Small-molecule screen identifies inhibitors of the neuronal K-Cl cotransporter KCC2
作者： E. Delpire , E. Days , L. M. Lewis , D. Mi , K. Kim
关键词: Cotransporter 、 Non-competitive inhibition 、 Biochemistry 、 Symporter 、 Biology 、 Drug discovery 、 Structure–activity relationship 、 Bumetanide 、 Small molecule 、 Loop of Henle
摘要: … Finally, another significant finding of this study is the characterization of inhibitor binding with respect to both external K and Cl ions. To determine the nature of D4 binding to KCC2, we …
harvard.edu
sci-hub.se 参考文章(43)
Peter M. Steinert, Marisa I. Gullino, Bovine epidermal keratin filament assembly invitro Biochemical and Biophysical Research Communications. ,vol. 70, pp. 221- 227 ,(1976) , 10.1016/0006-291X(76)91131-1
Leonard P. Rybak, Ototoxicity of Loop Diuretics Otolaryngologic Clinics of North America. ,vol. 26, pp. 829- 844 ,(1993) , 10.1016/S0030-6665(20)30770-2
Ingram Tt, TODAY'S DRUGS. FRUSEMIDE. BMJ. ,vol. 2, pp. 1640- 1641 ,(1964) , 10.1136/BMJ.2.5425.1638
S Cha, A simple method for derivation of rate equations for enzyme-catalyzed reactions under the rapid equilibrium assumption or combined assumptions of equilibrium and steady state. Journal of Biological Chemistry. ,vol. 243, pp. 820- 825 ,(1968) , 10.1016/S0021-9258(19)81739-8
E. Delpire, Cation-Chloride Cotransporters in Neuronal Communication. Physiology. ,vol. 15, pp. 309- 312 ,(2000) , 10.1152/PHYSIOLOGYONLINE.2000.15.6.309
Irwin H. Segel, Enzyme Kinetics: Behavior and Analysis of Rapid Equilibrium and Steady-State Enzyme Systems ,(1975)
R. Anthony DeFazio, Sotirios Keros, Michael W. Quick, John J. Hablitz, Potassium-Coupled Chloride Cotransport Controls Intracellular Chloride in Rat Neocortical Pyramidal Neurons The Journal of Neuroscience. ,vol. 20, pp. 8069- 8076 ,(2000) , 10.1523/JNEUROSCI.20-21-08069.2000
P A Hannaert, R P Garay, C Nazaret, E J Cragoe, Demonstration of a [K+,Cl-]-cotransport system in human red cells by its sensitivity to [(dihydroindenyl)oxy]alkanoic acids: regulation of cell swelling and distinction from the bumetanide-sensitive [Na+,K+,Cl-]-cotransport system. Molecular Pharmacology. ,vol. 33, pp. 696- 701 ,(1988)
Eric Delpire, Jianming Lu, Roger England, Christopher Dull, Tina Thorne, Deafness and imbalance associated with inactivation of the secretory Na-K-2Cl co-transporter Nature Genetics. ,vol. 22, pp. 192- 195 ,(1999) , 10.1038/9713
H. R. Pathak, F. Weissinger, M. Terunuma, G. C. Carlson, F.-C. Hsu, S. J. Moss, D. A. Coulter, Disrupted dentate granule cell chloride regulation enhances synaptic excitability during development of temporal lobe epilepsy. The Journal of Neuroscience. ,vol. 27, pp. 14012- 14022 ,(2007) , 10.1523/JNEUROSCI.4390-07.2007