The present review describes the current knowledge about the reaction mechanism of drosophilid alcohol dehydrogenases (DADH), a member of the short chain dehydrogenase/reductase (SDR) superfamily. Included is the binding order of the substrates to the enzyme, rate limiting steps, stereochemistry of the reaction, active site topology, role of important amino acids and water molecules in the reaction ...

Pseudolysin (PLN) is a metalloproteinase secreted from bacteria that degrades extracellular proteins to produce bacterial nutrition. It is thus expected that inhibitors against PLN can suppress the growth of bacteria and their pandemic spread. In addition, since these inhibitors do not attack to bacteria directly, there is a reduced risk for producing drug-resistant bacteria. On the other hand, as ...

The mitogen-activated protein kinase-activated protein kinase MK5 is ubiquitously expressed in vertebrates and is implicated in cell proliferation, cytoskeletal remodeling, and anxiety behavior. This makes MK5 an attractive drug target. We tested several diterpenoid alkaloids for their ability to suppress MK5 kinase activity. We identified noroxoaconitine as an ATP competitor that inhibited the ...

Professor Svein Dahl ved Universitetet i Tromsø var en framtredende og nyskapende legemiddelforsker. De metodene han benyttet, brukes den dag i dag av farmasøytisk industri og forskere over hele verden.

N‐methyl‐d‐aspartate receptors (NMDAR) are widely expressed in the brain. GluN2B subunit‐containing NMDARs has recently attracted significant attention as potential pharmacological targets, with emphasis on the functional properties of allosteric antagonists. We used primary cultures from chicken embryo forebrain (E10), expressing native GluN2B‐containing NMDA receptors as a novel model system. ...

The γ-aminobutyric acid (GABA) type B receptor (GABA<sub>B</sub-R) belongs to class C of the G-protein coupled receptors (GPCRs). Together with the GABA_A receptor, the receptor mediates the neurotransmission of GABA, the main inhibitory neurotransmitter in the central nervous system (CNS). In recent decades, the receptor has been extensively studied with the intention being to understand ...

Photodynamic therapy (PDT) is a safe and effective method currently used in the treatment of skin cancer. In ALA-based PDT, 5-aminolevulinic acid (ALA), or ALA esters, are used as pro-drugs to induce the formation of the potent photosensitizer protoporphyrin IX (PpIX). Activation of PpIX by light causes the formation of reactive oxygen species (ROS) and toxic responses. Studies have indicated that ...

Thyroid hormone disrupting chemicals (THDCs) are of major concern in ecotoxicology. With the increased number of emerging chemicals on the market there is a need to screen for potential THDCs in a cost-efficient way, and <i>in silico</i> modeling is an alternative to address this issue. In this study homology modeling and docking was used to screen a list of 626 compounds for potential thyroid hormone ...

The GABA_B receptor (GABA_B-R) is a heterodimeric class C G protein-coupled receptor comprised of the GABA_B1a/b and GABA_B2 subunits. The endogenous orthosteric agonist γ-amino-butyric acid (GABA) binds within the extracellular Venus flytrap (VFT) domain of the GABA_B1a/b subunit. The receptor is associated with numerous neurological and ...

Tetradecabromo-1,4-diphenoxybenzene (TeDB-DiPhOBz) is a highly brominated additive flame retardant (FR). Debrominated photodegradates of TeDBDiPhOBz are hydroxylated <i>in vitro</i> in liver microsomal assays based on herring gulls (<i>Larus argentatus</i>), including one metabolite identified as 4<i>″</i>-OH-2,2<i>′</i>,2<i>″</i>,4-tetrabromo-DiPhOBz. Chemically related methoxylated tetra- ...