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The phosphoinositide 3-kinase (PI3K)/protein kinase B (AKT)/mammalian target of rapamycin (mTOR) signaling pathway is a central regulator of cellular processes such as proliferation, growth, differentiation, and survival. At Alfa Cytology, we specialize in developing novel molecules targeting the PI3K/AKT/mTOR pathway for breast cancer therapy.
The PI3K/AKT/mTOR pathway is a highly interconnected signaling cascade that plays a crucial role in regulating various cellular functions. It is initiated by the activation of PI3K, a lipid kinase that phosphorylates the membrane lipid phosphatidylinositol-4,5-bisphosphate (PIP2) to generate phosphatidylinositol-3,4,5-trisphosphate (PIP3). PIP3 acts as a second messenger, recruiting and activating the serine/threonine kinase AKT. Activated AKT then phosphorylates a myriad of downstream effectors, including the mTOR complex.
Fig.1 Signaling by the PI3K/AKT/mTOR pathway and the respective inhibitors. (Li H., et al. 2021)
In breast cancer, the PI3K/AKT/mTOR pathway is frequently hyperactivated due to a variety of genetic and epigenetic alterations. The overactivation of this pathway contributes to the hallmarks of cancer, such as uncontrolled cell proliferation, evasion of apoptosis, and metabolic reprogramming. Moreover, the PI3K/AKT/mTOR pathway has been implicated in the development of resistance to various breast cancer therapies, including chemotherapy, targeted agents, and endocrine therapy. This highlights the urgent need for the development of novel therapeutic strategies that effectively target this critical signaling pathway.
| NCT | Target | Study | Phase |
| NCT01610284 | Class I P13K-p110α | BELLE-2 | |
| NCT01992952 | AKT | FAKTION | |
| NCT00863655 | mTOR1 | BOLERO-2 | |
| NCT00083993 | mTOR | HORIZON |
As a leading preclinical CRO, Alfa Cytology is committed to advancing the development of innovative cancer therapies, including PI3K/AKT/mTOR targeted inhibitors for breast cancer. Our state-of-the-art facilities and multidisciplinary team of experts provide comprehensive services to support the entire drug development process, from target identification and validation to preclinical studies and biomarker development.
| Our Small Molecule Inhibitors Development | Descriptions |
| PI3K/AKT/mTOR Targeted Agent Development | Pan-PI3K Inhibitor Development Isoform-Specific PI3K Inhibitor Development AKT Inhibitor Development mTOR Inhibitor Development |
| Co-targeting Inhibitors with the PI3K/AKT/mTOR Pathway | PI3K/PARP Inhibitor Development PI3K/Hsp90 Inhibitor Development PI3K/BTK Inhibitor Development PI3K/HDAC Inhibitor Development |
| Allosteric Inhibitors for the PI3K/AKT/mTOR Signaling Pathway | Allosteric AKT Inhibitor Development Allosteric mTOR Inhibitor Development |
| Covalent Inhibitors for the PI3K/AKT/mTOR Signaling Pathway | Selective covalent Inhibitor Development of PI3K Covalent allosteric AKT Inhibitor Development Selective mTOR Inhibitor Development |
| PROTACs in the PI3K/AKT/mTOR Pathway | PROTAC-based PI3K Degrader Development PROTAC-based AKT Degrader Development |
Building on our extensive expertise in breast cancer research, our therapeutics development platform for PI3K/AKT/mTOR inhibitors aims to accelerate the discovery and development of innovative therapies targeting critical pathways in cancer progression.
Alfa Cytology provides development services for PI3K/AKT/mTOR inhibitors, covering drug design, screening, and efficacy research to find ideal drug candidates for you and accelerate preclinical research on your breast cancer therapeutics. To learn more about our capabilities in PI3K/AKT/mTOR inhibitor development for breast cancer or to discuss potential collaborative opportunities, please don't hesitate to contact us.
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