Kinase drug discovery 20 years after imatinib: progress and future directions.
Kinase drug discovery 20 years after imatinib: progress and future directions.
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伊马替尼20年后的激酶药物发现：进步和未来方向。
DOI：
10.1038/s41573-021-00195-4
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发表时间：
2021-07
期刊：
影响因子：
--
通讯作者：
Jänne PA
中科院分区：
文献类型：
--
作者：
Cohen P;Cross D;Jänne PA
蛋白激酶调节细胞生命的几乎所有方面，其表达的改变或基因的突变会导致癌症和其他疾病。在这里，我们回顾了过去 20 年在提高蛋白质和脂质激酶小分子抑制剂的效力和特异性方面取得的显着进展，自 2001 年伊马替尼获得批准以来，已有 70 多种新药获得批准。这些化合物对我们现在治疗癌症和非癌症疾病的方式产生了重大影响。我们讨论如何应对激酶抑制剂耐药性的挑战以及激酶药物发现的未来。自第一个小分子蛋白激酶抑制剂伊马替尼获得 FDA 批准以来已经过去了二十年。在这里，科恩等人。回顾提高小分子蛋白激酶抑制剂的效力和特异性方面的进展，并评估克服耐药性挑战的方法。讨论了这些化合物在癌症和其他疾病中的应用，以及该领域的未来方向。
Protein kinases regulate nearly all aspects of cell life, and alterations in their expression, or mutations in their genes, cause cancer and other diseases. Here, we review the remarkable progress made over the past 20 years in improving the potency and specificity of small-molecule inhibitors of protein and lipid kinases, resulting in the approval of more than 70 new drugs since imatinib was approved in 2001. These compounds have had a significant impact on the way in which we now treat cancers and non-cancerous conditions. We discuss how the challenge of drug resistance to kinase inhibitors is being met and the future of kinase drug discovery. Twenty years have passed since the first small-molecule protein kinase inhibitor, imatinib, gained FDA approval. Here, Cohen et al. review advances in improving the potency and specificity of small-molecule protein kinase inhibitors and assess approaches to overcome the challenge of drug resistance. Applications of these compounds in cancers and other disorders, as well as future directions in the field, are discussed.
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影响因子：
50.3
作者：
Berger AH;Brooks AN;Wu X;Shrestha Y;Chouinard C;Piccioni F;Bagul M;Kamburov A;Imielinski M;Hogstrom L;Zhu C;Yang X;Pantel S;Sakai R;Watson J;Kaplan N;Campbell JD;Singh S;Root DE;Narayan R;Natoli T;Lahr DL;Tirosh I;Tamayo P;Getz G;Wong B;Doench J;Subramanian A;Golub TR;Meyerson M;Boehm JS
通讯作者：
Boehm JS
危及生命的Covid-19患者中针对I型IFN的自身抗体。
DOI：
10.1126/science.abd4585
发表时间：
2020-10-23
期刊：
Science (New York, N.Y.)
影响因子：
--
作者：
Bastard P;Rosen LB;Zhang Q;Michailidis E;Hoffmann HH;Zhang Y;Dorgham K;Philippot Q;Rosain J;Béziat V;Manry J;Shaw E;Haljasmägi L;Peterson P;Lorenzo L;Bizien L;Trouillet-Assant S;Dobbs K;de Jesus AA;Belot A;Kallaste A;Catherinot E;Tandjaoui-Lambiotte Y;Le Pen J;Kerner G;Bigio B;Seeleuthner Y;Yang R;Bolze A;Spaan AN;Delmonte OM;Abers MS;Aiuti A;Casari G;Lampasona V;Piemonti L;Ciceri F;Bilguvar K;Lifton RP;Vasse M;Smadja DM;Migaud M;Hadjadj J;Terrier B;Duffy D;Quintana-Murci L;van de Beek D;Roussel L;Vinh DC;Tangye SG;Haerynck F;Dalmau D;Martinez-Picado J;Brodin P;Nussenzweig MC;Boisson-Dupuis S;Rodríguez-Gallego C;Vogt G;Mogensen TH;Oler AJ;Gu J;Burbelo PD;Cohen JI;Biondi A;Bettini LR;D'Angio M;Bonfanti P;Rossignol P;Mayaux J;Rieux-Laucat F;Husebye ES;Fusco F;Ursini MV;Imberti L;Sottini A;Paghera S;Quiros-Roldan E;Rossi C;Castagnoli R;Montagna D;Licari A;Marseglia GL;Duval X;Ghosn J;HGID Lab;NIAID-USUHS Immune Response to COVID Group;COVID Clinicians;COVID-STORM Clinicians;Imagine COVID Group;French COVID Cohort Study Group;Milieu Intérieur Consortium;CoV-Contact Cohort;Amsterdam UMC Covid-19 Biobank;COVID Human Genetic Effort;Tsang JS;Goldbach-Mansky R;Kisand K;Lionakis MS;Puel A;Zhang SY;Holland SM;Gorochov G;Jouanguy E;Rice CM;Cobat A;Notarangelo LD;Abel L;Su HC;Casanova JL
通讯作者：
Casanova JL
影响因子：
120.1
作者：
Bukowski, Ronald M.;Yasothan, Uma;Kirkpatrick, Peter
通讯作者：
Kirkpatrick, Peter
影响因子：
7.5
作者：
Cohen, Philip
通讯作者：
Cohen, Philip
影响因子：
11.2
作者：
Burslem, George M.;Schultz, Anna Reister;Crews, Craig M.
通讯作者：
Crews, Craig M.