The naturally occurring bile acid lithocholic acid (LCA) has been a crucial core structure for many non-sugar-containing sialyltranferase (ST) inhibitors documented in literature. With the aim of elucidating the impac...
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The chemical screening of an algae-containing marine sponge identified as Lendenfeldia species has isolated two 24-homoscalarane sesterterpenoids, including a known compound, felixin A (1) and a new analogue, lendenfe...
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The naturally occurring bile acid lithocholic acid (LCA) has been a crucial core structure for many non-sugar-containing sialyltranferase (ST) inhibitors documented in literature. With the aim of elucidating the impac...
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The naturally occurring bile acid lithocholic acid (LCA) has been a crucial core structure for many non-sugar-containing sialyltranferase (ST) inhibitors documented in literature. With the aim of elucidating the impact of the terminal carboxyl acid substituent of LCA on its ST inhibition, in this present study, we report the (bio)isosteric replacement-based design and synthesis of sulfonate and sulfate analogues of LCA. Among these compounds, the sulfate analogue SPP-002 was found to selectively inhibit N-glycan sialylation by at least an order of magnitude, indicating a substantial improvement in both potency and selectivity when compared to the unmodified parent bile acid. Molecular docking analysis supported the stronger binding of the synthetic analogue in the enzyme active site. Treatment with SPP-002 also hampered the migration, adhesion, and invasion of MDA-MB-231 cells in vitro by suppressing the expression of signaling proteins involved in the cancer metastasis-associated integrin/FAK/paxillin pathway. In totality, these findings offer not only a novel structural scaffold but also valuable insights for the future development of more potent and selective ST inhibitors with potential therapeutic effects against tumor cancer metastasis.
作者：
Andrew Min Han ChinThomas MenkhoffHans-Dieter EversHoong Hui Daniel GnKevin KohChester Wey LeePatrick H. M. LohLinda LowSebastian TanTeng Seng TeoNatalie YapLee Kong Chian School of Business
Singapore Management University (SMU) 81 Victoria Street Singapore 188065 Singapore Andrew Chin Min Han graduated from Tsinghua University in Beijing
China with a Tsinghua–MIT Sloan International Master of Business Administration degree under the Singapore Government’s Asian Business Fellowship (ABF) scholarship program. He is the Program Director of Singapore Management University (SMU) Executive Certificate in China Business and of the SMU Internationalisation Series. He teaches as an Adjunct Faculty of Strategy and Organisation at the SMU Lee Kong Chian School of Business since January 2017. He teaches effectively in English and Chinese. With over 23 years of experience in education and publishing industry in Asia
Andrew Chin’s multi-sector career has enabled him to experience the full spectrum of the education industry in his roles as the Singapore EDB Officer handling the World-Class University portfolio and the Specialist Information and Publishing Industry portfolio Chief Representative and Country Manager (China) at Thomson Learning (Fortune 500 company) and Co-founder and CEO for an early childhood education business. Andrew was a Business Development Director (Universities) at Sodexo Group (Fortune 500 company) for the Asia-Pacific region. After working 10 years in Beijing
China Andrew returned to Singapore in 2012 to work closely with the top leadership at Singapore Management University on the SMU China & East Asia Initiatives. Thomas Menkhoff is the Professor of Organisational Behaviour & Human Resources (Education) at the Lee Kong Chian School of Business
Singapore Management University (SMU). Two of his recent publications include: (i) Menkhoff Thomas Ning Kan Siew Evers Hans-Dieter and Chay Yue Wah eds. Living in Smart Cities: Innovation and Sustainability (New Jersey: World Scientific Publishing 2018) and (ii) Chay
Yue Wah Menkhoff Thomas and Low Linda eds. China’s Belt and Road Initiative — Understanding the Dynamics of a Global Transfor
In this paper, we explain how an experiential learning course and study tour to Gansu Province (People’s Republic of China) enabled undergraduates at the Singapore Management University (SMU) to acquire 21st-century ...
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In this paper, we explain how an experiential learning course and study tour to Gansu Province (People’s Republic of China) enabled undergraduates at the Singapore Management University (SMU) to acquire 21st-century competencies and higher-order thinking skills by analyzing and evaluating specific aspects of China’s Belt and Road Initiative (BRI) and China–Singapore (Chongqing) Connectivity Initiative — New International Land–Sea Trade Corridor (CCI-ILSTC) with emphasis on developing viable Go-To-Market (GTM) strategies aimed at selling Gansu produce in four Southeast Asian markets. We share how the course was designed to support the attainment of key learning goals and discuss how we turned pedagogical aspirations into concrete learning outcomes. We introduce key aspects of the so-called “SMU-XO” project that the students conducted in partnership with an industry partner, Pacific International Lines (PIL), and discuss how the project work helped learners to gain global competency by (i) examining critical issues related to BRI such as multi-modal infrastructure connectivity, (ii) appreciating the local perspectives of project stakeholders in Lanzhou and Shanghai and (iii) successfully interacting with people from different cultures, namely China, Indonesia, Vietnam, Malaysia and Thailand.
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