Researchers from Bienta/Enamine presented a poster during MIPTEC exhibition’2017 in Basel, Switzerland: “Reduced cardiotoxicity of spiro-tetrahydropyran bupivacaine analogues”. The goal of this study was to create active structural analogs of bupivacaine with reduced general and cardiotoxicity due to in silico modifications designed to affect their interaction with Nav1.5 channel, which is believed to be the main target of bupivacaine toxicity.
Sergey Zozulya, V.P. Biology at Enamine, will be a speaker at the 4th year of the Summer Prague School ADVANCES IN DRUG DISCOVERY. Drug Discovery and Development from basic research through preclinical to clinical phases.
The event will take place in Prague, Czech Republic, September 4-8, 2017.
Topics to be covered this year:
- Target discovery
- General chemical approaches – medicinal chemistry
- Structure and In silico based drug design
- Lead structure characterization
- Precinical and clinical development
- Principles and examples of commercial drug development cycleS
- Specific section devoted to personalized medicine and related diagnostic.
The new Integrative Biology and Medicine Conference will be held in Kyiv, October 2-7, 2017. Main topics of the conference are bioinformatics, systems biology, evolution and personalized medicine, and the idea behind is an integrative approach to understanding of life and disease. Top scientists from a variety of biomedical research areas from 10 countries (USA, Great Britain, Canada, Germany, Switzerland, Denmark, Austria, Poland, Estonia and Ukraine) are expected as speakers. The conference is expected to become an informal space for exchanging experience and seeking for collaboration for future projects.
More information and registration available here.
To address rapidly growing demand in in vivo pharmacokinetic and toxicology studies, Bienta is currently building a new animal research facility. The new in vivo research lab will occupy over 500 m2 of lab space, equipped and maintained under highest quality standards. The new facility will be hosting up to 5000 animals (small rodents) and will allow to expand the list of animal testing services provided by Bienta. In particular, it is planned to develop here an array of disease models for studying various types of cancer and diabetes.
The new facility is expected to be launched in 1Q of 2018.
Enamine and the European Molecular Biology Laboratory (EMBL) agreed to a collaboration through which Enamine will provide library synthesis, medicinal chemistry, and biological services for EMBL’s small-molecule cancer drug discovery programs. Enamine will establish a team of full-time equivalent medicinal chemists to work on the project, which is focused on the development of cancer therapeutics with novel mechanisms of action, the organizations state.
EMBL has an existing relationship with Enamine. “We have been working with Enamine for several years, primarily to enhance the chemical space of our internal screening library,” explained Joe Lewis, Ph.D., head of Chemical Biology Core Facility at EMBL. “We realized quickly that their 2 million plus compound collection provides quality compounds allowing an increase in the chemical diversity of our screening deck.”
David Will, Ph.D., head of Medicinal Chemistry at EMBL, added, “This collaboration with Enamine will be pivotal for the success of our project for identifying targets from phenotypic screens and synthesizing and triaging new patentable preclinical compounds. Their agility and flexibility with access to the world’s largest collection of building blocks in stock at Enamine and integration of chemistry with a comprehensive biology service portfolio perfectly fit our goal of nominating a preclinical development candidate by 2018.”
Sergey Zozulya, Bienta’s CTO, participated in 3rd Prague Summer School Advances in Drug Discovery, with the lecture “High-throughput screening of compound libraries”. The School took place in Prague, September 5-9th, 2016, and focused on Drug Discovery and Development, from basic research through preclinical to clinical phases.
From 16.08.2016 to 16.09.2016, Bienta was honoured to host Dr. Alain Géloën, a visiting scientist from University of Lyon, CarMeN Laboratory, INSA de Lyon, France, under the two ongoing Horizon 2020 projects, Peptidomimetics with photocontrolled biological activity, and Carbon-based nano-materials for theranostic application. Alain performed an exciting research using a novel tomographic Nanolive 3D Cell Explorer microscope . Using the microscope, Alain managed to track the fate of carbon-based nanoparticles in cancer cell cultures, as well as made real-time observations of the cell response to the action of the photocontrolled antibiotics. This unprecedented new technology allowes to look into the live cells without damaging them, enabling marker-free and real-time imaging on single cells, cell cultures, cell multilayers and tissue slices.
Enamine/Bienta is participating in EU Horizon 2020 grant-funded program“Peptidomimetics with photocontrolled biological activity” headed by research teams from Karlsruhe Institute of Technology, University of Cambridge, Latvian Institute of Organic Synthesis and Enamine. Bienta’s preclinical biology team is supporting characterization of a photodynamic cancer drug candidate by DMPK and animal efficacy studies. In April 2016, Bienta’s researchers co-authored a prestigious paper on the subject (Babii et al., Angew.Chem.Int.Ed., 2016; 55: 5493-6).
Knowing specific sites and pathways of metabolic transformations is useful for guiding synthetic optimization of lead compounds to overcome stability or toxicity issues commonly occurring in drug discovery. Over the last few years, Bienta’s ADME/mass-spectrometry team has accumulated substantial experience in running efficient and affordably priced Metabolite ID projects to help tackling the challenges of synthetic optimization for Enamine’s clients.
Since the end of 2015, we are offering HitLocator Library (HLL) consisting of 511,360 compounds for contractual HTS campaigns at Bienta.
HLL is a carefully selected representation of the whole Enamine’s collection of more than 2,000,000 chemical compounds. HLL compounds were selected by applying chemical diversity and drug-likeness criteria and using extensive medchem filtering. HLL has an intelligently clustered design consisting of 5 “core” and 12 “radial” sets of 30,080 compounds each, which allows implementing screening strategies customized to the needs and budgets of any academic or industrial client. Bienta has already carried out productive hit finding campaigns on both the subsets and the whole HitLocator Library. HLL hits can be rapidly transformed to leads via hit expansion using the entire 2+ million off-the-shelf compounds, as well as multiple parallel synthesis from Enamine’s RealDatabase and focused Enamine-specific synthetic chemistry.
Bienta has just launched on-site laboratory for in vivo studies in rodents. This new animal facility allows us to continue expanding our services in preclinical toxicology and animal efficacy models, in addition to pharmacokinetics studies in mice and rats that Bienta was successfully offering for the last several years. Our immediate plans include setting up rodent efficacy models for the therapeutic areas of anti-infectives, inflammation and pain.
We will be paricipating in the 7th International Conference on Drug Discovery and Therapy (ICDDT), Sharjah, UAE, February 15th – 18th, 2016.
Bienta has recently supported molecular modeling assessment project ran at Tokyo Institute of Technology, Japan. YES tyrosine kinase targeted library created by 10 competing in silico molecular modeling teams organized by Initiative for Parallel Bioinformatics ( IPAB) was successfully screened by Bienta to identify hits. The library consisting of 600 compounds was selected from Enamine’s Screening Compounds Collection of close to 2,000,000 compounds. Bienta enjoys unlimited and immediate access to the vast Enamine compound repository, allowing prompt and efficient high-throughput screening, hit verification “from powders” and hit expansion follow-ups.
Bienta will be participating at MIPTEC 2014 conference, September 23-25, Basel, Switzerland. Meet us there!
Our team member, Ihor Zahanich, will be presenting a poster “Pharmacological characterization of potent and selective Free Fatty Acid Receptor 1 (FFA1/GPR40) agonists for the treatment of type 2 diabetes”. Author list: Ihor Zahanich, Olexandr Vasylchenko, Yuri Kheylik, Yulia Tokareva, Roman Moriev, Maxim Platonov, Vladimir Iurchenko, Sergey Zozulya. Poster Session (Poster Area) to be held on Wednesday, 24 September 2014 between 17:00h and 18:00h.
Introducing a new technology which is planned to be extensively used for screening projects at Bienta. Differential Scanning Fluorimetry (DSF, TSA) is a powerful biophysical method based on detecting the shifts in protein denaturation temperature upon ligand binding as reported by fluorescent dye interacting with protein core exposed by heat denaturation. DSF is a simple, label-free HTS technology applicable to most soluble proteins, irrespectively of their functions and activities. Now Bienta can provide on-site recombinant target protein production to support DSF-based screening projects.
You are welcome to visit our booth and meet representatives of Enamine&Bienta Sales team at ASMC 2013 (5 – 8 May) (more…)
A collaboration agreement has been signed between Enamine, the Medical Research Council Laboratory of Molecular Biology (MRC LMB), Cambridge, UK, and the Institute of Organic Chemistry and Biochemistry of the Academy of Sciences of the Czech Republic (IOCB), Prague, Czech Republic. (more…)
Enamine announces opening of contract biology laboratory at its main research site in Kyiv, Ukraine. Enamine’s BioLab will be providing ADMET (absorption, distribution, metabolism, excretion and toxicity) and biomolecular screening services to expand Enamine’s chemistry-driven CRO capabilities into the biological support of early phase drug discovery projects. (more…)