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A2E, a byproduct of the visual cycle
A substantial portion of the lipofuscin that accumulates with age and in some retinal disorders in retinal pigment epithelial (RPE) cells, forms as a consequence of light-related vitamin A recycling.Expand
Discovery and characterization of OC144-093, a novel inhibitor of P-glycoprotein-mediated multidrug resistance.
TLDR
The results demonstrate that OC144-093 is an orally active, potent, and nontoxic inhibitor of P-gp-mediated multidrug resistance that exhibits all of the desired properties for treatment and prevention of MDR prior to selection and/or induction of refractory disease. Expand
A2E, a fluorophore of RPE lipofuscin: can it cause RPE degeneration?
In atrophic age-related macular degeneration (AMD) and Stargardt disease, the death of retinal pigment epithelial (RPE) cell death leads to photoreceptor cell degeneration and visual impairment.Expand
"Venom" of the slow loris: sequence similarity of prosimian skin gland protein and Fel d 1 cat allergen
TLDR
This work clarifies the chemical nature of the brachial organ exudate and suggests a possible mode of action underlying the noxious effects of slow loris bites. Expand
Solid-state 2H NMR structure of retinal in metarhodopsin I.
TLDR
The structure of trans-retinal in the metarhodopsin I photointermediate (MI), where the retinylidene cofactor functions as an antagonist, is investigated to how photonic energy is channeled within the protein to allow the strained retinal conformation to relax, thereby forming the activated state of the receptor. Expand
2,4,5-Trisubstituted imidazoles: novel nontoxic modulators of P-glycoprotein mediated multidrug resistance. Part 1.
TLDR
N-4,5-Di-(4-dialkylamino)phenyl imidazoles (A) are potent modulators of P-glycoprotein mediated multidrug resistance and lead optimization of this novel class of inhibitors is described. Expand
Evidence from Chlamydomonas on the photoactivation of rhodopsins without isomerization of their chromophore.
TLDR
Responses to chromophores formed from naphthalene aldehydes suggest that charge separation within the excited chromophore leads to electric field-induced polarization of nearby amino acid residues and altered hydrogen bonding, which facilitates the reported multiple bond rotations and protein rearrangements of rhodopsin activation. Expand
Structural analysis and dynamics of retinal chromophore in dark and meta I states of rhodopsin from 2H NMR of aligned membranes.
TLDR
The results are pertinent to quantum and molecular mechanics simulations of ligands bound to GPCRs, and illustrate how (2)H NMR can be applied to study their biological mechanisms of action. Expand
Chemical complementation: A reaction-independent genetic assay for enzyme catalysis
TLDR
It is shown that the small-molecule yeast three-hybrid system can be used to read out cephalosporinase activity in vivo as a change in the level of transcription of a lacZ reporter gene and that the wild-type cep Halospor inase can be isolated from a pool of inactive mutants by using a LacZ screen. Expand
2,4,5-Trisubstituted imidazoles: novel nontoxic modulators of P-glycoprotein mediated multidrug resistance. Part 1.
Solution-phase combinatorial chemistry was applied to the optimization and development of clinical candidate OC144-093 (22), a novel and nontoxic modulator of P-glycoprotein mediated multidrugExpand
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