Coupling of agonist binding to channel gating in the GABA(A) receptor

Neurotransmitters such as acetylcholine and GABA (gamma-aminobutyric acid) mediate rapid synaptic transmission by activating receptors belonging to the gene superfamily of ligand-gated ion channels (LGICs). These channels are pentameric proteins that function as signal transducers, converting chemical messages into electrical signals. Neurotransmitters activate LGICs by interacting with a ligand-binding site, triggering a conformational change in the protein that results in the opening of an ion channel. This process, which is known as 'gating', occurs rapidly and reversibly, but the molecular rearrangements involved are not well understood. Here we show that optimal gating in the GABA(A) receptor, a member of the LGIC superfamily, is dependent on electrostatic interactions between the negatively charged Asp 57 and Asp 149 residues in extracellular loops 2 and 7, and the positively charged Lys 279 residue in the transmembrane 2-3 linker region of the alpha1-subunit. During gating, Asp 149 and Lys 279 seem to move closer to one another, providing a potential mechanism for the coupling of ligand binding to opening of the ion channel.     

一个新的单调类定理

定义了集类的ｗ类的概念,给出了ｗ类的单调类定理．     

一类新的多总线结构

研究每个处理挂在两条总线上的多总线结构的容错设计问题,提出了一类新的具有较佳(最佳)容错性和可扩充性的多总线结构.     

A new class of variational equation problems

Abstract Applying an analysis method to a group of multivariable equations, a new class of variational equations are proved. Thismethod is more concise and more direct than the others. This result can be applied to some stochastic control models.     

A new class of antimagic join graphs

A labeling/of a graph G is a bijection from its edge set E(G) to the set {1,2,…,|E(G)|},which is antimagic if for any distinct vertices x anAy,the sum of the labels on edges incident to x is different from the sum of the labels on edges incident to y.A graph G is antimagic if G has an f which is antimagic.Hartsfield and Ringel conjectured in 1990 that every connected graph other than K_2 is antimagic.In this paper,we show that if G_1 is an m-vertex graph with maximum degree at most 6r+l,and G_2 is an n-vertex(2r)-regular graph(m≥n≥3),then the join graph G_1 v G_2 is antimagic.     

图的一类新双变量色多项式

根据Klaus Dohmen等提出的图的新双变量色多项式概念,探究了一般图关于此定义的减边公式,利用它反复迭代后可以方便地求得任何图的新双变量色多项式,还利用它深入探讨了一些特殊图的新双变量色多项式公式.同时还探究了运用包含等偏序关系,利用M(o)bius反演法和“格子剖分”法求得图的新双变量色多项式.最后探讨了共点图的新双变量色多项式公式以及图的顶点和边与色多项式的关系.     

A new class of angiotensin-converting enzyme inhibitors

Much current attention focuses on the renin-angiotensin system in relation to mechanisms controlling blood pressure and renal function. Recent demonstrations (ref. 1, ref. 2 and refs therein) that angiotensin-converting enzyme inhibitors show promising clinical antihypertensive properties have been of particular interest. We now report on the design of a novel series of substituted N-carboxymethyl-dipeptides which are active in inhibiting angiotensin-converting enzyme at nanomolar levels. We suggest that these compounds are transition-state inhibitors and that extensions of this design to other metalloendopeptidases merit further study.     

一类新的记忆梯度法

提出了一类新的求解无约束优化问题的记忆梯度法,在较弱条件下证明了该方法的全局收敛性和线性收敛速率.该算法无需任何线搜索而具有充分下降性,且搜索方向自适应在一个信赖域范围之内;该方法继承了著名PRP方法的一个主要性质:当步长很小时,搜索方向靠近于最速下降方向,避免了连续小步长的产生.初步的数值实验结果表明该方法是有效的.     

狄拉克方程的新一类解

研究了位于由两对双曲柱面构成的波导管电磁场里的单电子的性质,得到了单电子在场中狄拉克方程的新一类精确解;计算了极化算符的本征函数。结果表明,自旋系数可用恒定极化算符的本征值确定。这种方法可描述任意类型波导管里的电流磁化。     

一类新的上可嵌入图

图G的CB一划分是指:G的一个顶点划分{V1,V2,…,Vn},使得每个G[Vi]为多重完全二部图(1≤i≤n).结合图的顶点CB-划分条件,确定了一类顶点的度在moalulo 4下值为0,1或3的上可嵌入图类,较完整地刻画了这类图的上可嵌入情况.     

A new class of homoserine lactone quorum-sensing signals

Quorum sensing is a term used to describe cell-to-cell communication that allows cell-density-dependent gene expression. Many bacteria use acyl-homoserine lactone (acyl-HSL) synthases to generate fatty acyl-HSL quorum-sensing signals, which function with signal receptors to control expression of specific genes. The fatty acyl group is derived from fatty acid biosynthesis and provides signal specificity, but the variety of signals is limited. Here we show that the photosynthetic bacterium Rhodopseudomonas palustris uses an acyl-HSL synthase to produce p-coumaroyl-HSL by using environmental p-coumaric acid rather than fatty acids from cellular pools. The bacterium has a signal receptor with homology to fatty acyl-HSL receptors that responds to p-coumaroyl-HSL to regulate global gene expression. We also found that p-coumaroyl-HSL is made by other bacteria including Bradyrhizobium sp. and Silicibacter pomeroyi. This discovery extends the range of possibilities for acyl-HSL quorum sensing and raises fundamental questions about quorum sensing within the context of environmental signalling.     

一类新的Salagean-type调和单叶函数

通过定义一类新的Salagean-type调和单叶函数,得到了该函数类的一个充分条件和偏差定理.     

基于有理Bernstein函数类的一类有理Bezier曲线

从Bernstein多项式和参数有理变换出发,构造了一类新型的有理调配函数—有理Bernstein函数类,讨论了它的分析性质;运用该函数类给出了一类有理Bezier曲线的生成方法,研究了一类有理Bezier曲线的几何性质和几种实用的有理Bezier曲线并给出了数值例子。     

A new class of anthelmintics effective against drug-resistant nematodes

Anthelmintic resistance in human and animal pathogenic helminths has been spreading in prevalence and severity to a point where multidrug resistance against the three major classes of anthelmintics--the benzimidazoles, imidazothiazoles and macrocyclic lactones--has become a global phenomenon in gastrointestinal nematodes of farm animals. Hence, there is an urgent need for an anthelmintic with a new mode of action. Here we report the discovery of the amino-acetonitrile derivatives (AADs) as a new chemical class of synthetic anthelmintics and describe the development of drug candidates that are efficacious against various species of livestock-pathogenic nematodes. These drug candidates seem to have a novel mode of action involving a unique, nematode-specific clade of acetylcholine receptor subunits. The AADs are well tolerated and of low toxicity to mammals, and overcome existing resistances to the currently available anthelmintics.     

一类新的含反常积分的非线性不等式

对满足一类新的含反常积分非线性不等式的有界函数建立了先验逐点估计．这类含反常积分的非线性不等式与笔者以前证明的某些非线性积分不等式密切相关．     

一类新的随机三项共轭梯度算法

针对经验风险最小化(ERM)这一无约束优化问题,使用随机优化算法.为了提高损失函数值的下降速度,考虑三项共轭梯度法的优点,提出一类新的随机三项共轭梯度算法.并将新算法与经典的随机梯度下降(SGD)类算法和已有的随机共轭梯度算法CGVR进行比较,数值结果表明新算法比SGD类算法在求解ERM问题上更有优势.