Structure–activity relationship study of acridine analogs as haspin and DYRK2 kinase inhibitors

Haspin is a serine/threonine kinase required for completion of normal mitosis that is highly expressed during cell proliferation, including in a number of neoplasms. Consequently, it has emerged as a potential therapeutic target in oncology. A high throughput screen of approximately 140,000 compounds identified an acridine analog as a potent haspin kinase inhibitor. Profiling against a panel of 270 kinases revealed that the compound also exhibited potent inhibitory activity for DYRK2, another serine/threonine kinase. An optimization study of the acridine series revealed that the structure–activity relationship (SAR) of the acridine series for haspin and DYRK2 inhibition had many similarities. However, several structural differences were noted that allowed generation of a potent haspin kinase inhibitor (33, IC50 <60 nM) with 180-fold selectivity over DYRK2. In addition, a moderately potent DYRK2 inhibitor (41, IC50 <400 nM) with a 5.4-fold selectivity over haspin was also identified

Evaluation of a Re-designed Framework for Embodied Cognition Math Games

Embodied cognition posits that the development of thinking skills is distributed among mind, senses, and the environment. Research in this field has resulted into the development of applications in different areas including mathematics. This paper reports one part of a larger series of studies on the design and implementation of embodied cognition-based mathematics educational systems. We describe the evaluation of a game called Estimate It!, a wearable-based game for teaching measurement estimation and geometry. Experts were invited to evaluate the game, resulting in a generally positive rating. The game’s collaborative nature, its hands-on way of teaching estimation, and the incorporation of technology were seen as promising points. Infrastructure readiness, classroom control, and adjustment to the new technology were areas of concern

Migration and evaluation of a framework for developing embodied cognition learning games

A theory of cognition called embodied cognition believes that the development of thinking skills is distributed among mind, senses and the environment. Research into this field has resulted into the development of applications in different areas including Mathematics. This paper reports one part of a larger series of studies on the design and implementation of embodied cognition of Mathematics educational systems. We describe the migration and evaluation of a game called Estimate It , a wearables-based game for teaching measurement estimation and geometry. Teachers and students were invited to evaluate the game. The students found it to be generally fun and expressed their concerns with the game\u27s usability in the smartwatch as a point of improvement. The teachers noted that the game\u27s collaborative nature, its hands-on way of teaching estimation, and the incorporation of technology were seen as promising points. Infrastructure readiness, classroom control and adjustment to the new technology were areas of concern

Wearable Learning: Multiplayer Embodied Games for Math

We present a new technology-based paradigm to support embodied mathematics educational games, using wearable devices in the form of SmartPhones and SmartWatches for math learning, for full classes of students in formal in-school education settings. The Wearable Learning Games Engine is web based infrastructure that enables students to carry one mobile device per child, as they embark on math team-based activities that require physical engagement with the environment. These Wearable Tutors serve as guides and assistants while students manipulate, measure, estimate, discern, discard and find mathematical objects that satisfy specified constraints. Multi-player math games that use this infrastructure have yielded both cognitive and affective benefits. Beyond math game play, the Wearable Games Engine Authoring Tool enables students to create games themselves for other students to play; in this process, students engage in computational thinking and learn about finite-state machines. We present the infrastructure, games, and results for a series of experiments on both game play and game creation

Card-Collection Mechanics in Educational Location-Based AR Games: Transforming Learning Goals to Virtual Rewards

Location-based AR (LBAR) games offer a potentially viable learning platform for history-related content, but the experience is impaired by player fatigue due to compulsory movement between real-world locations, causing engagement to drop as the length of the game increases. This paper proposes incorporating card-collection mechanics (virtual collectibles/achievements in contemporary games) into an existing history-related, narrative-based LBAR game, Igpaw: Loyola, to counter the effect of fatigue to player engagement while increasing their capacity to absorb educational content. Participants, divided into control and experimental batches, were tasked to play Igpaw: Loyola without and with the collection mechanic, respectively, under logged observation. Both versions of the game included required and optional locations. The control and experimental batches reported only minor differences in application usability, but a majority of the experimental batch visited the optional locations as opposed to none from the control batch. In the post-quiz, the experimental batch scored the same or better (on average and on each individual question) than the control batch. This leads to the conclusion that the card-collection mechanic significantly and positively impacts both the engagement and learning retention of players, and it is recommended for future LBAR games

Igpaw: Loyola — Design of a Campus-Wide Augmented Reality Game Using MAGIS

We present Igpaw: Loyola, a new location-based mobile AR (augmented reality) adventure game designed to be played within the campus grounds of the Ateneo de Manila University. Igpaw: Loyola improves upon its predecessor, Igpaw: Intramuros, by upgrading gameplay mechanics to accommodate lengthier learning modules, improving the usability of both interactive (AR) and navigation (non-AR) portions of the game, and enhancing the game authoring process with the help of an improved version of the MAGIS (Mobile Augmented-Reality Game-Engine for Instructional Support) framework. A preliminary user evaluation is also presented