SCIENCE & TECHNOLOGY

Resistance to standard chemotherapeutic treatments and poor responses to immune-based therapies represent major challenges in cancer treatment as many patients respond poorly or not at all to currently available treatment options.
BiPER Therapeutics aims to bridge this important treatment gap by developing novel therapeutic solutions based on these core principles:
Targeting the global metabolism of cancer cells
Developing First-In-Class drug candidates selectively targeting key proteins involved in metabolism of cancer cells and overcoming treatment resistance and cancer cell survival
Triggering selective death of cancer cells
Demonstrating efficacy and tolerability in vivo in vitro and ex-vivo from freshly isolated patients cells
BiPER Therapeutics science and technology has been rewarded by recognized prizes: INCA, Grand CoPOc, Sanofi e-Award, Grand Prix Académie de Médecine and iLab
Our lead candidate is a first-in-class BiP Inhibitors triggering cancer cell death through induction of unresolved Endosplasmic reticulum stress

Tumors thrive under adverse conditions, such as hypoxia, nutrient starvation, and oxidative stress, by adjusting their protein-folding and homeostasis capacity via overexpression of BiP . Overexpression of BiP is associated with very poor prognosis of patients in a broad range of cancer indications.
BiP is a master regulator of the Endoplasmic Reticulum Stress Pathway and the folding of misfolded proteins
The ER Stress is a key survival and resistance mechanism in cancer cells controlled by BiP as a chaperone of the three ER Stress Effectors

Inhibiting the ER Stress controller function of BiP lead to uncontrolled and unresolved ER Stress activating apoptosis and autophagy, two mechanisms of cancer cell death in tumors
ER Stress plays also an important role in subverting the protective function of innate immune cells in the tumor microenvironment to cripple the development of anti-tumor immunity. Inducing ER Stress re-activate immune-mediated cell death in tumor microenvironement

Compounds Triggering ER Stress Exert Anti-Melanoma Effects and Overcome BRAF Inhibitor Resistance Cancer Cell
Discovery and Optimization of N-(4-(3-Aminophenyl)thiazol-2-yl)acetamide as a Novel Scaffold Active against Sensitive and Resistant Cancer Cells J. Med. Chem. LINK
New anti-cancer molecules targeting HSPA5/BIP to induce endoplasmic reticulum, stress, autophagy and apoptosis Autophagy
Structure activity relationship and optimization of N-(3-(2-aminothiazol-4-yl)aryl)benzenesulfonamides as anti-cancer compounds against sensitive and resistant cells Bioorganic & Medicinal Chemistry Letters
The GRP78/BiP inhibitor HA15 synergizes with mitotane action against adrenocortical carcinoma cells through convergent activation ER stress pathways Molecular and Cellular Endocrinology
Development and in vivo evaluation of fused benzazole analogs of anti-melanoma agent HA15 Future medicinal chemistry