Functional molecules: Photopharmacology
P1: Photocontrolled HDAC inhibitor
Key features: P1 is a potent HDAC2 inhibitor that increases its activity 40x upon irradiation with UV light, reaching IC50 of 0.55 µM. The cis isomer also shows higher toxicity to cancer cells. The activity of P1 is retained in adult mouse brains.
Photochemistry: 365 nm / white light; Half-life: hours
Creators: Wiktor Szymanski, Marilena Ourailidou
P2: Photocontrolled BRAFV600E inhibitor
Key features: P2 is a photoswitchable inhibitor of the BRAF kinase that reversibly increases its potency 10-fold under irradiation with UV light.
Photochemistry: 365 nm / white light; Half-life: hours
Creators: Wiktor Szymanski, Mark Hoorens
Literature: paper 1
P3: Photocontrolled glutamate transport inhbitors
Key features: P3 is a photoswitchable glutamate transport inhibitor that enables reversible control of the function of ley glutamate transporters.
Photochemistry: 365 nm / white light; Half-life: hours
Creators: Mark Hoorens, Haigen Fu
P4: Photoactivated dopamine
Key features: P4 responds to red light by releasing dopamine.
Photochemistry: 650 nm
Creators: Kaja Sitkowska
Literature: paper 1
P5: Photoswitchable FraC nanopore
Key features: P5 is the Y140C mutant of cytotoxic FraC nanopore, in which the introduced cysteine is modified with a polar azobenzene switch. It enables reversible control of the insertion of FraC into the memberanes of mammalian cells and its toxicity.
Photochemistry: 365 nm / White light
Creators: Jana Volaric, Natalie Mutter
Literature: paper 1
P6: Photoswitchable circadian rhythm regulator
Key features: P6 is a Longdaysin-based, visible-light responsive regulator of circadian rhythm period that enables the regulation of period and phase in cells and tissues. It acts as a light-controlled inhibitor of CKI kinases.
Photochemistry: green (530 nm) / violet (400 nm) light
Creators: Dusan Kolarski
Literature: paper 1
P7: Azobenzene-based amino acid for controlling beta-hairpin structure
Key features: P7 (AMPO) is a photoswitchable amino acid that can be introduced in SPPS into peptides to mimic the beta-hairpin structure in the cis isomer. It is designed to exactly match the strand distance in beta-hairpin derived amyloid fibers.
Photochemistry: 365 nm / White light
Creators: Jana Volaric, Raffaella Parlato
Literature: paper 1
P8: Photoswtichable inhibitor of Casein Kinase 1delta
Key features: P8 (DK557) is a photoswitchable, cis-on inhibitor of Casein Kinase 1delta, featuring an aryazlopyrazole switch and characterized by high photostoatniory states in both directions.
Photochemistry: 365 nm / Blue light
Creators: Dusan Kolarski, Albert Schulte
Literature: paper 1