On October 11, 2017 Janpix Inc., a privately held biopharmaceutical company dedicated to the discovery and development of inhibitors targeted to Signal Transducer & Activator of Transcription (STAT) proteins, reported that it has closed a US $19M investment round led by Medicxi, a GSK and J&J backed venture fund, which initially seeded the company (Press release, Janpix, OCT 11, 2017, View Source [SID1234530950]).
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Armed with a new understanding of how these proteins can simultaneously impact tumors as well as the tumor micro-environment, the company is advancing selective, small molecule inhibitors of STAT proteins, originally discovered at the University of Toronto Mississauga (UTM), towards clinical development.
STAT proteins, in particular STAT 3 and STAT 5, play a key role in regulating cell cycle, apoptosis, and proliferation, and it is widely recognized that their up-regulation is implicated in a number of solid and hematological cancers. More recent research suggests that inhibition of STAT proteins has also a profound impact on the tumor microenvironment, which offers the potential for these inhibitors to have a dual impact on tumors.
Until now, though, STAT proteins remained a hard-to-crack molecular target as intracellular protein-protein interactions are notoriously difficult to inhibit with small molecules. Previous efforts in this field have often resulted in either non-selective compounds or compounds binding to upstream targets. Using technologies and new chemistry developed by Prof Patrick Gunning, the Canada Research Chair in Medicinal Chemistry and a co-founder, Janpix has now been able to discover highly potent and selective STAT3 and STAT5 inhibitors, as well as pan-STAT3/5 inhibitors. With selective compounds in hand, the hope is that these targets can now be further investigated in the clinic.
"Immunotherapy is one of the biggest advances in cancer therapy in recent decades but it doesn’t work in a significant number of patients," said Roman Fleck, PhD, founding CEO of Janpix and an advisor to Medicxi. "By targeting the tumor directly along with its microenvironment we may be able to expand the universe of patients that can benefit from immunotherapies."
"It is exciting to see such an investment, which will translate academic concepts into practical applications," said Professor Ulrich Krull, UTM’s Vice-President and Principal. "These innovations in chemistry that have been pioneered at UTM will potentially support a better quality of life, and perhaps even save lives, for many patients in Canada and around the world."
"We are excited to continue supporting Janpix and Prof Gunning’s work on STAT inhibitors," said Giovanni Mariggi, PhD, a Principal at Medicxi and Board Member of Janpix. "Janpix has made great progress in developing tractable compounds that inhibit these difficult-to-target proteins. The role of STATs in multiple tumor types is supported by vast data and the emerging evidence of their role in tumor immunity adds an extra dimension to the potential impact these new drugs could have on patients."