCL6 Inhibitors

优化形状互补性有助于发现高效的三环BCL6抑制剂

期刊:Journal of Medicinal Chemistry
影响因子:6.8
doi:10.1021/acs.jmedchem.1c02174
Davis, Owen A; Cheung, Kwai-Ming J; Brennan, Alfie; Lloyd, Matthew G; Rodrigues, Matthew J; Pierrat, Olivier A; Collie, Gavin W; Le Bihan, Yann-Vaï; Huckvale, Rosemary; Harnden, Alice C; Varela, Ana; Bright, Michael D; Eve, Paul; Hayes, Angela; Henley, Alan T; Carter, Michael D; McAndrew, P Craig; Talbot, Rachel; Burke, Rosemary; van Montfort, Rob L M; Raynaud, Florence I; Rossanese, Olivia W; Meniconi, Mirco; Bellenie, Benjamin R; Hoelder, Swen
BCL6
发表日期：2022
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Improved Binding Affinity and Pharmacokinetics Enable Sustained Degradation of BCL6 In Vivo

提高结合亲和力和药代动力学可实现体内BCL6的持续降解

期刊:Journal of Medicinal Chemistry
影响因子:6.8
doi:10.1021/acs.jmedchem.1c02175
Huckvale, Rosemary; Harnden, Alice C; Cheung, Kwai-Ming J; Pierrat, Olivier A; Talbot, Rachel; Box, Gary M; Henley, Alan T; de Haven Brandon, Alexis K; Hallsworth, Albert E; Bright, Michael D; Akpinar, Hafize Aysin; Miller, Daniel S J; Tarantino, Dalia; Gowan, Sharon; Hayes, Angela; Gunnell, Emma A; Brennan, Alfie; Davis, Owen A; Johnson, Louise D; de Klerk, Selby; McAndrew, Craig; Le Bihan, Yann-Vaï; Meniconi, Mirco; Burke, Rosemary; Kirkin, Vladimir; van Montfort, Rob L M; Raynaud, Florence I; Rossanese, Olivia W; Bellenie, Benjamin R; Hoelder, Swen
BCL6
发表日期：2022
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Into Deep Water: Optimizing BCL6 Inhibitors by Growing into a Solvated Pocket

深入探索：通过向溶剂化口袋生长来优化 BCL6 抑制剂

期刊:Journal of Medicinal Chemistry
影响因子:6.8
doi:10.1021/acs.jmedchem.1c00946
Lloyd, Matthew G; Huckvale, Rosemary; Cheung, Kwai-Ming J; Rodrigues, Matthew J; Collie, Gavin W; Pierrat, Olivier A; Gatti Iou, Mahad; Carter, Michael; Davis, Owen A; McAndrew, P Craig; Gunnell, Emma; Le Bihan, Yann-Vaï; Talbot, Rachel; Henley, Alan T; Johnson, Louise D; Hayes, Angela; Bright, Michael D; Raynaud, Florence I; Meniconi, Mirco; Burke, Rosemary; van Montfort, Rob L M; Rossanese, Olivia W; Bellenie, Benjamin R; Hoelder, Swen
BCL6
发表日期：2021
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Introduction of a Methyl Group Curbs Metabolism of Pyrido[3,4- d]pyrimidine Monopolar Spindle 1 (MPS1) Inhibitors and Enables the Discovery of the Phase 1 Clinical Candidate N(2)-(2-Ethoxy-4-(4-methyl-4 H-1,2,4-triazol-3-yl)phenyl)-6-methyl- N(8)-neopentylpyrido[3,4- d]pyrimidine-2,8-diamine (BOS172722)

引入甲基可抑制吡啶并[3,4-d]嘧啶单极纺锤体1 (MPS1) 抑制剂的代谢，并促成了 1 期临床候选药物 N(2)-(2-乙氧基-4-(4-甲基-4H-1,2,4-三唑-3-基)苯基)-6-甲基-N(8)-新戊基吡啶并[3,4-d]嘧啶-2,8-二胺 (BOS172722) 的发现。

期刊:Journal of Medicinal Chemistry
影响因子:6.8
doi:10.1021/acs.jmedchem.8b00690
Woodward, Hannah L; Innocenti, Paolo; Cheung, Kwai-Ming J; Hayes, Angela; Roberts, Jennie; Henley, Alan T; Faisal, Amir; Mak, Grace Wing-Yan; Box, Gary; Westwood, Isaac M; Cronin, Nora; Carter, Michael; Valenti, Melanie; De Haven Brandon, Alexis; O'Fee, Lisa; Saville, Harry; Schmitt, Jessica; Burke, Rosemary; Broccatelli, Fabio; van Montfort, Rob L M; Raynaud, Florence I; Eccles, Suzanne A; Linardopoulos, Spiros; Blagg, Julian; Hoelder, Swen
代谢
发表日期：2018
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