Aileron & Roche in Stapled Peptides Pact

Roche has agreed to pay up to $1.1 billion for access to technology at Aileron Therapeutics, a tiny Cambridge, Mass.-based biotech focused on developing stapled peptides. As part of the deal, Roche and Aileron will develop drug candidates against five targets. Stapled peptides make intriguing drug candidates for their ability to access previously intractable targets. As we’ve described: Protein-embedded α-helices mediate key protein handshakes in cancer, HIV, and other diseases. But actually using an α-helix as a drug has proven tricky. So-called stapled α-helices, boasting sturdy cross-links between nonnatural amino acid side chains, just might change that. This class of stabilized peptides can regulate signaling pathways to subvert cancer. They also appear to overcome several of the usual problems that have hampered the development of peptide drugs. Stapled peptides are locked into the biologically active shape, enabling the drug to penetrate the cell and bind tightly to protein surfaces. Last fall, Harvard chemical biologist and Aileron’s scientific founder Gregory L. Verdine and colleagues showed the helix-stabilizing strategy could be used to turn off the Notch transcription factor complex, a master cell regulator in cancer that has gone awry in over half of patients with a certain type of leukemia. It was the first direct inhibitor of the Notch complex. Aileron gets $25 million upfront and R&D funding, but could score a bounty in milestones if drug candidates against all five targets reach the market. Roche was clearly keeping close tabs on the technology. The Swiss pharma firm’s corporate venture fund was one of several big pharma funds to invest in the $40 million round raised by Aileron last summer.

Author: Lisa Jarvis

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