Aileron's history

1970's - 1990's
Peptides gained popularity as a potential superclass of drugs for a plethora of extracellular targets and related diseases. However, by the late-1980s and 1990s there was a major shift toward highly modified, small-sized peptidomimetics with hope that such molecules might overcome the metabolic instability (by proteases) and ultra-short pharmacokinetic (half-life) properties of peptides

2000
June – G.L. Verdine et.al. publish the first hydrocarbon cross-linking system for stabilizing peptides in the Journal of the American Chemistry Society

2004
September – L.D. Walensky, G.L. Verdine, S.J. Korsmeyer and colleagues publish in Science the activation of BCL-2 mediated apoptosis in vivo with a BH3 stapled peptide

2005
June – Aileron founded to pursue stapled peptides with initial funding from Apple Tree Partners
December – Robert H. Grubbs awarded the Nobel Prize in Chemistry along with Richard R. Schrock and Yves Chauvin for work in the field of olefin metathesis, specifically the Grubbs Catalyst

2006
August – Aileron acquires exclusive rights from Harvard and the Dana-Farber Cancer Institute to develop and commercialize a drug discovery pipeline based on Stapled Peptides
December – Aileron acquires rights from Materia to utilize key catalysts, including the Nobel prize-winning Grubbs metathesis, in the development of Aileron’s products
P.S. Arora and colleagues published several key advances advancing the chemical synthesis of stapled peptides

2008
February – Aileron acquires exclusive rights from NYU for additional methods to stabilize peptides and peptidomimetics to develop and commercialize Aileron’s pipeline
October – L.D. Walensky and colleagues published in Nature the identification and activation of a novel trigger site on the death protein BAX using a novel “BIM-SAHB” stapled peptide
December – Aileron and collaborating investigators from the Dana-Farber Cancer Institute present multiple preclinical studies on stapled peptide drug candidates at the American Society of Hematology meeting

2009
March – Aileron receives grant funding from the Multiple Myeloma Research Foundation for the development of stapled peptides with potential in treating multiple myeloma
June – Aileron closes $40 million Series D lead by SR One Ltd., and Excel Venture Management, with unprecedented participation from four pharmaceutical venture funds (SR One, Novartis Venture Fund, Lilly Ventures and Roche Venture Fund)
November – Aileron collaborators J.E. Bradner and G.L. Verdine publish in Nature in vivo research using a stapled peptide to achieve the first direct inhibition of the Notch1 transcription factor oncogene

2010
Aileron creates a molecular armamentarium of Stapled Peptide drugs for protein-protein target space across multiple therapeutic areas leveraging sophisticated drug design, innovative chemistry, production-scale synthesis, biophysical and cell-based proprietary methods to become the world leader in creating a new modality in synthetic biologics to fight disease.
August – Aileron and Roche enter first industry collaboration for Stapled Peptide technology, a multi-target alliance worth up to $1.1 billion to develop Stapled Peptide drugs for diseases across multiple therapeutic areas