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Towards Multitargeted Ligands as Pain Therapeutics: Dual Ligands of the Cavα2δ-1 Subunit of Voltage-Gated Calcium Channel and the μ-Opioid Receptor
In collaboration with WeLab Barcelona, we report the synthesis and biological activity of novel pain therapeutics, which target both Cavα2δ-1 and MOR. One of these disubstituted pyrrolidines demonstrated an analgesic effect in various rodent models of pain, and a lack of unfavorable off-target interactions, showing no evident signs of withdrawal or tolerance. Click on the link below for a short summary of this publication.
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Innovative macrocycles as powerful Mcl-1 inhibitors
This is a recap of the article “Development of potent Mcl-1 inhibitors: structural investigations on macrocycles originating from a DNA-encoded chemical library screen” published in the Journal of Medicinal Chemistry. Myeloid cell leukemia 1 (Mcl-1) is a protein that plays a crucial role in the regulation of cell survival and cell death. It is part of a family of proteins called the Bcl-2 family, which are known for their involvement in controlling the life span of cells.
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Oncolines unveils new State-of-the-Art Laboratories
In a significant stride towards advancing cancer research and drug development, Oncolines, has officially received the keys to its new laboratories and offices situated within the prestigious Curie Building on the Pivot Park in Oss, the Netherlands.
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Our Article Published in the Journal of Medicinal Chemistry
Symeres is thrilled to announce the publication of a scientific article in the prestigious Journal of Medicinal Chemistry with our colleague Koen Hekking as the main author and many more Symerians involved! We are incredibly proud of our colleagues who were instrumental in the research and development of this innovative project.
Latest patents
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Compounds and their use as PDE4 activators
Number: WO/2024/038129
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Compounds and their use as PDE4 activators
Number: WO/2024/038128
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Crystalline and liquid crystalline 25-hydroxy-cholest-5-en-3-sulfate sodium and methods for preparing same (Organix)
Number: US 2023/0056273 A1
Latest publications
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Towards Multitargeted Ligands as Pain Therapeutics: Dual Ligands of the Cavα2δ-1 Subunit of Voltage-Gated Calcium Channel and the μ-Opioid Receptor
Article: ChemMedChem 2024, e202300473
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High Target Homology Does Not Guarantee Inhibition: Aminothiazoles Emerge as Inhibitors of Plasmodium falciparum
Article: ACS Infect. Dis. 2024, XXXX, XXX, XXX-XXX
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Development of Potent Mcl-1 Inhibitors: Structural Investigations on Macrocycles Originating from a DNA-Encoded Chemical Library Screen
Article: J. Med. Chem. 2024 (67), 3039-3065
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