190 zoekresultaten voor “inhibitors” in de Publieke website
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When structure-affinity relationships meet structure-kinetics relationships: 3-((Inden-1-yl)amino)-1-isopropyl-cyclopentane-1-carboxamides as
Source: Eur J Med Chem (2015)
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Using insertional mutagenesis to identify breast cancer drivers and therapy resistance genes in mice
In this thesis, we used genetically engineered mouse models to identify genes and pathways that are involved in ILC formation and in the development of resistance to FGFR-targeted therapy.
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Regulation of actomyosin contraction as a driving force of invasive lobular breast cancer
In this thesis, we used genetically engineered mouse models and a variety of cell-culture based assays to identify genes and pathways that are involved in the development and treatment of invasive lobular carcinoma (ILC).
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Activity-based protein profiling in drug discovery
In the last decades, activity-based protein profiling (ABPP) has emerged as a powerful chemical tool that may aid the ever-challenging drug discovery process.
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Grants & Awards
Grants awarded to molecular physiology research
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Chemical biology of sphingolipids: fundamental studies and clinical applications
Overkleeft
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Student projects
Bachelor and Master students of all chemistry related studies are more than welcome to take part in our research activities. We have projects on design and synthesis of biologically relevant compounds within an ongoing research project. Supervision, following the apprentice/teacher model, is one of…
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Small molecule prevents tumour cells from spreading
Leiden chemists, together with colleagues at the University of York (UK) and Technion (Israel) have discovered a small, sugar-like molecule that maintains the integrity of tissue around a tumour during cancer. This molecule prevents tumour cells from spreading from the primary cancer site to colonise…
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Elliot Mock
Our response to stress is regulated by the ‘bliss molecule’ anandamide but how exactly remained unknown. Until recently, that is. Elliot Mock has now succeeded in developing a new substance that reduces anandamide, called LEI-401. This has made it easier to conduct research into the role of anandamide…
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Reflect react and interact
The roles of shame, guilt and social access in adolescent aggression
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Support Leiden's corona research
Scientists at the LUMC are working hard on potential virus inhibitors, antiviral screening and a treatment for COVID-19. But finding funding for the research project wastes precious time. SteunLeiden.nl has therefore started a crowdfunding for Professor of Virology Eric Snijder and his team. Donate…
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Pursuing new anti-cancer therapy as a team
Cancer is the leading cause of death in the Netherlands, and, with over 100 different types of cancer, it’s not a simple disease. Today, skin, breast, lung, prostate and colon cancer are the most diagnosed forms. Therefore, the discovery and development of new drugs has the ability to significantly…
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Studies on molecular basics of metabolic syndrome in zebrafish
The research described in this thesis has, using the zebrafish as a model system, shed new light on the intricate relationship between TB and DM2, in particular on the role of leptin, SHP-1 and glucocorticoids.
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Halting protein degradation may contribute to new cancer treatment
Chemist Gerjan de Bruin has designed a method of slowing down the degradation process of proteins in cells. This may contribute to new cancer medicines with fewer side-effects. PhD defence on 1 June.
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Biology Lecture: Discovery of the Phase I Clinical Agent and MPS1 inhibitor BOS172722 for the Treatment of Triple Negative Breast Cancer
Lezing
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700,000 euros for the fight against aggressive breast cancer
To inhibit proteins that contribute to the growth of aggressive cancer cells, that’s the plan of Professor Bob van de Water and his team. They will receive over 700,000 euros from the KWF Dutch Cancer Society for their research. Researcher Maaike Vreeswijk and pathologist Danielle Cohen are affiliated…
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The scientists behind LED3
LED3 is the combined effort of three excellent institutes of Leiden University. Through joined hands, we are able to give rise to a more effective early drug discovery pipeline. Let us briefly introduce the three institutes.
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PhD Theses
A full overview of MacBio PhD Theses.
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Do internationally adopted children in the Netherlands use more medication than their non-adopted peers?
Adoptees in the Netherlands generally do not use more medication than their non-adopted peers.
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Chara
The Green algae Chara as model system for intra and inter cellular transport processes.
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Key publications
Key publications of the Quantitative Pharmacology group
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More effective blocking of CCR2 receptor
The discovery of new medicines is a tedious and lengthy process. On average, over 10,000 molecules need to be studied for one to become a drug and reach the patient. Part of that process are the very costly clinical trials in humans, and candidate drugs often fail due to side effects or lack of efficacy.…
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Research
Research at the Macromolecular Biochemistry group is comprised of the following research themes:
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Hit Discovery
The goal of hit discovery is to identify suitable chemical starting points to modulate a drug target. A hit can be, a.o., a small molecule, a protein or mRNA. Hit identification is performed via rational design, genome mining, (targeted) library screening, or in silico approaches.
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Bio-organic Synthesis
The research in the Biosyn group is focused on the design, synthesis and function of the four major types of biomolecules: nucleic acids, carbohydrates, peptides and lipids and hybrid structures thereof. These biomolecules and their derivatives are used in drug discovery and chemical biology, to develop…
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Annelot van Esbroeck wins Best Oral Communication Prize
Annelot van Esbroeck-Weevers, PhD student at the Molecular Physiology research group at the Leiden Institute of Chemistry, headed by Dr. Mario van der Stelt, has been awarded the Best Oral Communication Prize at the 8th European Workshop on Cannabinoid Research, held from 31 August to 2 September 2017…
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Anthe Janssen wins the YMCS Public's Choice Prize
Anthe Janssen, a PhD student in the Molecular Physiology research group of Prof. Mario van der Stelt, has been awarded the Public's Choice Prize for Best Oral Presentation during the Young Medicinal Chemist Symposium '18 in Ljubljana, Slovenia.
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The EPIC Alliance joins forces to combat antibiotic resistance
No, this isn’t about a Star Wars Alliance that wants to suppress The Resistance. Rather, the EPIC Alliance brings together scientific experts from seven countries to address the growing threat of antibiotic resistance. Leiden professor Nathaniel Martin is part of the 11-member consortium.
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VICI for Mario van der Stelt
For his ground-breaking chemical biological research, a VICI-grant has been awarded to Mario van der Stelt, professor of Molecular physiology at Leiden University. In a new research line, he aims to discover binding sites for new medicines against inflammations in the brain.
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‘How can we translate the language of cells into cancer therapies?’
On 23 April 2021, Professor Alfred Vertegaal from the Department of Cell and Chemical Biology at the Leiden University Medical Center (LUMC) delivered his inaugural lecture ‘Unraveling and exploiting cellular communication codes’. Vertegaal used the opportunity to describe how research in the field…
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Deadly infections on the increase: urgent need for new antibiotics
Globally, the number of deaths from infections is on the rise as more bacteria become resistant to antibiotics. New classes are desperately needed. A promising resistance inhibitor is now being developed by the research group of Nathaniel Martin, Professor of Biological Chemistry. Inaugural speech on…
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Two-pronged attack on infectious diseases
A combination of two potential drugs gives hope of a 'super blockage' of an over-active immune system, Leiden researchers report in Nature. The breakthrough came from the crystallisation of a membrane protein.
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Zhiyi Yu - winner of LACDR Spring Symposium
Zhiyi Yu was elected as the winner of the annual PhD Competition at the LACDR Spring Symposium on June 17th 2014.
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Mario van der Stelt and Annelot van Esbroeck win awards at international conference in Canada
Mario van der Stelt (Head of the department of Molecular Physiology at the Leiden Institute of Chemistry) has received the Young Investigator Award from the International Cannabinoid Research Society during the annual meeting of the society in Montreal, Canada. The Young Investigator Award was given…
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ERC grant to improve post-vaccination protection in low-income countries
Maria Yazdanbakhsh, Professor of Parasitology at the Leiden University Medical Centre (LUMC), has been awarded an ERC Advanced Grant of 2.5 million euros. She will investigate why people in Africa and Southeast Asia respond less to certain vaccines than Europeans. Her goal is to find a solution for…
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Awards and Grants 2018
An overview of awards and prizes granted to our staff and students in 2018, as well as special appointments and royal distinctions.
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In Memoriam Professor Huib Ovaa
On the 19th of May 2020, our dear colleague and friend Professor Dr. Huib Ovaa has passed away from prostate cancer. Last summer Huib became ill, and in first instance it appeared that he had attracted a relatively harmless infectious disease. Unfortunately, it became soon apparent that he suffered…
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From lab discovery to a new drug: the Venture Challenge makes it possible
A breakthrough from the PhD research of medical chemist Elmer Maurits may help patients with autoimmune diseases and blood cancer in the future. But bringing a discovery from the lab to the clinic is not so easily done. Thanks to NWO's Venture Challenge, Maurits and his team will receive ten weeks of…
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EU awards 18 million euros for research into new antibiotics
An international consortium of research groups is aiming to develop novel antibiotics against the tuberculosis bacteria and two other deadly bacteria. The European Union has awarded a total of 18 million euros to the RespiriTB and RespiriNTM projects. Researchers from the Leiden University Medical Centre…
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New substances inhibit inflammation in the brain
Chemical biologists from Leiden, led by Dr Mario van der Stelt, have discovered substances that can reduce inflammation processes in the brain. This is a first step in the development of potential medicines for the treatment of brain diseases like Alzheimer's and Parkinson's. Published in Proceedings…
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Postdoctoral researcher in structural biology of glycan-modifying enzymes
Wiskunde en Natuurwetenschappen, Leids Instituut voor Chemisch Onderzoek (LIC)
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Teaching
Research projects for students of the University of Leiden and other Dutch Universities are often available at the MacBio group. The research lines are also described in the Research section. For details of specific projects contact the supervisor (Ubbink, Dame, Boyle).
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Using zebrafish to target the Achilles’ heel of cancer
Exploiting metabolic vulnerabilities to identify anticancer compounds in zebrafish synthetic lethality screens.
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Double success at the EMBL Chemical Biology Conference
Thomas Bakkum en Tom van der Wel, two PhD candidates from the Leiden Institute of Chemistry, have both won poster prizes at the EMBL Chemical Biology Conference 2018 in Heidelberg.
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Freek Janssen wins award for best European Young Medicinal Chemist
Freek Janssen, a PhD-student in the department of Molecular Physiology, has received an award for the best oral presentation during the Young Medicinal Chemist Symposium organised by the European Federation of Medicinal Chemistry (EFMC-YMCS’16). Freek Janssen presented his work on “Development of Highly…
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LUMC involved in development of novel drugs to treat and prevent SARS-CoV-2 and other coronaviruses
The Department of Medical Microbiology at Leiden University Medical Center (LUMC) is researching antiviral drugs that could treat and prevent SARS-CoV-2 in various projects. One part of the PanCoroNed project is being led by Martijn van Hemert and involves lab tests into the antiviral effect of molecules…
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Leiden University strengthens its focus on Chemical Biology and Medicinal Chemistry with seven new group leaders
Tackling key challenges of Chemical Biology and Medicinal Chemistry to aid drug discovery is one of the focus areas of Leiden University. To this end, the Leiden Early Drug Discovery & Development network (LED3) was established by the Leiden Institute of Chemistry (LIC), the Institute of Biology Leiden…
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Three Leiden Science projects receive computing time on national supercomputers
A night sky of more than 40 petabytes in size, simulating young star clusters and understanding how the body inhibits viruses: three Leiden projects have received computing time on one of the national computer systems.
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Aggressiveness of cancer cells halted
Zebrafish-human communication shows that cancer cells lacking a signaling protein are less able to develop aggressive metastatic properties. This discovery has been made by molecular cell biologist Claudia Tulotta. PhD defence 14 June.
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The body's own marijuana as inspiration for drug research
Endocannabinoids - the body's own marijuana - are promising departure points for drug research. Professor of Molecular Physiology Mario van der Stelt examines whether inhibiting their production can be a way to fight inflammatory brain disease and to combat obesity. Inaugural lecture 19 October.