Poly(N-(2-hydroxypropyl) methacrylamide) (PHPMA) is a promising drug platform as it is non-immunogenic, biocompatible and hydrophilic polymer. It is the first copolymer-drug conjugates to be evaluated in clinical trials. However, it is challenging to obtain well-controlled PHPMA with high conver...

Novel cationic gemini surfactants - pentanediyl-1,5-bis[mono(2-hydroxypropyl) alkylammonium] dibromide and pentanediyl-1,5-bis[di(2-hydroxypropyl) alkylammonium] dibromide {in the abbreviation form - CnC5Cn[iso-Pr(OH)] and CnC5Cn[iso-Pr(OH)]2; alkyl - CnH2n+1 with n = 8, 9, 12 and 16} were synth...

BackgroundPreviously, we found that the neuropeptide galanin was strongly upregulated soon after bilateral cavernous nerve injury (BCNI) and that galanin and its receptors were expressed in nitrergic erectile innervation. Galanin has been observed to exert neuroregenerative effects in dorsal roo...

The neuropeptide galanin (GAL) is widely distributed within intrinsic and extrinsic sources supplying the eye. It is involved in regulation of the vascular tone, thus important for ocular homeostasis. Since the presence/distribution of its receptors is unknown, we here screen for the presence of...

Galanin is a neuropeptide distributed in human and rat brain regions that are involved with emotional regulation, such as the dorsal raphe nucleus (DRN). Galanin effects in the DRN are mediated by GAL1 and GAL2 receptors. Intracerebral infusion of a GAL2 (AR-M1896) or a GAL1 (M617) agonist induc...

N-terminal fragments of galanin (2–11) and (2–15) are critical for binding to GalR1-3 receptors, members of the G-protein-coupled receptor superfamily, and are involved in myocardial protection against ischemia/reperfusion (I/R) injury. This study was designed to synthesize novel GalR1-3 agoni...

The increasing interest in peptides and peptide receptors in cancer is based on the possibility of receptor targeting, because peptide receptors are often expressed in different human tumors. The neuropeptide galanin has also been suggested to be involved in the development of neuroendocrine tum...

Overweight and obesity may cause several metabolic complications, including type 2 diabetes mellitus and hyperlipidemia. Despite years of progress in medicine, there are no highly effective pharmacological treatments for obesity. The natural compound celastrol, a pentacyclic triterpene extracted...

Galanin (GAL) is a neuro-regulatory peptide involved in many physiological and pathophysiological processes. While data of GAL origin/distribution in the human eye are rather fragmentary and since recently the presence of GAL-receptors in the normal human eye has been reported, we here systemati...

Agonists and antagonists for galanin receptor subtypes GalR1-3 can be used as putative therapeutics targets for the treatment of various human diseases. However, effects of galanin and its N-terminal fragments on myocardial ischemia/reperfusion injury remain unclear. This study was designed to a...

Antibodies are an integral biomedical tool, not only for research but also as therapeutic agents. However, progress can only be made with sensitive and specific antibodies. The regulatory (neuro)peptide galanin and its three endogenous receptors (GAL1-3-R) are widely distributed in the central a...

Galanin and galanin receptors (GalRs) play important roles in the transmission and modulation of nociceptive information. Our previous research has shown that the expression of GalR1 is upregulated and that GalR1 activation in the nucleus accumbens (NAc) of rats with neuropathic pain has an anti...

The chemosynthesis and potential as green herbicides of 4,8-dihydroxy-1-tetralone (4, 8-DHT) and its derivates were emphatically addressed in this study. Firstly, the synthesis of 4, 8-DHT from commercially available material 1, 5-dihydroxynaphthalene was carried out through a novel route of fiv...

A series of 7-N-acylaminoethyl/propyloxime derivatives of dehydroabietic acid were synthesized and investigated for their antibacterial activity against Staphylococcus aureus Newman strain and multidrug-resistant strains (NRS-1, NRS-70, NRS-100, NRS-108 and NRS-271). Most of the target compounds...

The deficiency of nucleos(t)ide analogues (NAs) as anti-hepatitis B virus (HBV) drugs in clinical use is attributable to their insufficient enrichment in liver and non-target organ toxicity. We aimed to develop potent anti-HBV adefovir derivatives with hepatotrophic properties and reduced nephro...

Chiral calix[4]arene derivatives functionalized at the lower rim with chiral aminonaphthol units have been prepared. The structures of these receptors were characterized by a combination of 1H NMR, 13C NMR, FTIR and elemental analysis. The transport of amino acid derivatives (phenylglycine, phen...

Permeabilization of the phospholipid membrane, induced by the antibiotic peptides zervamicin IIB (ZER), ampullosporin A (AMP) and antiamoebin I (ANT) was investigated in a vesicular model system. Membrane-perturbing properties of these 15/16 residue peptides were examined by measuring the K+ tra...

The backbone dynamics of the channel-forming peptide antibiotic zervamicin IIB (Zrv-IIB) in methanol were studied by 15N nuclear magnetic resonance relaxation measurements at 11.7, 14.1 and 18.8 T magnetic fields. The anisotropic overall rotation of the peptide was characterized based on 15N rel...

Zervamicin IIB (Zrv-IIB) is a channel-forming peptaibol antibiotic of fungal origin. The measured transhydrogen bond 3hJNC′ couplings in methanol solution heaving average value of −0.41 Hz indicate that the stability of the Zrv-IIB helix in this milieu is comparable to the stability of helices ...

Zervamicin IIB is a 16-amino acid peptaibol that forms voltage-dependent ion channels with multilevel conductance states in planar lipid bilayers and vesicular systems. The spatial structure of zervamicin IIB bound to dodecylphosphocholine micelles was studied by nuclear magnetic resonance spect...