April, 2020: ACS Spring 2020 National Meeting & Expo (Virtual)
Oral presentation title: Inhibition of CYP26 to treat both proliferative skin disease and traumatic brain injury.
Synopsis: We described the latest results for our lead CYP26 inhibitors. The data presented shows that our lead compound (DX308) has high CYP26 A1 and B1 selectivity and potency, low systemic toxicity, and favorable brain/plasma ratios in vivo (for TBI treatment). We now have inhibitors that are selective and potent for A1 (DX385), for B1 (DX314), and for both A1 and B1 (DX308).
May, 2020: SID Annual Meeting (Virtual)
Poster title: Small molecule blockade of T-type calcium channels by DX416 inhibits itch and reduces corresponding inflammation in acute and chronic itch mouse models.
Synopsis: DermaXon virtually attended SID2020 and the accepted abstracts will be published in the Journal of Investigational Dermatology. We presented exciting new data on DX416 lead testing in three murine itch models to assess efficacy in both chronic and acute itch. We saw over 65% reduction in itch scores across models and inflammatory mediators relevant to itch were significantly reduced in the skin of DX416 treated mice. Small molecule blockade of T-type calcium channels represents a promising therapeutic strategy for the inhibition of itch and concurrent inflammation.
Poster title: AKR1B10 inhibition in keratinocytes as a strategy to improve retinaldehyde efficacy and increase endogenous atRA.
Synopsis: Work for Rodan+Fields was presented in a second abstract accepted to SID2020. Here we combined our expertise in basic biology and computational methods to pursue a novel strategy to increase endogenous retinoic acid in the skin. We are evaluating the use of both natural fatty acids and synthetic compounds that are compatible with cosmetic use and have initiated testing within human keratinocyte models.
October, 2019: Montana ACS Local Section (Butte MT, USA)
Oral presentation title: Topical Therapeutics to Treat Peripheral Neuropathy, Pruritis, Ichthyosis, and Other Diseases.
Synopsis: With the burgeoning growth of small biotech companies in western Montana, this venue provides us an opportunity to showcase our innovative technologies to local scientists. A brief overview of the various projects will encourage collaboration, and draw potential new employees as the company begins to grow.
October 2019: Annual Montagna Symposium on the Biology of Skin (Gleneden Beach, OR, USA)
Poster title: Small Molecule Inhibition of AKR1B10 to Improve Retinaldehyde Efficacy and Increase Endogenous atRA
Synopsis: We are investigating naturally derived AKR1B10 inhibitors to increase endogenous retinoic acid in the skin. Using recombinant AKR1B10 and docking studies, we have identified a panel of DX small molecules as promising AKR1B10 inhibitors.
Poster title: T-type Calcium Channel Blockers Modulate Inflammatory and Pruritic Mediators in Immune Cells and Keratinocytes.
Synopsis: DermaXon attended the Montagna Symposium-Decoding Complex Skin Disease to present additional research on immune responses during pruritus, or itch. This work highlights DermaXon’s highly fruitful collaboration with Drs. Zamponi and Gadotti at the University of Calgary in studying the neuroimmune axis of itch and pain.
September 2019: CBSD Symposium (Missoula, MT, USA)
Poster title: Itch Blockade and Immune Modulation Through T-Type Calcium Channels.
Poster title: Deciphering biosynthesis of all-trans-retinoic acid and the regulation of retinoid homeostasis in multi-differential keratinocytes.
Synopsis for the 2 posters above: DermaXon’s work was presented at the Center for Biomolecular Structure and Dynamics 2019 annual symposium by two summer undergraduate researchers; highlighting DermaXon’s close collaborations with and full support of local academic research.
August 2019: The Gordon Research Seminars, Medicinal Chemistry (Colby College, New London NH, USA)
Poster title: “Carbazole-based T-type Calcium Channel Inhibitors to Treat Neuropathic Pain”
Synopsis: Our initial analgesic therapeutics were developed from cannabinoid-inspired carbazole derivatives. The information presented on this poster details the early SAR analysis from those compounds, ultimately directing us to the highly active, CaV3.2 inhibitors we utilize at present.
June 2019: The World Congress of Dermatology (Milan, Italy)
Poster title: Epidermal barrier modifications by retinoid homeostasis disruption.
Synopsis: We demonstrated that treatment of reconstructed epidermis with our atRA-based type I CYP26B1 selective inhibitor, results in an increase in epidermal barrier function and regulation of specific atRA signaling pathways whereas cotreatments with a low dose of atRA and a dual CYP26A1 and B1 inhibitor or a PPAR β/δ activator result in a decrease of epidermal barrier function and regulation of specific atRA signaling pathways.
May 2019: Society for Investigative Dermatology (SID) (San Francisco, CA., USA)
Poster title: Deciphering biosynthesis of all-trans-retinoic acid from retinaldehyde and the regulation of retinoid homeostasis in skin.
Synopsis: DermaXon attended the Society of Investigative Dermatology annual meeting in Chicago, IL to present research on a Rodan+Fields collaborative project. This exciting project is working toward novel therapeutic strategies for controlling endogenous concentrations of all trans retinoic acid and providing insights into the mechanisms underlying all trans retinoic acid homeostasis.
Oral Presentation: Peripheral Blockade of T-type Calcium Channels by DX416 Inhibits Acute Itch And Modulates Immune Response.
Synopsis: DermaXon was invited as a SID 2019 platform presentation to share cutting edge research on a novel small molecule, DX416. We highlighted the unique potential of DX416 to reduce itch signaling transmitted by pruriceptors while simultaneously suppressing itch-inducing cytokine expression from activated immune cells—a combination that could be highly efficacious in the difficult-to-treat itch that underlies so many dermatological diseases and peripheral neuropathies.
May 2019: Neurotech Investing & Partnering Conference (Boston, MA, USA)
Oral Presentation: From Cannabinoids to calcium channel blockers for the treatment of pain and itch.
Synopsis: Local administration of our topical calcium channel blockers DX416 results in an inhibition of acute itch and pain in vivo without impairing motor function. Furthermore, DX416 treatment results in a pronounced reduction of inflammatory mediators, such as IL-31 and TNFα, during acute inflammation modeled through in vitro stimulation of human peripheral blood monocytes and THP-1 derived antigen presenting cells. Collectively, our data revealed that DX416 is a promising lead compound for the inhibition of itch, pain and concurrent acute inflammation. In this seminar, we reported details of the design, in vitro characterization, and in vivo testing of this new series of compounds.
March 2019: American Academy of Dermatology (AAD) Annual Meeting (Washington, DC., USA)
Poster title: Effect of retinaldehyde and calcium on epidermal barrier function in reconstructed human epidermis
Synopsis: With over 9000 medical and research professionals in attendance, DermaXon was excited to present new work conducted for Rodan+Fields at AAD 2019. This project used 3D reconstructed human epidermis to test the capability of Hydroxyapatite (HAP), a natural, biocompatible, and stable calcium-containing mineral found in the human body to increase the stability of retinal. By increasing the stability of retinal, we can feed the retinoic acid pathway in a sustained manner to positively impact epidermal barrier formation and function.
October 2018: The 12th Annual Pain and Migraine Therapeutics Summit – Industry Registration (San Francisco, CA, USA)
Oral Presentation: Multi-Target-Directed Ligands for the Treatment of Pain.
Synopsis: In this seminar, we reported details of the design of our new series of calcium channel blockers starting from cannabinoid derivatives.
May 2018: Society for Investigative Dermatology (SID) (Chicago, IL, USA)
Poster title: Combination of retinaldehyde and hydroxylapatite mimics the effects of all-trans retinoic acid in reconstructed human epidermis
Poster title: Novel CYP26B1-selective inhibitor increases measures of epidermal barrier function in healthy, darier’s, and ichthyotic econstructed human epidermis”
March 2018: American Academy of Dermatology (AAD) Annual Meeting (Washington, DC., USA)
Oral presentation: Effect of retinaldehyde and calcium on epidermal barrier function in reconstructed human epidermis.
Synopsis: In this study, we have confirmed the stabilization effect of hydroxyapatite on retinaldehyde. We have also studied the effects of retinaldehyde alone and in combination with hydroxyapatite on epidermal barrier functionality, using transepithelial electrical resistance (TEER) measurements and modulation of gene expression.
May 2017: Society for Investigative Dermatology (SID) (Chicago, IL, USA)
Poster title: Novel CYP26 inhibitors potentiate the effects of all-trans-retinoic acid on phenotype of normal and Darier disease keratinocytes in reconstructed human epidermis