Health Boards
Anacor Pharmaceuticals announced today that a peer-reviewed article describing the recent progress of boron-based compounds in medicine and the properties of these compounds that support their development for the treatment of various skin disorders will be published in the February 17, 2014 edition of the Journal of Clinical and Aesthetic Dermatology. “From the Test Tube to the Treatment Room: Fundamentals of Boron-Containing Compounds and Their Relevance to Dermatology” is co-authored by James Q. Del Rosso, D.O., F.A.O.C.D., dermatologist in private practice at Las Vegas Skin and Cancer Clinics in Henderson, Nevada and Clinical Professor of Dermatology at Touro University College of Osteopathic Medicine in Henderson, Nevada and Jacob. J. Plattner, Ph.D., Senior Vice President of Research, Anacor Pharmaceuticals.
The authors note that the therapeutic benefit of incorporating boron into a chemical compound is derived from boron’s unique physical, chemical and structural properties. Boron has an empty p-orbital which gives it the capacity to form covalent bonds at a target site on a protein, rendering the protein inactive or less active. Several examples of proteins that boron-containing compounds have been found to inhibit include phosphodiesterase-4 (PDE4) thereby reducing the cytokine production in psoriasis and atopic dermatitis; leucyl tRNA synthetase thereby blocking protein synthesis in dermatophytes; and β-lactamases, thereby reducing resistance to antibiotic therapy.
The authors also note that, until recently, the use of boron in drug development has been widely overlooked. Initially, boron was incorporated into drug candidates as boronic acid which made the compounds overly reactive resulting in off-target binding and decreasing their potential effectiveness as therapeutic agents. However, since then, researchers found that if they incorporated boron into compounds as part of a cyclic structure rather than as an acid, they were able to produce small boron-based molecules that are highly stable, demonstrate effective target binding and selectivity and exhibit optimal physical properties that allow access to the necessary site of the disease target.
“The use of boron in drug discovery and development is very exciting to dermatology and other fields of medicine. Boron’s unique properties allow it to bind to target proteins involved in key pathophysiologic pathways which has opened the door to new potential therapies in dermatology including fungal infections such as onychomycosis, atopic dermatitis, psoriasis, acne, bacterial infections and other skin diseases,” said Dr. Del Rosso.
Boron-based compounds currently in development for dermatologic indications include tavaborole, which is being reviewed by the FDA for the treatment of toenail onychomycosis and AN2728, a PDE4 inhibitor which has completed Phase 2 studies in psoriasis and atopic dermatitis. A third compound, AN3365, is being evaluated as a gram-negative antibiotic. All three compounds were discovered and are being developed by Anacor Pharmaceuticals.
Source: anacor.com
*Anacor is a biopharmaceutical company focused on discovering, developing and commercializing novel small-molecule therapeutics derived from its boron chemistry platform.
The authors note that the therapeutic benefit of incorporating boron into a chemical compound is derived from boron’s unique physical, chemical and structural properties. Boron has an empty p-orbital which gives it the capacity to form covalent bonds at a target site on a protein, rendering the protein inactive or less active. Several examples of proteins that boron-containing compounds have been found to inhibit include phosphodiesterase-4 (PDE4) thereby reducing the cytokine production in psoriasis and atopic dermatitis; leucyl tRNA synthetase thereby blocking protein synthesis in dermatophytes; and β-lactamases, thereby reducing resistance to antibiotic therapy.
The authors also note that, until recently, the use of boron in drug development has been widely overlooked. Initially, boron was incorporated into drug candidates as boronic acid which made the compounds overly reactive resulting in off-target binding and decreasing their potential effectiveness as therapeutic agents. However, since then, researchers found that if they incorporated boron into compounds as part of a cyclic structure rather than as an acid, they were able to produce small boron-based molecules that are highly stable, demonstrate effective target binding and selectivity and exhibit optimal physical properties that allow access to the necessary site of the disease target.
“The use of boron in drug discovery and development is very exciting to dermatology and other fields of medicine. Boron’s unique properties allow it to bind to target proteins involved in key pathophysiologic pathways which has opened the door to new potential therapies in dermatology including fungal infections such as onychomycosis, atopic dermatitis, psoriasis, acne, bacterial infections and other skin diseases,” said Dr. Del Rosso.
Boron-based compounds currently in development for dermatologic indications include tavaborole, which is being reviewed by the FDA for the treatment of toenail onychomycosis and AN2728, a PDE4 inhibitor which has completed Phase 2 studies in psoriasis and atopic dermatitis. A third compound, AN3365, is being evaluated as a gram-negative antibiotic. All three compounds were discovered and are being developed by Anacor Pharmaceuticals.
Source: anacor.com
*Anacor is a biopharmaceutical company focused on discovering, developing and commercializing novel small-molecule therapeutics derived from its boron chemistry platform.