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47633

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Stefan Eissler et al.
Journal of peptide science : an official publication of the European Peptide Society, 23(10), 757-762 (2017-06-22)
In solid-phase peptide synthesis, the nominal batch size is calculated using the starting resin substitution and the mass of the starting resin. The starting resin substitution constitutes the basis for the calculation of a whole set of important process parameters
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
Loay Awad et al.
Chembiochem : a European journal of chemical biology, 17(24), 2353-2360 (2016-10-28)
We present the design, synthesis, and characterization of a novel photocaged glutamine derivative (modified on the side chain of glutamine), and describe its use in enhancing peptide stability and solubility. Our results demonstrate that this approach can be used to
Zhimou Yang et al.
Chemical communications (Cambridge, England), (35)(35), 4414-4416 (2005-09-02)
Two types of therapeutic agents, which have discrete yet complementary functions, self-assemble into nanofibers in water to formulate a new supramolecular hydrogel as a self-delivery biomaterial to reduce the toxicity of uranyl oxide at the wound sites.
Facile solid-phase synthesis of cyclic decapeptide antibiotic streptocidins A-D
Qin C, et al.
Tetrahedron Letters, 45(1), 217-220 (2004)
Franziska Thomas et al.
Biochemistry, 56(50), 6544-6554 (2017-11-23)
Coiled coils (CCs) are among the best-understood protein folds. Nonetheless, there are gaps in our knowledge of CCs. Notably, CCs are likely to be structurally more dynamic than often considered. Here, we explore this in an abundant class of CCs
Zdenek Kukacka et al.
ChemMedChem, 13(9), 909-915 (2018-02-24)
α-Galactosidase (αGal) is a lysosomal enzyme that hydrolyses the terminal α-galactosyl moiety from glycosphingolipids. Mutations in the encoding genes for αGal lead to defective or misfolded enzyme, which results in substrate accumulation and subsequent organ dysfunction. The metabolic disease caused
Markus Beck Erlach et al.
Journal of biomolecular NMR, 69(2), 53-67 (2017-09-16)
For evaluating the pressure responses of folded as well as intrinsically unfolded proteins detectable by NMR spectroscopy the availability of data from well-defined model systems is indispensable. In this work we report the pressure dependence of
C R Jan et al.
The Chinese journal of physiology, 43(1), 29-33 (2000-06-17)
This report demonstrates that NPC-15199 [(N-(9-fluorenylmethoxycarbonyl)L-leucine)], a novel anti-inflammatory agent, increases intracellular Ca2+ concentration ([Ca2+]i) in human bladder female transitional cancer (BFTC) cells. Using fura-2 as a Ca2+ probe, NPC-15199 (0.1-2 mM) was found to increase [Ca2+]i concentration-dependently. The response
Fan Gao et al.
Small (Weinheim an der Bergstrasse, Germany), 14(37), e1802403-e1802403 (2018-08-22)
Chemotherapy is well recognized to induce immune responses during some chemotherapeutic drugs-mediated tumor eradication. Here, a strategy involving blocking programmed cell death protein 1 (PD-1) to enhance the chemotherapeutic effect of a doxorubicin nanoprodrug HA-Psi-DOX is proposed and the synergetic
M J Miller et al.
The Journal of pharmacology and experimental therapeutics, 266(1), 468-472 (1993-07-01)
Anti-inflammatory properties have been ascribed to a series of N-(fluorenyl-9-methoxycarbonyl) amino acids called leumedins that inhibit the activity of granulocytes and T-lymphocytes. We evaluated one of these leumedins, N-(fluorenyl-9-methoxycarbonyl) leucine (NPC 15199), in a model of ileitis in guinea pigs.
Catalytic Oligopeptide Synthesis
Liu Z, et al.
Organic Letters, 20(3), 612-615 (2018)
Rapid, high-yield, solid-phase synthesis of the antitumor antibiotic sansalvamide A using a side-chain-tethered phenylalanine building block
Lee Y and Silverman RB
Organic Letters, 2(23), 3743-3746 (2000)
G Cheng et al.
Langmuir : the ACS journal of surfaces and colloids, 26(7), 4990-4998 (2010-01-16)
The self-assembly and hydrogelation properties of two Fmoc-tripeptides [Fmoc = N-(fluorenyl-9-methoxycarbonyl)] are investigated, in borate buffer and other basic solutions. A remarkable difference in self-assembly properties is observed comparing Fmoc-VLK(Boc) with Fmoc-K(Boc)LV, both containing K protected by N(epsilon)-tert-butyloxycarbonate (Boc). In
Yun Song et al.
Cell reports, 30(8), 2699-2711 (2020-02-27)
The transcriptional corepressor complex CoREST is one of seven histone deacetylase complexes that regulate the genome through controlling chromatin acetylation. The CoREST complex is unique in containing both histone demethylase and deacetylase enzymes, LSD1 and HDAC1, held together by the
Takhar Kasumov et al.
PloS one, 10(5), e0126910-e0126910 (2015-05-21)
Cardiovascular disease (CVD) is a serious comorbidity in nonalcoholic fatty liver disease (NAFLD). Since plasma ceramides are increased in NAFLD and sphingomyelin, a ceramide metabolite, is an independent risk factor for CVD, the role of ceramides in dyslipidemia was assessed
Weidang Wu et al.
Cancer science, 106(6), 747-756 (2015-04-14)
L-type amino acid transporter 1 (LAT1), overexpressed on the membrane of various tumor cells, is a potential target for tumor-targeting therapy. This study aimed to develop a LAT1-mediated chemotherapeutic agent. We screened doxorubicin modified by seven different large neutral amino
Michał Padjasek et al.
Chemistry (Weinheim an der Bergstrasse, Germany), 26(15), 3297-3313 (2019-12-18)
CdII is a major genotoxic agent that readily displaces ZnII in a multitude of zinc proteins, abrogates redox homeostasis, and deregulates cellular metalloproteome. To date, this displacement has been described mostly for cysteine(Cys)-rich intraprotein binding sites in certain zinc finger
Marius Brehm et al.
Small (Weinheim an der Bergstrasse, Germany), 16(10), e1905971-e1905971 (2020-01-28)
Miniaturization and parallelization of combinatorial organic synthesis is important to accelerate the process of drug discovery while reducing the consumption of reagents and solvents. This work presents a miniaturized platform for on-chip solid-phase combinatorial library synthesis with UV-triggered on-chip cell
Vibeke Miller Breinholt et al.
The Journal of pharmacology and experimental therapeutics, 370(3), 459-471 (2019-06-27)
TransCon CNP is a C-type natriuretic peptide (CNP-38) conjugated via a cleavable linker to a polyethylene glycol carrier molecule, designed to provide sustained systemic CNP levels upon weekly subcutaneous administration. TransCon CNP is in clinical development for the treatment of
Marcus Pickhardt et al.
Current Alzheimer research, 14(7), 742-752 (2017-02-06)
Anti-aggregation drugs play an important role in therapeutic approaches for Alzheimer's disease. We have previously developed a number of compounds that are able to inhibit the pathological aggregation of Tau protein. One common obstacle to application is the limited penetration
Chung-Ren Jan et al.
The Chinese journal of physiology, 45(3), 117-122 (2003-06-24)
In Madin-Darby canine kidney (MDCK) cells, effect of NPC-15199 on intracellular Ca2+ concentration ([Ca2+]i) was investigated by using fura-2. NPC-15199 (100-1000 microM) caused a rapid and sustained increase of [Ca2+]i in a concentration-dependent manner (EC50=500 microM). NPC-15199-induced [Ca2+]i rise was
Synthesis and Evaluation of Coumaroyl Dipeptide Amide as Potential Whitening Agents
Lee H-S, et al.
Bull. Korean Chem. Soc., 34(10), 3017-3021 (2013)
Hong Cheng et al.
Macromolecular bioscience, 19(4), e1800410-e1800410 (2018-12-24)
In this paper, a self-delivery chimeric peptide PpIX-PEG8 -KVPRNQDWL is designed for photodynamic therapy (PDT) amplified immunotherapy against malignant melanoma. After self-assembly into nanoparticles (designated as PPMA), this self-delivery system shows high drug loading rate, good dispersion, and stability as
Fatemeh Zabihi et al.
Journal of controlled release : official journal of the Controlled Release Society, 242, 35-41 (2016-07-30)
Nanogels offer many unique features rendering them as very attractive candidates for drug delivery. However, for their applications the loading capacity and specific encapsulation, in particular for hydrophobic drugs, in a complex media are two critical factors. In this work
Jingwen Song et al.
Small (Weinheim an der Bergstrasse, Germany), 16(8), e1907309-e1907309 (2020-01-30)
There is a real need for new antibiotics against self-evolving bacteria. One option is to use biofriendly broad-spectrum and mechanically tunable antimicrobial hydrogels that can combat multidrug-resistant microbes. Whilst appealing, there are currently limited options. Herein, broad-spectrum antimicrobial biometallohydrogels based
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