1,889 search results for “drug discovery” in the Public website
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Quantitative Systems Pharmacology
This research area is focused on the development and application of novel concepts and models in the emerging area of quantitative systems pharmacology (QSP).
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Binding kinetics
A tantalizing concept that has emerged in our recent research is binding kinetics. An important parameter is residence time (RT), a direct reflection of how long a drug stays bound to its target. This parameter is of crucial importance, because drug action lasts only as long as the receptor-ligand complex…
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The impact of obesity on the pharmacokinetics of drugs in adolescents and adults
Promotores: C.A.J. Knibbe; J.N. van den Anker, Co-promotores: H.P.A. van Dongen; B. van Ramshorst
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Hildert Bronkhorst
Science
h.bronkhorst@biology.leidenuniv.nl | +31 71 527 4964
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Key publications
Key publications of the Cancer Drug Target Discovery group
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Hit and Lead Optimization
The goal of hit and lead optimization is to optimize suitable chemical starting points that can modulate a drug target. The methods and technologies used are similar to those in Hit Discovery, but once the compound has shown activity in an animal model, it moves from 'hit' to 'lead.'
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resources for Iberian empires: ecology and globalization in the age of discovery
An interdisciplinary and innovative research group combining History, underwater archaeology, GIS and wood provenancing methods.
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Agonists for the Adenosine A1 Receptor with Tunable Residence Time. A Case for Nonribose 4-Amino-6-aryl-5-cyano-2-thiopyrimidines
Source: J Med Chem, Volume 57, Issue 8, pp. 3213-22 (2014)
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Key publications
Key publications of the Predictive Pharmacology group.
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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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TARGETBIO: Transmission of Antimicrobial Resistance Genes and Engineered DNA from Transgenic Biosystems in Nature
This project aims to assess the risk of spread of antimicrobial resistance genes in the environment derived from currently used synthetic biology approaches in the field of drug discovery.
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Chemical genetics strategy to profile kinase target engagement reveals role of FES in neutrophil phagocytosis, Nat. Comm. 2020
Chemical tools to monitor drug-target engagement of endogenously expressed protein kinases are highly desirable for preclinical target validation in drug discovery. Here, we describe a chemical genetics strategy to selectively study target engagement of endogenous kinases.
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In silico characterization of a GPCR focused library
Supervisor: Gerard van Westen
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A much-needed new class of antibiotics
Antimicrobial resistance (AMR) is the phenomenon that pathogens become insensitive to the antibiotics that we use against them. A growing number of pathogens is becoming resistant, with methicillin-resistant S. aureus (MRSA) as the most famous example. But while the threat of AMR represents a slow-moving…
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Systems microscopy to unravel cellular stress response signalling in drug induced liver injury
Promotor: B. van de Water
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Genomics driven metabolomics novel strategies for the discovery and identification of secondary metabolites
Promotor: Prof.dr. T. Hankemeier, Co-promotor: R.J. Vreeken
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Cheminformatics: Analyzing small-molecule activity data
While bioinformatics methods deal with the analysis of sequence information (be it proteins or DNA), the field of cheminformatics is concerned with the analysis of small-molecule datasets.
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Career prospects
Many students receive their first job offer during or right after their Business Studies internship. After graduating you can also aim for a career in Bio-Pharmaceutical research.
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quantification of growth hormone secretion : application of model-informed drug development in acromegaly
Growth hormone profiles are pulsatile and highly variable between individuals, limiting the implementation of mathemathical models to quantify an individual's secretion.
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NWO grant for smart software that searches for new medicines
Gerard van Westen and his group, together with pharmaceutical company Galapagos, start on developing software that invents new effective molecules. They will receive an NWO LIFT grant of 280,000 euros, of which 63,000 euros will come from Galapagos. The company will also bring its expertise in biology,…
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Gene networks-based mechanistic assessment of drug-induced organ toxicity: a focus on liver and kidney
Drug induced organ toxicity is the main problem of the drug development and drug usage in the clinic. The liver and kidneys are the most sensitive organs towards drug induced toxicity.
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value of semi-physiological models for clearance of renally excreted drugs across the paediatric age range
The kidneys play a major role in the elimination of drugs. In children, the exact age-related physiological changes underlying kidney function remain largely unknown.
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Tom van der Wel
Science
t.van.der.wel@lic.leidenuniv.nl | +31 71 527 3527
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Microvasculature in Microfluidics: matching complexity with compatibility
In vitro disease models play a fundamental role in drug research. They enable the systemic identification and validation of disease mechanisms and the discovery of possible drug targets. However, more than often, drug candidates that are identified in vitro fail in the later clinical stages of drug…
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Affinity
Designing and synthesizing high-affinity ligands for a given drug target have always been among the more important challenges in the drug discovery process.
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system-based pharmacology approach to predict developmental changes in renal drug clearance in children
Promotores: Prof.dr. C.A.J. Knibbe, Prof.dr. M. Danhof, Prof.dr. K. Allegaert (Leuven)
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Polypept(o)ide-based Cylindrical Polymer Brushes as Multifunctional Drug Delivery Systems
The polypept(o)ide hybrid material attracted more and more attention over the past decade by combining the multifunctional characteristics of polypeptides with the shielding characteristics of polypeptoid-pSar possessing similar properties as a shielding material as polvethylene glycol(PEG). Polysarcosine…
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Whole-cell biosensor for label-free detection of GPCR-mediated drug responses in personal cell lines
Source: Biosens Bioelectron, Volume 74, pp. 233-42 (2015)
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Research
The current projects of the Molecular Physiology group focus on proteins of the endocannabinoid system, kinases and antibacterial targets. MSc- and BSc-students can contact Jessica van Krimpen-Kraaijenoord to apply for research internships.
- Admission & Application
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Discovery and exploitation of the transcriptional regulatory system of pectinases in Aspergillus niger
Pectin is a plant cell wall polysaccharide made of mainly D-galacturonic acid (GA) subunits. The potency of the filamentous fungus Aspergillus niger to naturally secrete high amounts of pectinases to degrade pectin has been utilized for the industrial production of pectinases.
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Discovery and development of inhibitors selective for human constitutive proteasome and immunoproteasome active sites
This thesis describes the design and development of subunit‐selective inhibitors of particular catalytically active subunits of human constitutive proteasomes and immunoproteasomes.
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The role of zebrafish (Danio rerio) larvae in developing new drug candidates for treating anxiety, from natural sources
Can zebrafish larvae be used as a behavioural model for screening natural products as potential neurotropic drugs?
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Champion in headwind and predictions
It is a stormy Sunday afternoon, with gusts of a whopping 110 kilometres per hour. Chemist Teun Sweere defies the enormous headwind on his city bike and wins the NK Headwind cycling after 22,5 minutes. A new highlight follows six months later: his PhD defence (14 June).
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Ukraine
This is an Erasmus+ International Credit Mobility project of the Faculty of Sciences with one partner in Ukraine.
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A large-scale crop protection bioassay data set
ChEMBL is a large-scale drug discovery database containing bioactivity information primarily extracted from scientific literature.
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Cannabinoid CB2 receptor ligand profiling reveals biased signalling and off-target activity, Nat. Commun., 2017
The cannabinoid CB2 receptor (CB2R) represents a promising therapeutic target for various forms of tissue injury and inflammatory diseases. Although numerous compounds have been developed and widely used to target CB2R, their selectivity, molecular mode of action and pharmacokinetic properties have…
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Microscale Analytical Tools
Enabling volume-restricted metabolomics using next-generation microscale analytical tools.
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Extra curricular
Are you interested in taking up an extra challenge during your master’s programme? Have you thought about applying for our Summer School programme or are you interested in developing your personal leadership style?
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Vision and Mission
The need for novel drugs as well as innovations in their development and application is as urgent as ever. Below we present our vision , mission, and our key research areas.
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The hunt for selective drugs
How do you ensure that a drug has an effect on the right protein – and nothing else? Chemist Anthe Janssen explored various methods for determining the selectivity of potential medicines. He also looked at the substance BIA 10-2474, after a man died in a French clinical trial in 2016. PhD defence on…
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COMMUNITY: unraveling the regulatory networks in Streptomyces that switch on antibiotic production on demand
Through his project we will unravel the global regulatory networks that control gene expression in Streptomyces bacteria and allow them to properly respond to major changes in the environment; we will then harness this knowledge to activate and identify novel antibiotics
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Alexander Kros
Science
a.kros@chem.leidenuniv.nl | +31 71 527 4234
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Partner Institutes
The IBL represents the core of modern biological research at Leiden and we interact closely with the other life science Partner Institutes in the faculty:
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Laura Heitman appointed as Professor of Molecular Pharmacology
As of 1 November, Laura Heitman has been appointed full Professor of Molecular Pharmacology at the Leiden Academic Centre for Drug Research (LACDR). Heitman has been working on the understanding and improvement of drug-receptor interactions in early drug discovery. ‘My ultimate aim is to make medicines…
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Discovery of a NAPE-PLD inhibitor that modulates emotional behavior in mice, Nat. Chem. Biol. 2020
N-acylethanolamines (NAEs), which include the endocannabinoid anandamide, represent an important family of signaling lipids in the brain. The lack of chemical probes that modulate NAE biosynthesis in living systems hamper the understanding of the biological role of these lipids.
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Covalent inhibitors of G protein-coupled receptors: the case of adenosine receptors
Supervisor: Xue Yang
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About the programme
The two-years MSc programme spans the entire spectrum of Analytical BioSciences, Biopharmaceutics, Drug Delivery Technology, Medicinal Chemistry, Pharmacology and Toxicology.
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New project uses artificial intelligence in drug development
In health care, artificial intelligence is quite normal: it is used, for example, as an aid in making diagnoses. However, artificial intelligence is not yet used as much in drug development. A new prestigious partnership is therefore going to investigate how artificial intelligence can contribute to…
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Career prospects
With an MSc degree in BPS and Science Communication & Society you are well prepared for a broad array of career prospects in research or industry. The master’s degree is an excellent preparation for a career at the interface of science and public affairs.