Download Tieӧs Pharmaceuticals uses Cyclica`s platform to discover novel

Tieӧs Pharmaceuticals uses Cyclica’s
platform to discover novel cancer drugs
“We engaged Cyclica with a revolutionary idea that, if successful, has significant impact in the
field of oncology. By using their platform, our goal was to computationally create the first
molecules thought to address multiple cancer specific metabolic pathways simultaneously. I
strongly believe Cyclica is the future of drug discovery and development.”
-
Dr. Andrew Roberts, MD, Co-founder and President at Tieӧs Pharmaceuticals
Challenge
There is an overwhelming need to formulate and supply low cost, low toxicity, and effective anticancer therapeutics. Tieös is focused on challenging the current cancer paradigm by developing
novel small molecule inhibitors that can be used to target metabolic behaviors unique to cancer
cells. By achieving this, Tieös will help fill a growing void by providing patients with treatment
options that will actively improve function, tolerability, and ultimately lead to tangible mortality
benefits for patients.
While the idea of using metabolic inhibitors to treat cancer is not entirely new, the targeted
interruption of relevant targets has had little success. The challenges facing the development of
a targeted agent include: 1) delivery into cancer cells specifically and 2) ensuring specificity for
desired targets.
Tieös has devised a unique strategy to address the issues with previous attempts. Tieös’
solution fit perfectly with Cyclica’s Ligand Express™ technology. Together, Cyclica and Tieos
undertook a project to design therapeutic agents that overcome pitfalls observed with other
agents.
“What we gained through this engagement exceeded our
expectations and helped us save years of R&D.”
- Dr. Andrew Roberts, MD, Co-founder and President at Tieӧs
Solution
To help discover novel small molecule inhibitors that target metabolic pathways common to
many variations of cancer, Tieös utilized Cyclica’s Ligand Express™ platform and other
proprietary software. Cyclica generated lead molecules for Tieös, which thanks to its
technology, was produced faster and at a lower cost to conventional approaches. As Dr.
Andrew Roberts remarked, “What we gained through this engagement exceeded our
expectations and helped us save years of R&D.”
Cyclica focuses on the development of new computational approaches for predictive informatics
in drug discovery. Specifically, Cyclica focuses on anticipating the polypharmacology of a drug
and its resulting biological effects, which is meaningful information to utilize when developing a
therapeutic. In utilizing Ligand Express™, Tieös was able to explore the entire structurally
characterized proteome, including cell-metabolism proteins, and predict likely ligand-protein
interactions for carefully selected query ligands.
Determining the full landscape of probable protein targets provided key insights for furnishing
agents with promising pharmacological profiles. Additional tools featured on Cyclica’s platform
streamlined the development of new chemical entities for Tieös, which were iteratively designed
to possess polypharmacological profiles befitting a molecule that targets cancer cell
metabolism.
Results
Tieös will explore the proposed polypharmacological agents developed through Cyclica’s Ligand
Express and confirm their anti-tumour activity. If successful, the outcome of this project can
have substantial impact on human health and may even impact the way drugs are designed in
the future.