ToBeLi-for-GPR3-6-12
Financiado
Towards high-affinity ligands for orphan receptors GPR3, GPR6 & GPR12
The family of G protein-coupled receptors (GPCRs) comprises more than 800 human cell surface receptors that perceive and transmit extracellular stimuli into the cell interior. Due to their involvement in numerous biochemical proce...
The family of G protein-coupled receptors (GPCRs) comprises more than 800 human cell surface receptors that perceive and transmit extracellular stimuli into the cell interior. Due to their involvement in numerous biochemical processes, GPCRs represent prime targets for the treatment of various diseases and are modulated by more than 30% of approved drugs today. However, a large proportion of the druggable GPCRome remains pharmacologically untapped, including the so-called ‘orphan’ GPCRs (oGPCRs) - receptors for which the endogenous ligands remain unknown.GPR3, 6 and 12 constitute a cluster of orphan GPCRs that is involved in numerous (patho-)physiological processes including neurodegenerative disorders such as Parkinson’s and Alzheimer’s dementia. GPR3 and GPR12 further mediate meiotic arrest in oocytes and suppress the development of metabolic diseases. Other physiological processes and diseases associated with GPR3/6/12 are neuropathic pain perception, addiction and different forms of cancer. Although these receptors represent promising pharmacological targets and researchers have been trying to discover molecules targeting these receptors for more than two decades, only a limited set of five ligands is currently available. Modern GPR3/6/12-targeted drug discovery is still hampered by the lack of verified endogenous ligands, our poor understanding of their structural organization and signalling cascades promoted by these receptors, and a limited panel of assays revealing GPR3/6/12 activity in living cells.Here, I propose to implement an interdisciplinary research approach combining computational methodologies with advanced biosensor technology in order to discover advanced ligands for these attractive drug targets. These novel compounds will aid in developing advanced therapeutics tackling severe human diseases and our reseach will highlight the power of interdisciplinary drug discovery approaches, promoting their implementation in the GPCR field and beyond.
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Duración del proyecto: 25 meses
Fecha Inicio: 2022-06-01
Fecha Fin: 2024-07-31
Fecha Fin: 2024-07-31
Línea de financiación: concedida
El organismo HORIZON EUROPE notifico la concesión del proyecto el día 2024-07-31
Línea de financiación objetivo
El proyecto se financió a través de la siguiente ayuda:
HORIZON-MSCA-2021-PF-01-01:
MSCA Postdoctoral Fellowships 2021
Cerrada
hace 3 años
Líder del proyecto
PHILIPPS UNIVERSITAET MARBURG
No se ha especificado una descripción o un objeto social para esta compañía.
Perfil tecnológico
TRL
4-5
Perfil tecnológico
TRL
4-5