G-Protein Coupled Receptors in Human Sperm: An In Silico Approach to Identify Potential Modulatory Targets

G protein-coupled receptors (GPCRs) are involved in several physiological processes, and they represent the largest family of drug targets to date. However, the presence and function of these receptors are poorly described in human spermatozoa. Here, we aimed to identify and characterize the GPCRs present in human spermatozoa and perform an in silico analysis to understand their potential role in sperm functions. The human sperm proteome, including proteomic studies in which the criteria used for protein identification was set as <5% FDR and a minimum of 2 peptides match per protein, was crossed with the list of GPCRs retrieved from GLASS and GPCRdb databases. A total of 71 GPCRs were identified in human spermatozoa, of which 7 had selective expression in male tissues (epididymis, seminal vesicles, and testis), and 9 were associated with male infertility defects in mice. Additionally, ADRA2A, AGTR1, AGTR2, FZD3, and GLP1R were already associated with sperm-specific functions such as sperm capacitation, acrosome reaction, and motility, representing potential targets to modulate and improve sperm function. Finally, the protein-protein interaction network for the human sperm GPCRs revealed that 24 GPCRs interact with 49 proteins involved in crucial processes for sperm formation, maturation, and fertilization. This approach allowed the identification of 8 relevant GPCRs (ADGRE5, ADGRL2, GLP1R, AGTR2, CELSR2, FZD3, CELSR3, and GABBR1) present in human spermatozoa that can be the subject of further investigation to be used even as potential modulatory targets to treat male infertility or to develop new non-hormonal male contraceptives.     

不同细胞质雄性不育小麦阳离子过氧化物酶和IAA-氧化酶活性的研究

选用Ｃ－型、Ｍ－型、Ｍｔ２－型、Ｇ－型４个不同类型的细胞质雄性不育（ＣｙｔｏｐｌａｓｍｉｃＭａｌｅＳｔｅｒｉｌｉｔｙ，ＣＭＳ）小麦为材料，以其保持系中国春作对照，用低ｐＨ值（ｐＨ４．６）提取酶液，对分蘖期、拔节期、孕穗期和抽穗期叶、穗和花药中的阳离子过氧化物酶和ＩＡＡ－氧化酶活性进行了研究．结果表明：分蘖期和拔节期不育系叶中阳离子过氧化物酶和ＩＡＡ－氧化酶活性都比保持系略低；抽穗期叶、穗和花药中不育系两种酶的活性都比保持系高．故认为，小麦植株随着发育进程，其体内尤其是穗和花药中阳离子过氧化物酶和ＩＡＡ－氧化酶活性增强，导致ＩＡＡ亏缺，引起雄性不育的发生     

细胞质雄性不育小麦抽穗期阳离子过氧化物酶同工酶的研究

选用Ｃ－型、Ｇ－型、Ｍ－型、Ｍｔ２－型４种细胞质类型的７个不育系小麦为材料，以其保持系中国春作对照，用低ｐＨ值（ｐＨ４．６）提取酶液，采用正极和负极向垂直板聚丙烯酸胺凝胶电泳，对抽穗期时、穗和花药的阳离子过氧化物酶同工酶进行了研究．结果表明：花药中不育系和保持系之间无论是正极向还是负极向的过氧化物酶差异均显著．负极向的过氧化物酶不育系比保持系多了两条带且酶带显色更深，反映其酶活性更强；正极向的过氧化物酶中，不育系也比保持系多了两条带，但没有保持系特有的４条酶带（Ａ７～Ａ１０），并且快带也只有一条．花药中阳离子过氧化物酶同工酶谱带数增多，活性增强，可能是小麦雄性不育发生的原因之一．     

（无芒山羊草）中国春等小麦雄性不育系小孢子败育及育性恢复的初步研究

研究了（无芒山羊草）中国春、（尾状山羊草）中国春和（拟斯卑尔脱山羊草）中国春三种小麦细胞质雄性不育系（ｃｖｔｏｐｌａｓｍｉｃｍａｌｅｓｔｅｒｉｌｅｌｉｎｅ，ＣＭＳ）小孢子败育特点及育性恢复特性，结果表明：１．（无芒山羊草）中国春ＣＭＳ小孢子败育主要发生在单核晚期和二核期，以园败为主，园败频率为７５．９％；２·（尾状山羊单）中国春ＣＭＳ和（拟斯卑尔脱山羊草）中国春ＣＭＳ小孢子败育主要发生在单核晚期，以典败为主，典败频率分别为８０．５％和９２．５％；３．上述三种小麦ＣＭＳ易恢性不同，其中（拟斯卑尔脱山羊草）中国春ＣＭＳ易恢性相对较好，而（无芒山羊草）中国春ＣＭＳ相对较差．在测交试验中，三种ＣＭＳ都找到了育性可完全恢复的恢复系．拟斯卑尔脱山羊草细胞质和尾状山羊草细胞质在杂种小麦生产应用中可能有较大潜力．     

男性不育患者精浆锌含量的分析

为探讨锌与男性不育患者的关系 ,本文研究测定了 173例男性不育患者精浆锌的含量 ,同时与正常生育男性进行比较。结果显示 ,正常生育男性与不育男性中少精子症、精子活率 <55%、活动力Ⅲ、Ⅳ级 <2 5% ,梗阻性无精子症 ,精液白细胞≥ 10 6 mL之间均有显著性差异。说明锌对男性生育过程起相当重要的作用 ,它在精浆中含量的变化可能是导致男性不育的原因之一。     

Calorimetric and DSC studies of mitochondria isolated from cytoplasmic male sterile line of rice

In this paper, the thermogenesis and differential scanning calorimetry (DSC) curves of energy release of the mitochondria isolated from variant strains of cytoplasmic male sterile lines of rices have been determined by using an LKB2277 Bioactivity Monitor and a DuPont 910 differential scanning calorimeter. The regularity and characteristics of the energy release of the mitochondria at constant and changing temperature were investigated, the differences in shape of the curves and the thermodynamic and kinetic characteristics of the thermogenesis of the mitochondria were compared, the thermodynamic and kinetic parameters of energy release of the mitochondria in the thermogenesis increasing stage were calculated, and the experimental thermokinetic equations describing the different thermogenesis processes were established. This revised version was published online in July 2006 with corrections to the Cover Date.     

Sur un théorème de P. Lelong pour les fonctions solutions d'une équation aux dérivées partielles elliptique

L'objet principal de ce travail est de généraliser un résultat de P. Lelong d'après lequel certaines fonctions analytiques de deux groupes variables réelles sont analytiques pour l'ensemble des variables. On se restreindra aux fonctions solutions d'une équation aux dérivées partielles elliptique à coefficients constants. Pour cela on introduit une fonction extrémale, associée à ces fonctions, qui paraît posséder certaines similitudes avec la fonction extrémale plurisousharmonique classique.     

第29届奥运会中外男篮技术成绩统计分析

本文对第29届奥运会中国男篮同相遇对手的技术成绩指标,进行了相关性、偏相关、回归分析等多元统计分析,通过回归方程找出影响总得分的主要因素,利用多因变量的线性模型对29届中国队与对手整体上进行比较,并对中国队在28、29两届上进行了整体的比较。结果显示:29届奥运会上中国队和对手在整体水平上有一定的差异;和28届相比,中国队前后差异不大,说明中国男篮进步幅度不是太大。     

Total Syntheses of AF-2785 and Gamendazole—Experimental Male Oral Contraceptives

Both AF-2785 and gamendazole are experimental male oral contraceptives. The total syntheses of these two compounds are achieved in good yields.

Supplemental materials are available for this article. Go to the publisher's online edition of Synthetic Communications® to view the free supplemental file.     

PAK1 as a Potential Therapeutic Target in Male Smokers with EGFR-Mutant Non-Small Cell Lung Cancer

P21-activated kinases (PAKs) are serine/threonine protein kinases that contribute to several cellular processes. Here, we aimed to determine the prognostic value of PAK1 and its correlation with the clinicopathological characteristics and five-year survival rates in patients with non-small cell lung cancer (NSCLC). We evaluated PAK1 mRNA and protein expression in NSCLC cells and resected tumor specimens, as well as in healthy human bronchial epithelial cells and adjacent healthy lung tissues, respectively, for effective comparison. Immunohistochemical tissue microarray analysis of 201 NSCLC specimens showed the correlation of PAK1 expression with clinicopathological characteristics. The mRNA and protein expression of PAK1 were 2.9- and 4.3-fold higher in six of seven NSCLC cell types and human tumors (both, p < 0.001) than in healthy human bronchial epithelial BEAS-2B cells and adjacent healthy lung tissues, respectively. Decreased survival was significantly associated with PAK1 overexpression in the entire cohort (χ² = 8.48, p = 0.0036), men (χ² = 17.1, p < 0.0001), and current and former smokers (χ² = 19.2, p < 0.0001). Notably, epidermal growth factor receptor (EGFR) mutation-positive lung cancer patients with high PAK1 expression showed higher mortality rates than those with low PAK1 expression (91.3% vs. 62.5%, p = 0.02). Therefore, PAK1 overexpression could serve as a molecular target for the treatment of EGFR mutation-positive lung cancer, especially among male patients and current/former smokers.