41 search results for “glycosidases” in the Public website
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Inhibitors and probes targeting endo-glycosidases
The chemical synthesis of inhibitors and probes targeting endo-glycosidases.
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Understanding functional dynamics and conformational stability of beta-glycosidases
Due to their central physiological roles in living organisms, retaining beta-glycosidases have been the subject of tremendous research efforts to examine their structure/function relation using numerous biophysical and biochemical approaches.
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Cyclophellitol analogues for profiling of exo- and endo-glycosidases
To this day, all cyclophellitol-based inhibitors and ABPs have been close analogues of their natural substrate counterparts. As a result, these probes showed high selectivity towards their target glycosidases.
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Fluorescence Polarization Activity-Based Protein Profiling on Retaining Glycosidases
Glycosidases are important enzymes in the turnover of polysaccharides and glycoconjugates, and are involved in a range of human pathologies including genetic disorders such as Gaucher and Pompe disease, but also in various cancers.
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Exploring chemical space in covalent and competitive glycosidase inhibitor design
Glycoside hydrolases (glycosidases/GHs) are widely abundant enzymes in all kingdoms of life and are important biocatalysts that catalyze the hydrolysis of glycosidic linkages in oligo/polysaccharides, glycoproteins and glycolipids with tremendous efficiency
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Cyclophellitol and its derivatives: synthesis and application as beta-glycosidase inhibitors
Promotores: Prof.dr. H.S. Overkleeft, Prof.dr. G.A. van der Marel
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conformational inhibitors and activity-based probes for retaining glycosidases
Glycosidases are essential in fundamental biological processes and are responsible for the degradation of most (oligo)saccharides, glycolipids and glycoproteins.
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Fundamental and applied biochemical investigations on retaining glycosidases
The studies described in this thesis deal with glycosidases, in particular alpha-galactosidases.
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carbohydrate-mimetic cyclitols: towards deactivators of inverting glycosidases and glycosyl transferases
Synthetic methodlogy is described, aiding in the synthetic preparation of putative inhibitors of retaining and inverting glycosidases and glycosyl transferases. All constructs are cyclophellitol-based cyclitols.
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Direct and two-step activity-based profiling of proteases and glycosidases
Promotores: Prof.dr. H.S. Overkleeft, Prof.dr. G.A. van der Marel
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Applications for activity-based probes in biomedical research on glycosidases
Lysosomal glycosidases are acid hydrolases that fragment glycoconjugates in lysosomes.
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Inhibitors and activity-based probes for β-D-glucuronidases, heparanases and β-L-arabinofuranosidases
Glycosidases (GHs) are enzymes responsible for the degradation of carbohydrates and play many roles in human health and pathophysiology. Often, abnormal levels of glycosidase activity are markedly linked to human pathologies.
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Projects
Research projects
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Carbohydrate chemistry champion: Hermen Overkleeft claims prestigious award
Professor Hermen Overkleeft has received the esteemed Roy L. Whistler International Award in Carbohydrate Chemistry for 2024 by the International Carbohydrate Organization. The award recognises Overkleeft’s outstanding contributions to the field of carbohydrate chemistry and biochemistry.
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Glycosidases as an analytical tool in glycomics assays
PhD defence
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Exploring chemical space in covalent and competitive glycosidase inhibitor design
PhD defence
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Research
Through metabolism, biochemical processes give rise to the complexity of life. Acquired and inborn errors in metabolism underlie many diseases occurring in man. The challenge for present day medical biochemistry is to find, and integrate, pieces of information at molecular, cell and organismal level…
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Novel Activity-Based Probes for Broad-Spectrum Profiling of Retaining β-Exoglucosidases In Situ and In Vivo
A high-end label: Cyclophellitol aziridine-type activity-based probes allow for ultra-sensitive visualization of mammalian β-glucosidases (GBA1, GBA2, GBA3, and LPH) as well as several non-mammalian β-glucosidases (see picture). These probes offer new ways to study β-exoglucosidases, and configurational…
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Hermen Overkleeft
Science
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Madouc Bergers made her own enzyme inhibitors for her bachelor’s thesis
For her bachelor’s thesis, Molecular Science and Technology student Madouc Bergers synthesized her own molecule that can inhibit the breakdown of sugars. Although most students do not even manage to make one building block, Madouc made three. Partly because of this, she has been nominated for the Science…
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Fundamental and translational medical biochemistry
Through metabolism, biochemical processes give rise to the complexity of life. Acquired and inborn errors in metabolism underlie many diseases occurring in man. The challenge for present day medical biochemistry is to find, and integrate, pieces of information at molecular, cell and organismal level…
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PhD Theses
A full overview of MacBio PhD Theses.
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Activity-based protein profiling of glucosidases, fucosidases and glucuronidases
Promotores: H.S. Overkleeft, G.A. van der Marel, Co-promotor: B.I. Florea
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Inhibitors and probes targeting mannanases
This thesis describes the synthesis and biochemical evaluation of a variety of cyclophellitol based activity-based probes and inhibitors targeting various endo- and exo-acting retaining glycosidases. In the last two decades a variety of probes and inhibitors for (hemi)cellulose degrading enzymes have…
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Chemical biology of sphingolipids: fundamental studies and clinical applications
Overkleeft
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Research
Research at the BIOSYN group is comprised of the following research themes:
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Activity-based protein profiling for drug discovery
Activity-based protein profiling (ABPP, also termed chemical proteomics), is one of the pillars of chemical biology, and at LED3 we have taken it to the next level. ABPP allows the assessment of protein function in live cells and tissues, which means that the activity of a complete protein family can…
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Chemical Probe Facility
The Chemical Probe Facility is part of the Leiden Early Drug Discovery & Development (LED3) center. Activity-based protein profiling (ABPP) is one of the pillars of chemical biology. ABPP determines the activity of entire protein families in living cells and tissues under physiological conditions, such…
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Chemical biology of glucosylceramide metabolism: fundamental studies and clinical applications for Gaucher disease
How can we develop new chemical biology tools and approaches to understand and interfere with glucosylceramide metabolism in relation to Gaucher disease?
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Paradigm-shifting theory highlights the importance of substrate flexibility in enzymatic reactions
Leiden chemists have proposed a new model for enzymatic reactions, in which the flexibility of the substrate is much more important than previously thought. Their results are paradigm-shifting and could have major implications for drug research and enzyme engineering. Publication in Angewandte Chemi…
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Changing enzymes for clean energy and disease prevention
They can play a role in metabolic disorders and can break down tough plant fibers: β-glycosidases are enzymes that play many roles in nature. Fredj Ben Bdira changed these enzymes in order to enhance the production of clean energy and to improve the treatment of patients with metabolic diseases.
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Michel Orrit and Hermen Overkleeft members KNAW
The Royal Netherlands Academy of Arts and Sciences (KNAW) selects prominent researchers as members based on their scientific achievements. On September 17th, the KNAW will install 21 new members, including Leiden physicist Michel Orrit and chemist Hermen Overkleeft.
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Cancer pathogenesis and therapy
With cancer, a person’s body cells grow uncontrollably. Putting together a detailed picture of how this comes about makes it possible to develop efficient therapies. Researchers at the Leiden University Medical Centre (LUMC) and Leiden University are working together to gain a better understanding…
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Hermen Overkleeft new Scientific Director of chemistry institute LIC
As of July 1, Professor of Bio-organic Synthesis Hermen Overkleeft will be appointed as the Scientific Director of the Leiden Institute of Chemistry (LIC). He will succeed Jaap Brouwer, who has been managing the institute for the past twelve years. Overkleeft has been appointed for a period of four…
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Collaborative and effective drug development
There are many complex links in the chain that provides patients with new drugs: from fundamental science, to clinical tests, to production. The entire chain can be found in Leiden. Leiden University, the Leiden University Medical Center (LUMC) and the businesses at the Leiden Bio Science Park (LBSP)…
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Life Science & Technology (MSc)
Increased molecular knowledge of the mechanisms of processes in the cell can lead to better medicines or new methods for combating diseases. Our MSc students in Life Science and Technology (LST) specifically learn to understand the molecular and structural chemical and biological aspects of disease-related…
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Inhibitors and activity-based probes for retaining β-D-glucuronidases, heparanases and β-L-arabinofuranosidases
PhD defence
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Reedijk Symposium 2023
Conference
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Five Leiden professors elected to KNAW
The Royal Netherlands Academy of Arts and Sciences has elected five Leiden professors from different disciplines as new members. Two of the new members are women.
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LIC Lecture + drinks
Lecture
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Reedijk Symposium 2023 poster session
Conference