CS

Institute of Organic Chemistry
and Biochemistry of the CAS

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PhD projects at IOCB Prague 2025 – Call for applications
PhD projects at IOCB Prague 2025 – Call for applications
9 January 2025
We are looking for talented, independent, and highly motivated PhD students with an MSc. degree or equivalent in life sciences or related fields.
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New drug discovery could help lower cholesterol
New drug discovery could help lower cholesterol
20 February 2025
High cholesterol and fatty liver disease are growing health concerns worldwide, often linked to unhealthy dietary habits and lifestyle choices. But what if we could precisely…
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Scientists from CIIRC CTU and IOCB Prague lead a benchmarking effort for AI-driven discovery of molecules
Scientists from CIIRC CTU and IOCB Prague lead a benchmarking effort for AI-driven discovery of…
18 February 2025
In April 2024, brothers Roman and Anton Bushuiev from the teams of Tomáš Pluskal at IOCB Prague and Josef Šivic at CIIRC CTU initiated a collaboration between experts from 14…
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Event calendar

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19
MAR
Invited Lecture – Henrik Ottosson
19 March 2025, IOCB Prague
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15
APR
Invited Lecture – Cristina Alberini
15 April 2025, IOCB Prague
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28
APR
mzmine Community Meeting 2025
28 April — 29 April 2025, IOCB Prague
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13
MAY
Invited Lecture – Nicolai Cramer
13 May 2025, IOCB Prague
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Take the step towards a career in organic chemistry and biochemistry...
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Publications

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Discovery of Orally Available Prodrugs of Itaconate and Derivatives
Discovery of Orally Available Prodrugs of Itaconate and Derivatives
C. B. Lee I. Šnajdr L. Tenora J. Alt S. Gori M. Krečmerová R. M. Maragakis J. Paule S. Tiwari J. Iyer R. Talwar L. Garza P. Majer B. S. Slusher R. Rais
Journal of Medicinal Chemistry 68 (3): 3433–3444 (2025)
Itaconate, an endogenous immunomodulator from the tricarboxylic acid (TCA) cycle, shows therapeutic effects in various disease models, but is highly polar with poor cellular permeability. We previously reported a novel, topical itaconate derivative, SCD-153, for the treatment of alopecia areata. Here, we present the discovery of orally available itaconate derivatives for systemic and skin disorders. Four sets of prodrugs were synthesized using pivaloyloxymethyl (POM), isopropyloxycarbonyloxymethyl (POC), (5-methyl-2-oxo-1,3-dioxol-4-yl) methyl (ODOL), and 3-(hexadecyloxy)propyl (HDP) pro-moieties pairing with itaconic acid (IA), 1-methyl itaconate (1-MI), and 4-methyl itaconate (4-MI). Among these, POC-based prodrugs (P2, P9, P13) showed favorable stability, permeability, and pharmacokinetics. Notably, P2 and P13 significantly inhibited Poly(I:C)/IFNγ-induced inflammatory cytokines in human epidermal keratinocytes. Oral studies demonstrated favorable pharmacokinetics releasing…
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Small-molecule activators of NRF1 transcriptional activity prevent protein aggregation
J. Sedláček Z. Šmahelová M. Adámek D. Šubová L. Svobodová A. Kadlecová P. Majer A. Machara K. Grantz Šašková
Biomedicine & Pharmacotherapy 183: 117864 (2025)
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Using environment-sensitive tetramethylated thiophene-BODIPY fluorophores in DNA probes for studying effector-induced conformational changes of protein–DNA complexes
M. Šoltysová P. Güixens-Gallardo I. Sieglová A. Soldánová V. Krejčiříková M. Fábry J. Brynda P. Khoroshyy M. Hocek P. Řezáčová
RSC Chemical Biology 2025: Early View
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