Empowering Phosphatase Drug Discovery
Nerio is building a new generation of therapeutics targeting protein phosphatases for immunotherapy
Empowering Phosphatase Drug Discovery
Nerio is building a new generation of therapeutics targeting protein phosphatases for immunotherapy
About
Hundreds of protein phosphatases have yet to be targeted with small molecules, offering a rich opportunity to discover novel therapeutics.
Protein phosphatases constitute a large family of signaling enzymes that operate primarily through a mechanism of substrate-selective dephosphorylation. By contrast, kinases phosphorylate proteins. Together, these posttranslational mechanisms work in concert to tune cellular regulatory networks.
While kinases have garnered considerable success as drug targets with over 70 approvals, successful phosphatase programs have remained elusive due to challenges associated with the inability to selectively target the catalytic domain of these enzymes. Historically, most small molecule phosphatase inhibitors that have been identified suffer from lack of bioavailability, cell penetration and poor phosphatase selectivity. However, recent advances in the field have shown that successful phosphatase inhibitor development can be achieved.
Nerio is focused on identifying highly selective, competitive inhibitors and pioneering the discovery of allosteric and uncompetitive phosphatase modulators.
Approximately 200 protein phosphatases are encoded in the human genome which are largely untapped as therapeutic targets. Nerio is pursuing the potential for therapeutic intervention with selective, cell-permeable, bioavailable, and efficacious small molecule phosphatase modulators.
About
Hundreds of protein phosphatases have yet to be targeted with small molecules, offering a rich opportunity to discover novel therapeutics.
Protein phosphatases constitute a large family of signaling enzymes that operate primarily through a mechanism of substrate-selective dephosphorylation. By contrast, kinases phosphorylate proteins. Together, these posttranslational mechanisms work in concert to tune cellular regulatory networks.
While kinases have garnered considerable success as drug targets with over 70 approvals, successful phosphatase programs have remained elusive due to challenges associated with the inability to selectively target the catalytic domain of these enzymes. Historically, most small molecule phosphatase inhibitors that have been identified suffer from lack of bioavailability, cell penetration and poor phosphatase selectivity. However, recent advances in the field have shown that successful phosphatase inhibitor development can be achieved.
Nerio is focused on identifying highly selective, competitive inhibitors and pioneering the discovery of allosteric and uncompetitive phosphatase modulators.
Approximately 200 protein phosphatases are encoded in the human genome which are largely untapped as therapeutic targets. Nerio is pursuing the potential for therapeutic intervention with selective, cell-permeable, bioavailable, and efficacious small molecule phosphatase modulators.
Science
PTPN2/N1: Intracellular Checkpoints of Inflammation
The protein tyrosine phosphatases PTPN2 and PTPN1 function as negative regulators of cytokine signaling and T cell receptor signaling and have recently emerged as potent immunotherapy targets. Published studies have shown that deletion or small molecule inhibition of PTPN2 or PTPN1 drive enhanced anti-tumor activity in multiple preclinical models.
Nerio PTPN2/N1 Inhibitors for Immunotherapy
Nerio has developed novel, potent and highly selective PTPN2/N1 inhibitors with excellent drug-like properties. Nerio’s best-in-class PTPN2/N1 inhibitors enhance immune function as well as sensitize tumors to proinflammatory signals. In preclinical tumor models, Nerio’s compounds reshape the immune landscape of the tumor microenvironment and drive robust anti-tumor activity as a monotherapy as well as in combination with a checkpoint inhibitor. Nerio anticipates an IND submission for its lead asset in 2H 2024.
Science
PTPN2/N1: Intracellular Checkpoints of Inflammation
The protein tyrosine phosphatases PTPN2 and PTPN1 function as negative regulators of cytokine signaling and T cell receptor signaling and have recently emerged as potent immunotherapy targets. Published studies have shown that deletion or small molecule inhibition of PTPN2 or PTPN1 drive enhanced anti-tumor activity in multiple preclinical models.
Nerio PTPN2/N1 Inhibitors for Immunotherapy
Nerio has developed novel, potent and highly selective PTPN2/N1 inhibitors with excellent drug-like properties. Nerio’s best-in-class PTPN2/N1 inhibitors enhance immune function as well as sensitize tumors to proinflammatory signals. In preclinical tumor models, Nerio’s compounds reshape the immune landscape of the tumor microenvironment and drive robust anti-tumor activity as a monotherapy as well as in combination with a checkpoint inhibitor. Nerio anticipates an IND submission for its lead asset in 2H 2024.
Team
Nerio is led by an experienced biopharmaceutical team with deep scientific expertise.
Sanford (Sandy) Madigan, Ph.D.
Co-Founder and Chief Executive Officer
Sergio Duron, Ph.D.
Co-Founder and Chief Scientific Officer
Eben Massari, Ph.D.
Senior Vice President of Biology
Jason Roland, Ph.D.
Co-Founder and Vice President of Chemistry
Jay B. Lichter, Ph.D.
Board Member
Tighe M. Reardon, CPA
Board Member
Stefan Heller, Ph.D.
Board Member
Nunzio Bottini, MD, Ph.D
Academic Founder and Advisor
Stephanie Stanford, Ph.D
Advisor
Sanford (Sandy) Madigan, Ph.D.
Board Member
