Syntheses and EGFR and HER-2 kinase inhibitory activities of 4-anilinoquinoline-3-carbonitriles: analogues of three important 4-anilinoquinazolines currently undergoing clinical evaluation as therapeutic antitumor agents

The syntheses and biological evaluations of 4-anilinoquinoline-3-carbonitrile analogues of the three clinical lead 4-anilinoquinazolines Iressa, Tarceva, and CI-1033 are described. The EGFR and HER-2 kinase inhibitory activities and the cell growth inhibition of the two series are compared with each other and with the clinical lead EKB-569. Similar activities are observed between these two series.     

Caligus solea n. sp. (Copepoda: Caligidae) parasitic on the common sole Solea solea (Linnaeus) from the north-eastern Mediterranean off the Turkish coast

A new species of caligid copepod, Caligus solea n. sp., is described from the common sole Solea solea (Linnaeus) caught off the north-eastern Mediterranean coast of Turkey. Both sexes of the parasite were collected from all over the upper body surface of its host. The new species belongs to the macarovi-group of species as established by Boxshall & Gurney (Bull Br Mus (Nat Hist) (Zool), 39:161–178, 1980), with which it shares the following four characters: (i) leg 4 with two-segmented exopod, distal segment carrying three apical spines but no lateral spine; (ii) distal exopodal segment of leg 1 with three plumose setae posteriorly plus four distal margin elements, spine 1 naked, spines 2 and 3 with accessory process and spine 4 about twice length of the others; (iii) females with one-segmented abdomen while males with two-segmented abdomen; (iv) male maxilliped with myxal process opposing the tip of the subchela. However, the new species differs from its congeners within the macarovi-group in the number of sensillae on each papilla on and around the postantennal process, and also in the absence of serrations along the distal margin of the maxilla. This is the twenty-eighth species of Caligus to be reported from the Mediterranean Sea.     

RING-type E3 ligases: Master manipulators of E2 ubiquitin-conjugating enzymes and ubiquitination

RING finger domain and RING finger-like ubiquitin ligases (E3s), such as U-box proteins, constitute the vast majority of known E3s. RING-type E3s function together with ubiquitin-conjugating enzymes (E2s) to mediate ubiquitination and are implicated in numerous cellular processes. In part because of their importance in human physiology and disease, these proteins and their cellular functions represent an intense area of study. Here we review recent advances in RING-type E3 recognition of substrates, their cellular regulation, and their varied architecture. Additionally, recent structural insights into RING-type E3 function, with a focus on important interactions with E2s and ubiquitin, are reviewed. This article is part of a Special Issue entitled: Ubiquitin–Proteasome System. Guest Editors: Thomas Sommer and Dieter H. Wolf.     

Improving the science-policy dialogue to meet the challenges of biodiversity conservation: having conversations rather than talking at one-another

A better, more effective dialogue is needed between biodiversity science and policy to underpin the sustainable use and conservation of biodiversity. Many initiatives exist to improve communication, but these largely conform to a ‘linear’ or technocratic model of communication in which scientific “facts” are transmitted directly to policy advisers to “solve problems”. While this model can help start a dialogue, it is, on its own, insufficient, as decision taking is complex, iterative and often selective in the information used. Here, we draw on the literature, interviews and a workshop with individuals working at the interface between biodiversity science and government policy development to present practical recommendations aimed at individuals, teams, organisations and funders. Building on these recommendations, we stress the need to: (a) frame research and policy jointly; (b) promote inter- and trans-disciplinary research and “multi-domain” working groups that include both scientists and policy makers from various fields and sectors; (c) put in place structures and incentive schemes that support interactive dialogue in the long-term. These are changes that are needed in light of continuing loss of biodiversity and its consequences for societal dependence on and benefits from nature.     

Fibre cables in the lacunae of Typha leaves contribute to a tensegrity structure

Background and Aims

Cables composed of long, non-lignified fibre cells enclosed in a cover of much shorter thin-walled, crystal-containing cells traverse the air chambers (lacunae) in leaves of the taller species of Typha. The non-lignified fibre cables are anchored in diaphragms composed of stellate cells of aerenchyma tissue that segment the long air chambers into smaller compartments. Although the fibre cables are easily observed and can be pulled free from the porous-to-air diaphragms, their structure and function have been ignored or misinterpreted.

Methods

Leaves of various species of Typha were dissected and fibre cables were pulled free and observed with a microscope using bright-field and polarizing optics. Maximal tensile strength of freshly removed cables was measured by hanging weights from fibre cables, and Instron analysis was used to produce curves of load versus extension until cables broke.

Key Results and Conclusions

Polarized light microscopy revealed that the cellulose microfibrils that make up the walls of the cable fibres are oriented parallel to the long axis of the fibres. This orientation ensures that the fibre cables are mechanically stiff and strong under tension. Accordingly, the measured stiffness and tensile strength of the fibre cables were in the gigapascal range. In combination with the dorsal and ventral leaf surfaces and partitions that contain lignified fibre bundles and vascular strands that are strong in compression, the very fine fibre cables that are strong under tension form a tensegrity structure. The tensegrity structure creates multiple load paths through which stresses are redistributed throughout the 1–3 m tall upright leaves of Typha angustifolia, T. latifolia, T. × glauca, T. domingensis and T. shuttleworthii. The length of the fibre cables relative to the length of the leaf blades is reduced in the last-formed leaves of flowering individuals. Fibre cables are absent in the shorter leaves of Typha minima and, if present, only extend for a few centimetres from the sheath into the leaf blade of Typha laxmannii. The advantage of the structure of the Typha leaf blade, which enables stiffness to give way to flexibility under windy conditions, is discussed for both vegetative and flowering plants.     

Costs of deception and learned resistance in deceptive interactions

The costs that species suffer when deceived are expected to drive learned resistance, although this relationship has seldom been studied experimentally. Flowers that elicit mating behaviour from male insects by mimicking conspecific females provide an ideal system for such investigation. Here, we explore interactions between a sexually deceptive daisy with multiple floral forms that vary in deceptiveness, and the male flies that pollinate it. We show that male pollinators are negatively impacted by the interaction, suffering potential mating costs in terms of their ability and time taken to locate genuine females within deceptive inflorescences. The severity of these costs is determined by the amount of mating behaviour elicited by deceptive inflorescences. However, inexperienced male flies exhibit the ability to learn to discriminate the most deceptive inflorescences as female mimics and subsequently reduce the amount of mating behaviour they exhibit on them with increased exposure. Experienced males, which interact with sexually deceptive forms naturally, exhibit similar patterns of reduced mating behaviour on deceptive inflorescences in multiple populations, indicating that pollinator learning is widespread. As sexually deceptive plants are typically dependent on the elicitation of mating behaviour from male pollinators for pollination, this may result in antagonistic coevolution within these systems.