PI3K/AKT/mTOR Pathway Inhibitor Development

PI3K/AKT/mTOR Pathway Inhibitor Development

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.

Introduction to PI3K/AKT/mTOR Pathway Inhibitor for Breast Cancer

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)Fig. 1 Signaling by the PI3K/AKT/mTOR pathway and the respective inhibitors. (Li H., et al. 2021)

PI3K/AKT/mTOR Pathway Inhibitor Development for Breast Cancer

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

Our Services

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

Our Therapeutics Development Platform for PI3K/AKT/mTOR Inhibitors Development

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.

Reference

  1. Li H., Prever L., and et al. Targeting PI3K/AKT/mTOR Signaling Pathway in Breast Cancer. Cancers 2021, 13, 3517.
All our services and products are exclusively intended for preclinical research purposes. They are not intended for diagnostic, therapeutic, or patient management applications.