Nrf2 Herder

May 2, 2024

Happy early “May the 4th Be With You” aka #StarWarsDay.

If fans of Star Trek are called Trekkies, or Trekkers, fans of Lord of the Rings are called Tolkienites or Ringers, and fans of Harry Potter are called Potterheads, then what is the equivalent for Star Wars fans? We looked online for inspiration and found only a scattering of names listed below to which we have added emojis that communicate how we feel about them:

Star Wars Fans 🥱💤 (boring, really boring)
Jed-Heads 🥋😐 (neutral)
Virgins ☹️ 👎🏻 (boo)
Super Awesome People 👍‼️ (right on)
Nerf Herders 😙👌 (really like it!) (Nerf herders are like shepherds – we think)

We are partial to the last one (and the one before it), not least because the EpicentRx lead small molecule, RRx-001 (nibrozetone) is an agonist of the antioxidant transcription factor, Nrf2, pronounced like Nerf2. Nrf2 must translocate from the cytoplasm to the nucleus for it to activate its downstream targets called antioxidant regulated elements (ARE), whose role is to protect cells from damaging free radical stress. In the presence of RRx-001 (nibrozetone) Nrf2 dissociates from its inhibitor, called Keap 1, and shuttles to the nucleus, where it binds to a small protein called Maf and transcribes a whole host of detoxifying and antioxidant genes that protect against toxicity from foreign chemicals, and the development of cancer, as illustrated below.

Put another way, RRx-001 is responsible for “herding” Nrf2 from the cytoplasm to the nucleus, which makes it an antioxidant Nrf2 herder, albeit a non-scruffy one.