![](\"http://www.guidetopharmacology.org/GRAC/images_dev27082012/go.jpg\")
1. Bergeron P, Koehler MF, Blackwood EM, Bowman K, Clark K, Firestein R, Kiefer JR, Maskos K, McCleland ML, Orren L et al..(2016)Design and Development of a Series of Potent and Selective Type II Inhibitors of CDK8. 2. Cee VJ, Chen DY, Lee MR, Nicolaou KC.(2009)Cortistatin A is a high-affinity ligand of protein kinases ROCK, CDK8, and CDK11. 3. Dale T, Clarke PA, Esdar C, Waalboer D, Adeniji-Popoola O, Ortiz-Ruiz MJ, Mallinger A, Samant RS, Czodrowski P, Musil D et al..(2015)A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease. 4. Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP.(2011)Comprehensive analysis of kinase inhibitor selectivity. 5. Hatcher JM, Wang ES, Johannessen L, Kwiatkowski N, Sim T, Gray NS.(2018)Development of Highly Potent and Selective Steroidal Inhibitors and Degraders of CDK8. 6. Ito M, Tanaka T, Toita A, Uchiyama N, Kokubo H, Morishita N, Klein MG, Zou H, Murakami M, Kondo M et al..(2018)Discovery of 3-Benzyl-1-( trans-4-((5-cyanopyridin-2-yl)amino)cyclohexyl)-1-arylurea Derivatives as Novel and Selective Cyclin-Dependent Kinase 12 (CDK12) Inhibitors. 7. Mallinger A, Schiemann K, Rink C, Sejberg J, Honey MA, Czodrowski P, Stubbs M, Poeschke O, Busch M, Schneider R et al..(2016)2,8-Disubstituted-1,6-Naphthyridines and 4,6-Disubstituted-Isoquinolines with Potent, Selective Affinity for CDK8/19. 8. Paiva C, Godbersen JC, Soderquist RS, Rowland T, Kilmarx S, Spurgeon SE, Brown JR, Srinivasa SP, Danilov AV.(2015)Cyclin-Dependent Kinase Inhibitor P1446A Induces Apoptosis in a JNK/p38 MAPK-Dependent Manner in Chronic Lymphocytic Leukemia B-Cells. 9. Pelish HE, Liau BB, Nitulescu II, Tangpeerachaikul A, Poss ZC, Da Silva DH, Caruso BT, Arefolov A, Fadeyi O, Christie AL et al..(2015)Mediator kinase inhibition further activates super-enhancer-associated genes in AML. 10. Reichelt A, Bailis JM, Bartberger MD, Yao G, Shu H, Kaller MR, Allen JG, Weidner MF, Keegan KS, Dao JH.(2014)Synthesis and structure-activity relationship of trisubstituted thiazoles as Cdc7 kinase inhibitors. 11. Schneider EV, Böttcher J, Blaesse M, Neumann L, Huber R, Maskos K.(2011)The structure of CDK8/CycC implicates specificity in the CDK/cyclin family and reveals interaction with a deep pocket binder. 12. Wodicka LM, Ciceri P, Davis MI, Hunt JP, Floyd M, Salerno S, Hua XH, Ford JM, Armstrong RC, Zarrinkar PP et al..(2010)Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. CDK8 subfamily: cyclin dependent kinase 8. Last modified on 28/08/2018. Accessed on 18/05/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1980.
行业新闻
- 2016年Discovery Studio学习体验日（免费）
- Horizon Discovery中国总代理
- DiscoverX授权代理商，正品 Discoverx询价
- 默瑞生物取得Discoverx公司的中国代理商
- DiscoverX公司代理生物计划 discoverx美国
- 默瑞生物举办系列DiscoveRX药筛服务讲座
- New Tools for Alzheimer's Disease Research【ABBIOTEC】
- Biomarker Discovery Research Pilot Grants
- Meso Scale Discovery
- Discoverx
- 默瑞生物是美国DiscoveRX公司产品中国独家代理商
- 默瑞生物与Discoverx公司共同举办药物筛选专题讲座
cyclin dependent kinase 8 | CDK8 subfamily | IUPHAR/BPS Guide to PHARMACOLOGY
Annotated and awaiting review. Please contact us if you can help with reviewing. Cell division protein kinase 8|Mediator of RNA polymerase II transcription subunit CDK8|cyclin-dependent kinase 8 Description: CDK8/CYCC in complex with 8-{3-Chloro-5-[4-(1-methyl-1H-pyrazol-4-yl)-phenyl]-pyridin-4-yl}-2,8-diaza-spiro[4.5]decan-1-one. Description: Crystal structure of human CDK8-Cyclin C in complex with cortistatin A. Download all structure-activity data for this target as a CSV file 1. Bergeron P, Koehler MF, Blackwood EM, Bowman K, Clark K, Firestein R, Kiefer JR, Maskos K, McCleland ML, Orren L et al..(2016)Design and Development of a Series of Potent and Selective Type II Inhibitors of CDK8. 2. Cee VJ, Chen DY, Lee MR, Nicolaou KC.(2009)Cortistatin A is a high-affinity ligand of protein kinases ROCK, CDK8, and CDK11. 3. Dale T, Clarke PA, Esdar C, Waalboer D, Adeniji-Popoola O, Ortiz-Ruiz MJ, Mallinger A, Samant RS, Czodrowski P, Musil D et al..(2015)A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease. 4. Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP.(2011)Comprehensive analysis of kinase inhibitor selectivity. 5. Hatcher JM, Wang ES, Johannessen L, Kwiatkowski N, Sim T, Gray NS.(2018)Development of Highly Potent and Selective Steroidal Inhibitors and Degraders of CDK8. 6. Ito M, Tanaka T, Toita A, Uchiyama N, Kokubo H, Morishita N, Klein MG, Zou H, Murakami M, Kondo M et al..(2018)Discovery of 3-Benzyl-1-( trans-4-((5-cyanopyridin-2-yl)amino)cyclohexyl)-1-arylurea Derivatives as Novel and Selective Cyclin-Dependent Kinase 12 (CDK12) Inhibitors. 7. Mallinger A, Schiemann K, Rink C, Sejberg J, Honey MA, Czodrowski P, Stubbs M, Poeschke O, Busch M, Schneider R et al..(2016)2,8-Disubstituted-1,6-Naphthyridines and 4,6-Disubstituted-Isoquinolines with Potent, Selective Affinity for CDK8/19. 8. Paiva C, Godbersen JC, Soderquist RS, Rowland T, Kilmarx S, Spurgeon SE, Brown JR, Srinivasa SP, Danilov AV.(2015)Cyclin-Dependent Kinase Inhibitor P1446A Induces Apoptosis in a JNK/p38 MAPK-Dependent Manner in Chronic Lymphocytic Leukemia B-Cells. 9. Pelish HE, Liau BB, Nitulescu II, Tangpeerachaikul A, Poss ZC, Da Silva DH, Caruso BT, Arefolov A, Fadeyi O, Christie AL et al..(2015)Mediator kinase inhibition further activates super-enhancer-associated genes in AML. 10. Reichelt A, Bailis JM, Bartberger MD, Yao G, Shu H, Kaller MR, Allen JG, Weidner MF, Keegan KS, Dao JH.(2014)Synthesis and structure-activity relationship of trisubstituted thiazoles as Cdc7 kinase inhibitors. 11. Schneider EV, Böttcher J, Blaesse M, Neumann L, Huber R, Maskos K.(2011)The structure of CDK8/CycC implicates specificity in the CDK/cyclin family and reveals interaction with a deep pocket binder. 12. Wodicka LM, Ciceri P, Davis MI, Hunt JP, Floyd M, Salerno S, Hua XH, Ford JM, Armstrong RC, Zarrinkar PP et al..(2010)Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. CDK8 subfamily: cyclin dependent kinase 8. Last modified on 28/08/2018. Accessed on 18/05/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1980.
1. Bergeron P, Koehler MF, Blackwood EM, Bowman K, Clark K, Firestein R, Kiefer JR, Maskos K, McCleland ML, Orren L et al..(2016)Design and Development of a Series of Potent and Selective Type II Inhibitors of CDK8. 2. Cee VJ, Chen DY, Lee MR, Nicolaou KC.(2009)Cortistatin A is a high-affinity ligand of protein kinases ROCK, CDK8, and CDK11. 3. Dale T, Clarke PA, Esdar C, Waalboer D, Adeniji-Popoola O, Ortiz-Ruiz MJ, Mallinger A, Samant RS, Czodrowski P, Musil D et al..(2015)A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease. 4. Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP.(2011)Comprehensive analysis of kinase inhibitor selectivity. 5. Hatcher JM, Wang ES, Johannessen L, Kwiatkowski N, Sim T, Gray NS.(2018)Development of Highly Potent and Selective Steroidal Inhibitors and Degraders of CDK8. 6. Ito M, Tanaka T, Toita A, Uchiyama N, Kokubo H, Morishita N, Klein MG, Zou H, Murakami M, Kondo M et al..(2018)Discovery of 3-Benzyl-1-( trans-4-((5-cyanopyridin-2-yl)amino)cyclohexyl)-1-arylurea Derivatives as Novel and Selective Cyclin-Dependent Kinase 12 (CDK12) Inhibitors. 7. Mallinger A, Schiemann K, Rink C, Sejberg J, Honey MA, Czodrowski P, Stubbs M, Poeschke O, Busch M, Schneider R et al..(2016)2,8-Disubstituted-1,6-Naphthyridines and 4,6-Disubstituted-Isoquinolines with Potent, Selective Affinity for CDK8/19. 8. Paiva C, Godbersen JC, Soderquist RS, Rowland T, Kilmarx S, Spurgeon SE, Brown JR, Srinivasa SP, Danilov AV.(2015)Cyclin-Dependent Kinase Inhibitor P1446A Induces Apoptosis in a JNK/p38 MAPK-Dependent Manner in Chronic Lymphocytic Leukemia B-Cells. 9. Pelish HE, Liau BB, Nitulescu II, Tangpeerachaikul A, Poss ZC, Da Silva DH, Caruso BT, Arefolov A, Fadeyi O, Christie AL et al..(2015)Mediator kinase inhibition further activates super-enhancer-associated genes in AML. 10. Reichelt A, Bailis JM, Bartberger MD, Yao G, Shu H, Kaller MR, Allen JG, Weidner MF, Keegan KS, Dao JH.(2014)Synthesis and structure-activity relationship of trisubstituted thiazoles as Cdc7 kinase inhibitors. 11. Schneider EV, Böttcher J, Blaesse M, Neumann L, Huber R, Maskos K.(2011)The structure of CDK8/CycC implicates specificity in the CDK/cyclin family and reveals interaction with a deep pocket binder. 12. Wodicka LM, Ciceri P, Davis MI, Hunt JP, Floyd M, Salerno S, Hua XH, Ford JM, Armstrong RC, Zarrinkar PP et al..(2010)Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. CDK8 subfamily: cyclin dependent kinase 8. Last modified on 28/08/2018. Accessed on 18/05/2020. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1980.