Showing 1-30 of 114 results for "411027"
Daniel W Kung et al.
Bioorganic & medicinal chemistry letters, 22(13), 4281-4287 (2012-06-09)
The discovery of spirocyclic piperidine-azetidine inverse agonists of the ghrelin receptor is described. The characterization and redressing of the issues associated with these compounds is detailed. An efficient three-step synthesis and a binding assay were relied upon as the primary...
Binu Jacob et al.
Journal of peptide science : an official publication of the European Peptide Society, 19(11), 700-707 (2013-10-10)
KR-12 (residues 18-29 of LL-37) was known to be the smallest peptide of human cathelicidin LL-37 possessing antimicrobial activity. In order to optimize α-helical short antimicrobial peptides having both antimicrobial and antiendotoxic activities without mammalian cell toxicity, we designed and...
Li Hong Zhang et al.
Spectrochimica acta. Part A, Molecular and biomolecular spectroscopy, 97, 639-647 (2012-08-04)
Rhodamine S could emit strong and stable room temperature phosphorescence (RTP) on polyamide membrane (PAM) in the presence of heavy atom perturber Pb(2+). When Rhodamine S-piperidine solution was dropped on PAM, the red (Rhod.S)(n)-P-SOR (Rhod.S, (Rhod.S)(n), P and SOR refer...
Ryan J Wade et al.
Nature communications, 6, 6639-6639 (2015-03-24)
Electrospun nanofibres are promising in biomedical applications to replicate features of the natural extracellular matrix (ECM). However, nearly all electrospun scaffolds are either non-degradable or degrade hydrolytically, whereas natural ECM degrades proteolytically, often through matrix metalloproteinases. Here we synthesize reactive...
Daniel J Rubin et al.
ACS nano, 9(3), 3360-3368 (2015-03-12)
The rigid geometry and tunable chemistry of D,L-cyclic peptides makes them an intriguing building-block for the rational design of nano- and microscale hierarchically structured materials. Herein, we utilize a combination of electron microscopy, nanomechanical characterization including depth sensing-based bending experiments...
Paresh A Parmar et al.
Biomaterials, 54, 213-225 (2015-04-25)
Regenerative medicine strategies for restoring articular cartilage face significant challenges to recreate the complex and dynamic biochemical and biomechanical functions of native tissues. As an approach to recapitulate the complexity of the extracellular matrix, collagen-mimetic proteins offer a modular template...
Shruti U Gandhy et al.
BMC cancer, 12, 564-564 (2012-12-01)
Curcumin inhibits growth of several cancer cell lines, and studies in this laboratory in bladder and pancreatic cancer cells show that curcumin downregulates specificity protein (Sp) transcription factors Sp1, Sp3 and Sp4 and pro-oncogenic Sp-regulated genes. In this study, we...
Soo Min Cho et al.
Scientific reports, 4, 6777-6777 (2014-10-28)
Amyloid-β (Aβ) is one of the few neuropathological biomarkers associated with transporters of the blood-brain barrier (BBB). Despite the well-characterized clinical indication of decreasing Aβ levels in the cerebrospinal fluid (CSF) during the development of Alzheimer's disease (AD), the link...
Marek Łuczkowski et al.
Inorganic chemistry, 47(23), 10875-10888 (2008-10-31)
A de novo protein design strategy provides a powerful tool to elucidate how heavy metals interact with proteins.Cysteine derivatives of the TRI peptide family (Ac-G(LKALEEK)4G-NH2) have been shown to bind heavy metals in an unusual trigonal geometry. Our present objective...
Lucia Silvestrini et al.
PloS one, 10(9), e0135416-e0135416 (2015-09-04)
A few yeasts, including Hansenula polymorpha are able to assimilate nitrate and use it as nitrogen source. The genes necessary for nitrate assimilation are organised in this organism as a cluster comprising those encoding nitrate reductase (YNR1), nitrite reductase (YNI1)...
Seyedsina Moeinzadeh et al.
Tissue engineering. Part A, 21(1-2), 134-146 (2014-07-23)
An attractive approach to reduce the undesired side effects of bone morphogenetic proteins (BMPs) in regenerative medicine is to use osteoinductive peptide sequences derived from BMPs. Although the structure and function of BMPs have been studied extensively, there is limited...
Jae H Park et al.
Journal of medicinal chemistry, 57(15), 6623-6631 (2014-07-16)
The aqueous solution structure of protoxin II (ProTx II) indicated that the toxin comprises a well-defined inhibitor cystine knot (ICK) backbone region and a flexible C-terminal tail region, similar to previously described NaSpTx III tarantula toxins. In the present study...
Guangxin Xia et al.
ChemMedChem, 8(4), 577-581 (2013-03-09)
R adamantly beats S: 11β-HSD1 is a target for treating metabolic syndrome. The R isomer 5 was selected as a starting point for optimization and SAR studies. Inhibitor 8 w emerged after several rounds of optimization, showing cross-species inhibition of...
Erik Serrao et al.
Journal of medicinal chemistry, 56(6), 2311-2322 (2013-03-01)
On the basis of an initial molecular modeling study suggesting the favorable binding of the "privileged" fragment 8-hydroxyquinoline with HIV-1 integrase (IN) at the IN-lens epithelium-derived growth factor/p75 (LEDGF/p75) interface , we developed a set of modified 8-hydroxyquinoline fragments demonstrating...
Raj Kumar Roy et al.
Nature communications, 6, 7237-7237 (2015-05-27)
Biopolymers such as DNA store information in their chains using controlled sequences of monomers. Here we describe a non-natural information-containing macromolecule that can store and retrieve digital information. Monodisperse sequence-encoded poly(alkoxyamine amide)s were synthesized using an iterative strategy employing two...
Aase M Raddum et al.
Biochemical pharmacology, 95(1), 1-15 (2015-03-17)
The progression of aggressive cancer occurs via angiogenesis and metastasis makes these processes important targets for the development of anti-cancer agents. However, recent studies have raised the concern that selective inhibition of angiogenesis results in a switch towards increased tumour...
Guowei Zhang et al.
PloS one, 10(3), e0120809-e0120809 (2015-03-24)
Huperzine A is important in the treatment of Alzheimer's disease. There are major challenges for the mass production of huperzine A from plants due to the limited number of huperzine-A-producing plants, as well as the low content of huperzine A...
Evgeni Eltzov et al.
Analytical chemistry, 87(7), 3655-3661 (2015-03-17)
Indoor air pollution became a recent concern found to be oftentimes worse than outdoor air quality. We developed a tool that is cheap and simple and enables continuous monitoring of air toxicity. It is a biosensor with both a nondisposable...
David Giganti et al.
Nature communications, 5, 4833-4833 (2014-09-11)
The Plasmodium subtilase SUB1 plays a pivotal role during the egress of malaria parasites from host hepatocytes and erythrocytes. Here we report the crystal structure of full-length SUB1 from the human-infecting parasite Plasmodium vivax, revealing a bacterial-like catalytic domain in...
Susanne Kirchhof et al.
European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V, 96, 217-225 (2015-08-09)
Eight-armed PEG was functionalized with furyl and maleimide groups (8armPEG20k-Fur and 8armPEG20k-Mal); degradable hydrogels were obtained by cross-linking via Diels-Alder chemistry. To increase the stability to degradation, the macromonomers were modified by introducing a hydrophobic 6-aminohexanoic acid spacer between PEG...
P Ricardo Girling et al.
Organic & biomolecular chemistry, 9(9), 3105-3121 (2011-03-11)
A review into the aza-Diels-Alder reaction, mainly concentrating on literature examples that form piperidin-4-ones from the reaction of imines and electron rich dienes or enones, either through a Lewis acidic/Brønsted acid approach or through the use of an organocatalyst. This...
Chiara Testa et al.
Journal of medicinal chemistry, 57(22), 9424-9434 (2014-10-28)
Side chain-to-side chain cyclizations represent a strategy to select a family of bioactive conformations by reducing the entropy and enhancing the stabilization of functional ligand-induced receptor conformations. This structural manipulation contributes to increased target specificity, enhanced biological potency, improved pharmacokinetic...
Christoph Hirschhäuser et al.
Organic letters, 14(18), 4846-4849 (2012-09-06)
Expedient routes to three classes of novel spiro-fused pyrrolidine, piperidine, and indoline heterocycle scaffolds are described. These three-dimensional frameworks, which conform to the "rule of three", are suitably protected to allow for site-selective manipulation and functionalization. Different modes of substrate...
Lars Erik Uggerhøj et al.
FEBS letters, 588(17), 3291-3297 (2014-07-27)
The inclusion of peptoid monomers into antimicrobial peptides (AMPs) increases their proteolytic resistance, but introduces conformational flexibility (reduced hydrogen bonding ability and cis/trans isomerism). We here use NMR spectroscopy to answer how the insertion of a peptoid monomer influences the...
Stancho Stanchev et al.
Journal of peptide science : an official publication of the European Peptide Society, 20(9), 725-735 (2014-06-13)
The antimicrobial 40-amino-acid-peptide lucifensin was synthesized by native chemical ligation (NCL) using N-acylbenzimidazolinone (Nbz) as a linker group. NCL is a method in which a peptide bond between two discreet peptide chains is created. This method has been applied to...
Marta Soler et al.
Inorganic chemistry, 54(22), 10542-10558 (2015-10-28)
The conjugation of redox-active complexes that can function as chemical nucleases to cationic tetrapeptides is pursued in this work in order to explore the expected synergistic effect between these two elements in DNA oxidative cleavage. Coordination complexes of biologically relevant...
Daniela S Ferreira et al.
Advanced healthcare materials, 4(4), 602-612 (2014-11-22)
The use of peptide engineering to develop self-assembling membranes that are responsive to cellular enzyme activities is reported. The membranes are obtained by combining hyaluronan (HA) and a rationally designed peptide amphiphile (PA) containing a proteolytic domain (GPQGIWGQ octapeptide) sensitive...
Charity Wayua et al.
Journal of nuclear medicine : official publication, Society of Nuclear Medicine, 56(1), 113-119 (2014-12-17)
Tumor-specific targeting ligands were recently exploited to deliver both imaging and therapeutic agents selectively to cancer tissues in vivo. Because the cholecystokinin 2 receptor (CCK2R) is overexpressed in various human cancers (e.g., lung, medullary thyroid, pancreatic, colon, and gastrointestinal stromal...
Nitin J Pawar et al.
The Journal of organic chemistry, 77(18), 7873-7882 (2012-08-10)
The Jocic-Reeve and Corey-Link type reaction of dichloromethyllithium with suitably protected 5-keto-hexofuranoses followed by treatment with sodium azide and sodium borohydride reduction gave 5-azido-5-hydroxylmethyl substituted hexofuranoses 7a-c with required geminal dihydroxymethyl group. Removal of protecting groups and converting the C-1...
Do-Wan Shim et al.
PloS one, 10(5), e0126871-e0126871 (2015-05-29)
Antimicrobial peptides (AMPs), also called host defense peptides, particularly those with amphipathic helical structures, are emerging as target molecules for therapeutic development due to their immunomodulatory properties. Although the antimicrobial activity of AMPs is known to be exerted primarily by...

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