Strategies to Modulate Specialized Metabolism in Mediterranean Crops: From Molecular Aspects to Field

Plant specialized metabolites (SMs) play an important role in the interaction with the environment and are part of the plant defense response. These natural products are volatile, semi-volatile and non-volatile compounds produced from common building blocks deriving from primary metabolic pathways and rapidly evolved to allow a better adaptation of plants to environmental cues. Specialized metabolites include terpenes, flavonoids, alkaloids, glucosinolates, tannins, resins, etc. that can be used as phytochemicals, food additives, flavoring agents and pharmaceutical compounds. This review will be focused on Mediterranean crop plants as a source of SMs, with a special attention on the strategies that can be used to modulate their production, including abiotic stresses, interaction with beneficial soil microorganisms and novel genetic approaches.     

Peptidyl Vinyl Ketone Irreversible Inhibitors of Rhodesain: Modifications of the P2 Fragment

In this paper, we report the design, synthesis and biological investigation of a series of peptidyl vinyl ketones obtained by modifying the P2 fragment of previously reported highly potent inhibitors of rhodesain, the main cysteine protease of Trypanosoma brucei rhodesiense. Investigation of the structure–activity relationship led us to identify new rhodesain inhibitors endowed with an improved selectivity profile (a selectivity index of up to 22 000 towards the target enzyme), and/or an improved antitrypanosomal activity in the sub-micromolar range.     

Design and eco-innovation: micro-evidence from the Eurobarometer survey

ABSTRACT

This paper investigates the role of design in making firms eco-innovate. Going beyond the ‘packed’ approach of environmental studies about ‘eco-design’, we maintain that the eco-innovative impact of design is correlated with the firm’s decision to invest in it. In turn, design investment is assumed connected with the use firms make of design. By pooling the Eurobarometer 2015 and 2016 surveys, we test for these arguments with respect to a sample of nearly 4500 European and non-European (US and Switzerland) manufacturing firms. Results confirm that the firms’ capacity of eco-innovating increases when they invest in design, also by making this investment dependent on the role of design within the firm. The relationship between eco-innovation and design appears robust with respect to the different kinds of ‘eco-innovators’ that the Eurobarometer enables us to consider, while some interesting variability emerges when splitting the sample by group of countries and industries.     

Investigation of cure kinetics in epoxy/multiwalled carbon nanotube nanocomposites

With the increased interest in thermoset resin nanocomposites, it is important to understand the effects of the material on nanoscale characteristics. In this study, a curing reaction of an epoxy resin, which contained 0.25, 0.50, or 1.00 wt % of multiwalled carbon nanotubes (MWCNTs), at different heating rates was monitored by differential scanning calorimetry; cure kinetics were also evaluated to establish a relationship between crosslinking (network formation) and mechanical properties. MWCNT concentrations above 0.25 wt % favored crosslinking formation and decreased the activation energy (E_a) in the curing reaction. Examination of the kinetic mechanism suggests that the MWCNT locally restricted the spatial volume and favored the formation of nodular morphology in the resin, especially for high MWCNT concentrations. The MWCNT exhibited some entanglement in the matrix, which hindered a more pronounced effect on the mechanical properties. © 2013 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2014 , 131, 39857.     

Bioreduction of α‐Acetoxymethyl Enones: Proposal for an SN2′ Mechanism Catalyzed by Enereductase

(Z)‐3‐Acetoxymethyl‐4‐R‐3‐buten‐2‐ones (R=aryl, alkyl) and (Z)‐3‐methyl‐4‐R‐3‐buten‐2‐ones (R=aryl) were synthesized and submitted to reduction by the yeast Saccharomyces cerevisiae producing the (R)‐ and (S)‐4‐R‐3‐methybutan‐2‐ones, respectively. This stereochemistry control strategy was applied in the syntheses of (R)‐ and (S)‐Tropional® with moderate to high enantiomeric excesses. Other (Z)‐3‐acyloxymethyl‐4‐phenyl‐3‐buten‐2‐ones showed similar behavior to the (Z)‐3‐acetoxymethyl counterpart, and the acylated Morita–Baylis–Hillman adduct 1‐acetoxy‐2‐methylene‐1‐phenylbutan‐3‐one produced a mixture of products, with and without the acetoxy group, via three different reaction pathways. In addition to experiments employing whole cells, those in which isolated enereductases were used suggested that the main pathway through which the loss of the acetoxy group occurs during the biocatalytic cascade is an S_N2′‐type reaction, rather than formal hydrogen addition followed by acetic acid elimination. Finally, related ethyl enones were reduced enantioselectively by the yeast Candida albicans, producing both (R)‐ and (S)‐reduction products, depending on the presence of the acetoxy group in the starting material.

     

Small‐Molecule Inhibitors of AF6 PDZ‐Mediated Protein–Protein Interactions

PDZ (PSD‐95, Dlg, ZO‐1) domains are ubiquitous interaction modules that are involved in many cellular signal transduction pathways. Interference with PDZ‐mediated protein–protein interactions has important implications in disease‐related signaling processes. For this reason, PDZ domains have gained attention as potential targets for inhibitor design and, in the long run, drug development. Herein we report the development of small molecules to probe the function of the PDZ domain from human AF6 (ALL1‐fused gene from chromosome 6), which is an essential component of cell–cell junctions. These compounds bind to AF6 PDZ with substantially higher affinity than the peptide (Ile‐Gln‐Ser‐Val‐Glu‐Val) derived from its natural ligand, EphB2. In intact cells, the compounds inhibit the AF6–Bcr interaction and interfere with epidermal growth factor (EGF)‐dependent signaling.     

材料的重要性

《材料的重要性》是《景观设计理论》的一段节选。《景观设计理论》旨在不使用专业术语或其他领域假说的前提下,结合景观设计过程向学生介绍内在理论思想。《材料的重要性》是本书的五章之一。每一章针对特定理论,解释了其基础和来源,探讨了它对设计的重要性,列举了20—21世纪与其相关的设计案例,整理了该理论的辩论(尤其是有关现代和后现代思想),最后还有相关阅读材料清单和需要学生们思考的问题。本文分为如下3个部分：第一部分,物质性,介绍“辩证唯物主义”“媒介即信息”“物质实践”和“编码”等理论及其在设计中的运用;第二部分,通过“建构表达”“地貌代理人策略”“石材的面层”“材料的暗示”“人造,但不是伪造”等理论,介绍材料的真实性及其在设计中的运用;第三部分,复写理论及应用,包括“剩余物”“复写的展示性”“未来的复写”和“虚构的复写”等内容。     

风景园林与绿色基础设施在城市流域水资源规划中的重要作用

通过绿色基础设施途径,处理美国波士顿北部的马萨诸塞州城市流域的水资源规划问题。从多个尺度为风景园林师提供水资源规划的经验与启发,探究公众对新型绿色基础设施解决方案的态度与偏好,以及公众偏好对于整体规划设计的重要作用。     

温州“城中村”改造实践与探索

温州的“城中村”改造当前所面临的问题是:规划研究与政策制定滞后、未能正确面对“三农”问题、与房地产市场调控相脱节等。应充分利用市场化手段,依靠和发动全社会开展“城中村”改造。