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

Inhibition of Bromodomain Proteins Enhances Oncolytic HAdVC5 Replication and Efficacy in Pancreatic Ductal Adenocarcinoma (PDAC) Models.

抑制溴结构域蛋白可增强溶瘤HAdVC5在胰腺导管腺癌(PDAC)模型中的复制和疗效

Miao Tizong, Symonds Alistair, Hickman Oliver J, Wu Dongsheng, Wang Ping, Lemoine Nick, Wang Yaohe, Linardopoulos Spiros, Halldén Gunnel

CCT245718, a dual FLT3/Aurora A inhibitor overcomes D835Y-mediated resistance to FLT3 inhibitors in acute myeloid leukaemia cells

CCT245718 是一种双重 FLT3/Aurora A 抑制剂,可克服急性髓系白血病细胞中由 D835Y 介导的 FLT3 抑制剂耐药性。

Tariq, Muhammad Usama; Furqan, Muhammad; Parveen, Hira; Ullah, Rahim; Muddassar, Muhammad; Saleem, Rahman Shah Zaib; Bavetsias, Vassilios; Linardopoulos, Spiros; Faisal, Amir

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。

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

RNAi screen reveals synthetic lethality between cyclin G-associated kinase and FBXW7 by inducing aberrant mitoses.

RNAi 筛选揭示了细胞周期蛋白 G 相关激酶和 FBXW7 之间的合成致死性,这种致死性通过诱导异常有丝分裂而产生

Dolly Saoirse O, Gurden Mark D, Drosopoulos Konstantinos, Clarke Paul, de Bono Johann, Kaye Stan, Workman Paul, Linardopoulos Spiros

Aurora Kinase Inhibitors: Current Status and Outlook

极光激酶抑制剂:现状与展望

Bavetsias, Vassilios; Linardopoulos, Spiros

7-(Pyrazol-4-yl)-3H-imidazo[4,5-b]pyridine-based derivatives for kinase inhibition: Co-crystallisation studies with Aurora-A reveal distinct differences in the orientation of the pyrazole N1-substituent

7-(吡唑-4-基)-3H-咪唑并[4,5-b]吡啶类衍生物用于激酶抑制:与Aurora-A的共结晶研究揭示了吡唑N1取代基取向的明显差异

Bavetsias, Vassilios; Pérez-Fuertes, Yolanda; McIntyre, Patrick J; Atrash, Butrus; Kosmopoulou, Magda; O'Fee, Lisa; Burke, Rosemary; Sun, Chongbo; Faisal, Amir; Bush, Katherine; Avery, Sian; Henley, Alan; Raynaud, Florence I; Linardopoulos, Spiros; Bayliss, Richard; Blagg, Julian

Structure-based design of orally bioavailable 1H-pyrrolo[3,2-c]pyridine inhibitors of mitotic kinase monopolar spindle 1 (MPS1)

基于结构的口服生物利用度高的1H-吡咯并[3,2-c]吡啶类有丝分裂激酶单极纺锤体1 (MPS1) 抑制剂设计

Naud, Sébastien; Westwood, Isaac M; Faisal, Amir; Sheldrake, Peter; Bavetsias, Vassilios; Atrash, Butrus; Cheung, Kwai-Ming J; Liu, Manjuan; Hayes, Angela; Schmitt, Jessica; Wood, Amy; Choi, Vanessa; Boxall, Kathy; Mak, Grace; Gurden, Mark; Valenti, Melanie; de Haven Brandon, Alexis; Henley, Alan; Baker, Ross; McAndrew, Craig; Matijssen, Berry; Burke, Rosemary; Hoelder, Swen; Eccles, Suzanne A; Raynaud, Florence I; Linardopoulos, Spiros; van Montfort, Rob L M; Blagg, Julian

Functional viability profiles of breast cancer.

乳腺癌的功能性生存特征

Brough Rachel, Frankum Jessica R, Sims David, Mackay Alan, Mendes-Pereira Ana M, Bajrami Ilirjana, Costa-Cabral Sara, Rafiq Rumana, Ahmad Amar S, Cerone Maria Antonietta, Natrajan Rachael, Sharpe Rachel, Shiu Kai-Keen, Wetterskog Daniel, Dedes Konstantine J, Lambros Maryou B, Rawjee Teeara, Linardopoulos Spiros, Reis-Filho Jorge S, Turner Nicholas C, Lord Christopher J, Ashworth Alan

The aurora kinase inhibitor CCT137690 downregulates MYCN and sensitizes MYCN-amplified neuroblastoma in vivo

极光激酶抑制剂CCT137690可下调MYCN表达,并在体内增强MYCN扩增型神经母细胞瘤的敏感性。

Faisal, Amir; Vaughan, Lynsey; Bavetsias, Vassilios; Sun, Chongbo; Atrash, Butrus; Avery, Sian; Jamin, Yann; Robinson, Simon P; Workman, Paul; Blagg, Julian; Raynaud, Florence I; Eccles, Suzanne A; Chesler, Louis; Linardopoulos, Spiros

Aurora-A expressing tumour cells are deficient for homology-directed DNA double strand-break repair and sensitive to PARP inhibition

表达Aurora-A的肿瘤细胞缺乏同源定向DNA双链断裂修复能力,并且对PARP抑制剂敏感。

Sourisseau, Tony; Maniotis, Despina; McCarthy, Afshan; Tang, Chan; Lord, Christopher J; Ashworth, Alan; Linardopoulos, Spiros