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Nuevos compuestos moduladores del complejo enzimático AMPK para el tratamiento del cáncer de próstata andrógeno-independiente

Resumen

Tipo:
Oferta Tecnológica
Referencia:
TOES20161229001
Publicado:
17/01/2017
Caducidad:
17/01/2018
Resumen:
Un centro público español de investigación ha sintetizado una familia de compuestos que actúan como activadores de la proteína quinasa AMPK. Los resultados protegidos muestran que estos derivados ejercen una potente acción antitumoral contra células del cáncer de próstata, ofreciendo una prometedora estrategia terapéutica clínica para el tratamiento del cáncer de próstata andrógeno-independiente. Se buscan compañías farmacéuticas interesadas en desarrollar estos compuestos bajo licencia de patente.

Details

Tittle:
New compounds that modulate the AMPK enzymatic complex for the treatment of androgen-independent prostate cancer
Summary:
A Spanish public research organisation has synthetized a family of compounds which act as activators of protein kinase AMPK. The protected results show that these derivatives exert potent antitumoral actions against prostate cancer cells, indicating a promising clinical therapeutic strategy for the treatment of androgen-independent prostate cancer.

Pharmaceutical companies interested in the development of these compounds under a patent licence are sought.
Description:
The cellular metabolic sensor AMP-activated protein (AMPK) has emerged as a key therapeutic target for many cancer types as it controls the metabolic pathways that are usually reprogrammed in cancer cells. This is especially significant in prostate cancer in which increased lipid synthesis allows the survival of cancer cells and is associated with tumor progression.
A hallmark of prostate cancer is the increased de novo fatty acid and cholesterol synthesis which correlates with tumor progression and poorer prognosis. Thus, targeting these upregulated pathways with inhibitors of key enzymes and associated molecular regulators or by downregulation of lipogenic genes may be a favorable strategy whereby the properties of prostate cancer cells can be exploited for therapeutic gain. Considering the role of the AMPK as a sensor of cellular energy status, the AMPK modulation appears as a promising approach to develop new therapeutic strategies for cancer prevention and treatment.

Pharmaceutical companies interested in the development of these compounds under a patent licence are sought.
Advantages and Innovations:
¿ The most representative compound notably increased Thr172 AMPK phosphorylation and augmented ACC phosphorylation in cultured LNCaP and PC-3prostate cancer cells
¿ The compound caused LNCaP and PC-3 cells viability inhibition and decreased the expression of the cell cycle-related protein Cyclin D1
¿ Selective knocking down of a1 or a2 isoforms, as well as in vitro assays using human recombinant a1-Y-beta;1¿1 or a2-Y-beta;1¿1 AMPK isoforms, revealed that the most representative compound exhibit preference for AMPK a1
¿ Consistent with its in vitro activity the compound was efficacious in suppressing the growth of PC-3 xenograft tumors in nude mice
¿ Compound-treated tumors had increased levels of both phosphorylated AMPK and ACC
Stage of Development:
Field tested/evaluated
IPs:
Patent(s) applied for but not yet granted
CommeR Statunts Regarding IPR Status:
Spanish priority patent application

Partner sought

Type and Role of Partner Sought:
Pharmaceutical companies interested on the development of new drugs for the treatment of androgen-independent prostate cancer.
from preclinical phase or a SME that carries out at least preclinical phase with the ultimate aim of seeking sublicensees.

Client

Type and Size of Client:
R&D Institution
Already Engaged in Trans-National Cooperation:
No
Languages Spoken:
English
Spanish

Keywords

Technology Keywords:
06001003 Citología, cancerología, oncología
06001015 Productos farmacéuticos / medicamentos