Latvian Institute of Organic Synthesis
Paragraphs
Natalion

Latvian Institute of Organic Synthesis

Author
LIOS

March 21, 2023

Latvian Institute of Organic Synthesis (LIOS) is the leading drug discovery and development centre in the Baltics. LIOS has more than 65 years of experience in drug design and technology development. LIOS delivered 18 original and more than 100 generic medicines to our industrial partners. LIOS has been announced the best research institute in Latvia according to the last two instances of “International evaluation of scientific institutions activity”.

LIOS focuses on research providing solutions to important societal challenges (public health with drug discovery and development as a core competence as well as sustainable chemistry and technology). The research results of LIOS has a significant impact not only at the local but also at the international level.

LIOS researchers perfom basic and applied research in organic, biophysical,bioorganic, medicinal and process chemistry, in vitro and in vivo pharmacology and natural product research.

Research and innovation funding programme Horizon Europe projects:

# Test Project ID Implementation period: Total budget:
1. Fragment-Screen: From fragments to high affinity binders interfacing integrated structural biology, medicinal chemistry and artificial intelligence. 101094131 01.02.2023. – 31.01.2026. € 8 265 079,64 (EU contribution), LIOS budget € 217 600,00 (EU contribution)
2. Natalion: Natural Products Research at Latvian Institute of Organic Synthesis as a driver for Excellence in Innovation. 101087181 01.01.2023. – 31.12.2027. € 2 499 950 (EU contribution), LIOS budget € 2 499 950,00 (EU contribution)
3. Remote NMR (R-NMR): Moving NMR infrastructures to remote access capabilities. 101058595 01.07.2022 – 30.06.2025. € 1 350 000 (EU contribution), LIOS budget € 37500 (EU contribution)
4. ISIDORe: Integrated Services for Infectious Disease Outbreak Research. 101046133 01.02.2022. – 31.01.2025. € 20 998 624,00 (EU contribution), LIOS budget € 88406 (EU contribution)

LIOS has established a drug discovery and preclinical development (LIOS-DD) platform that consolidates the complementary expertise of LIOS research groups and the supporting infrastructure. The integrated expertise of  the platform consists of  3 major modules:

1. Discovery of drug candidates including a target identification and validation as well as range of tools for drug discovery (synthetic hit-to-lead & lead optimization, in silico drug design, structural biology assisted drug design, biochemical & biophysical screening, fragment based lead discovery, natural product inspired lead discovery)

2. Preclinical development including ADME, DMPK and safety testing and in ex vivo and in-vivo testing on a wide range of  desease models ,

3. Manufacturing technologies including route scouting, upscale, kg-scale synthesis and GMP-analytics

The focus areas at LIOS are discovery and development of:  

  1. antitumor agents,
  2. novel treatment for cardiometabolic disorders, 
  3. antibacterial, antiviral and antimalarial therapy, 
  4. therapies for the treatment of neurological disorders.

Infrastructure

1. Medicinal/organic chemistry infrastructure (3000 m2)

Hoods for synthetic chemistry with inert gas supply, vacuum pumps, routine equipment for synthesis and sample processing, parallel synthesis carousel stations, flow reaction systems, microwave synthesizer, preparative flash chromatographs with fraction collectors, UV and ELSD detectors, mass-triggered preparative HPLC-systems, preparative HPLC/UV systems  with sample evaporation systems, analytical HPLC/UV and UPLC/UV systems, analytical LC/SQ-MS systems, GC/MS systems, glovebox for handling of air/moisture sensitive materials, solvent purification stations, MestRenova NMR processing software, ChemDraw Professional 15.1 software, electronic laboratory notebooks, reagent and building block stock with ≈10’000 chemicals, both commercial and in-house prepared, Shroedinger and PyMole software and 120CPU/20GPU cluster.

2. Pharmacology infrastructure (800 m2 )

Cell cryopreservation and storage, cell culture maintenance, monitoring and visualization, including Stimulated Emission Depletion (STED) Microscopy facility, fluorescence, absorbance and luminescence microplate reader, radiolabelled laboratory materials and multi-detector instruments, non-invasive blood pressure, heart rate and ECG measurement, echocardiography, isoflurane inhalation system, small animal surgery equipment, blood sampling equipment, metabolic cages, traumatic brain injury and behavioural study setup, systems for high-resolution respirometry in mitochondrial physiology and pathology.

3. Biophysical and biooorganic chemistry infrastructure (600 m2) 800 MHz NMR (solution state HCN-probe, solid state probe), 600 MHz NMR (solution state HCN-probe, cryoprobe) systems, facility for protein expression in E.coli, insect and mamalian cells,  Surface Plasmon Resonance spectrometer, isothermal titration calorimeter, microscale thermophoresis (MST), thermal shift, and grating-coupled interferometry.

4. Centrally operated (core facility) analytical chemistry infrastructure (700 m2)

NMR systems – 400MHz (autosampler, solution state BB-probe), 300MHz (open access, autosampler), powder and single crystal X-ray diffractometers, Synapt GII q-ToF HRMS system with UPLC front-end, IT-ToF HRMS system with UPLC front-end, Quattro Micro, Xevo TQ-S, micro-TQ-S tandem mass-spectrometers with UPLC front-end with bioanalytical sample preparation equipment set, analytical HPLC-systems with UV, PDA, fluorescence, ELS detectors, polarimeter, GC-based microanalysis systems, FT-IR spectrometer with spectra library, GC/FID system.

5. Kilo-scale facility (150 m2)

Reactors and work-up stations for up to 63 L, Parr pressure reactor 25 L / 20 bar,  Parr pressure reactor 1.2 L / 200 bar, Rotary evaporator 20 L,  VTA Wiped-Film Evaporator (0.04-5 kg/hour), Centrifuge (14 L, 2500rpm),  PTFE pressure filters 40 L and 2 L, Shelf dryer 30 L.

6. Informational sources

Sci-Finder and Scopus data bases, subscription to main Organic and Medicinal chemistry journals.

Leading Researchers:

  1. Emilio Parisini, prof., Dr.chem., h-indekss 33 , ORCID 0000-0002-5529-0039 , Scopus ID 24756652800
  2. Maija Dambrova, prof., Dr.pharm, h-indekss 29 , ORCID 0000-0002-1739-0928 , Scopus ID 6603578804
  3. Edgars Liepiņš, Dr.pharm, h-indekss 27 , ORCID 0000-0003-2213-8337 , Scopus ID 7003732967
  4. Kristaps Jaudzems, prof., Dr.chem., h-indekss 22 , ORCID 0000-0003-3922-2447, Scopus ID 26535963800
  5. Pāvels Arsenjans, Dr.chem., h-indekss 21, ORCID 0000-0001-5875-2799, Scopus ID 7003485154
  6. Edgars Sūna prof., Dr.chem., h-indekss 19, ORCID 0000-0002-3078-0576, Scopus ID 6602322879
  7. Raivis Žalubovskis, asoc. prof., Dr.chem., h-indekss 19, ORCID 0000-0002-9471-1342, Scopus ID 6504802560
  8. Aigars Jirgensons, prof., Dr.chem., h-indekss 17, ORCID 0000-0002-8937-8792, Scopus ID 6505796562
  9. Sizovs Antons, Dr.chem., h-indekss 17, ORCID 0000-0001-6495-6317, Scopus ID 36635180600
  10. Līga Zvejniece, Dr.med., h-indekss 17, ORCID 0000-0003-4576-2386, Scopus ID 6507099649
  11. Liene Grigorjeva, Dr.chem., h-indekss 14, ORCID 0000-0003-3497-6776, Scopus ID 37090860500
  12. Bobrovs Raitis, Dr.chem., h-indekss 9, ORCID 0000-0002-0221-8658, Scopus ID 41560942300
  13. Jānis Veliks, Dr.chem., h-indekss 8, ORCID 0000-0003-0955-8257, Scopus ID 56373294500
  14. Gints Šmits, Dr.chem., h-indekss 8, ORCID 0000-0001-5044-4169, Scopus ID 55850540300
  15. Dace Rasiņa, Dr. chem., h-indekss 8, ORCID ORCID 0000-0002-7788-7100, Scopus ID 56682055100

More information: https://www.osi.lv/en/