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Search for "glycoprotein" in Full Text gives 61 result(s) in Beilstein Journal of Organic Chemistry.
Synthesis of 5-(ethylsulfonyl)-2-methoxyaniline: An important pharmacological fragment of VEGFR2 and other inhibitors
Beilstein J. Org. Chem. 2013, 9, 173–179, doi:10.3762/bjoc.9.20
- kinase 1, alpha and beta adrenoreceptors, glycogen phosphorylase, IMP dehydrogenase, MMPs 2, 3, 9 and 13, etc. [1]. Vascular endothelial growth factor (VEGF-A) is a homodimeric glycoprotein and thought to be the key signalling molecule of angiogenesis, i.e., the formation of new blood vessels from pre
Chemical–biological characterization of a cruzain inhibitor reveals a second target and a mammalian off-target
Beilstein J. Org. Chem. 2013, 9, 15–25, doi:10.3762/bjoc.9.3
- , compound 1 exhibits nonlinear exposure with escalating dose and is known to be a substrate of the drug transporter P-glycoprotein (P-gp). Finally, as a basic (protonatable) drug species, 1 could potentially accumulate in acidic lysosomes, where mammalian cathepsins (potential off-targets of 1) are located
Hydrophobic analogues of rhodamine B and rhodamine 101: potent fluorescent probes of mitochondria in living C. elegans
Beilstein J. Org. Chem. 2012, 8, 2156–2165, doi:10.3762/bjoc.8.243
- xenobiotic detoxification enzymes, including cytochrome P450s, phase-II transferases, and efflux pumps such as P-glycoprotein [35], to reach target tissues [29]. Thus, compounds such as HRB 9 and HR101 10 that show high potency in this animal have passed through a stringent biological filter, providing a
Total synthesis and biological evaluation of fluorinated cryptophycins
Beilstein J. Org. Chem. 2012, 8, 2060–2066, doi:10.3762/bjoc.8.231
- tumor cells express a P-glycoprotein, a drug efflux pump that transports xenobiotics out of the cell. A synthetic analogue, cryptohycin-52 (2, LY355703), has been investigated in clinical trials. However, this development was discontinued because of neurotoxic side effects and lacking efficacy in vivo
- are usually good substrates for the P-glycoprotein efflux pump resulting in a decreased bioactivity. Structures of cryptophycin-1 (1) and -52 (2). Fluorinated derivatives of cryptophycin-1 and -52 [20][21][22]. Access to the trifluoromethyl substituted unit A-building block 16. Reagents and conditions
Peptides presenting the binding site of human CD4 for the HIV-1 envelope glycoprotein gp120
Beilstein J. Org. Chem. 2012, 8, 1858–1866, doi:10.3762/bjoc.8.214
- Based on the structure of the HIV-1 glycoprotein gp120 in complex with its cellular receptor CD4, we have designed and synthesized peptides that mimic the binding site of CD4 for gp120. The ability of these peptides to bind to gp120 can be strongly enhanced by increasing their conformational stability
- protein binding site mimics. We have previously developed strategies for the design and generation of scaffolded and assembled peptides to generate protein binding site mimics [1]. The interaction of the HIV-1 envelope glycoprotein gp120 with its cellular receptor CD4 is the first step in the process of
- CD4bs fragments of gp120 [9]. This peptide is recognized by CD4, as well as by mAbs b12 and VRC01. The receptor glycoprotein CD4 is composed of four extracellular immunoglobulin domains (D1–D4), a short cytoplasmatic tail, and a single transmembrane helix [10]. Gp120 contacts the CD4 D1 domain, which
Synthesis of 5-oxyquinoline derivatives for reversal of multidrug resistance
Beilstein J. Org. Chem. 2012, 8, 1700–1704, doi:10.3762/bjoc.8.193
- 10.3762/bjoc.8.193 Abstract The inhibition of ABC (ATP binding cassette) transporters is considered a powerful tool to reverse multidrug resistance. Zosuquidar featuring a difluorocyclopropyl-annulated dibenzosuberyl moiety has been found to be an inhibitor of the P-glycoprotein, one of the best-studied
- “multidrug resistance”. Various transporters of the ATP-binding cassette family, so called ABC transporters, have been shown to be responsible for multidrug resistance [1]. Among these multidrug-resistance ABC transporters, the P-glycoprotein has been investigated most intensively [2]. As P-glycoprotein is
- considered to be a major player in multidrug resistance and has been found to be over expressed in tumor cells [3][4], considerable attempts have been made to develop inhibitors of P-glycoprotein in order to reverse multidrug resistance. These efforts were pursued for a longer period leading to a variety of
Design of a novel tryptophan-rich membrane-active antimicrobial peptide from the membrane-proximal region of the HIV glycoprotein, gp41
Beilstein J. Org. Chem. 2012, 8, 1172–1184, doi:10.3762/bjoc.8.130
- biological activity of antimicrobial peptides. This information was used to design a novel antimicrobial peptide sequence by using an intrinsically inactive membrane-associated peptide derived from the HIV glycoprotein, gp41, as a starting scaffold. This peptide corresponds to the tryptophan-rich membrane
- has four additional positive charges and is also antimicrobially inactive. The lack of antimicrobial activity may be related to the fact that the gp41w peptide appears to oligomerize in solution. When found in the HIV-1 Env glycoprotein complex, gp41 is known to exist as a trimer [26], and previous
The use of glycoinformatics in glycochemistry
Beilstein J. Org. Chem. 2012, 8, 915–929, doi:10.3762/bjoc.8.104
- protein databases. Tools to input, convert, or analyze glycan structures. Tools for prediction and analysis of carbohydrate/glycoprotein 3D structures. Prediction and analysis of glycosylation sites. Tools to support experimental analysis of glycans.
Synthetic glycopeptides and glycoproteins with applications in biological research
Beilstein J. Org. Chem. 2012, 8, 804–818, doi:10.3762/bjoc.8.90
- backbones, or mimics thereof, offer further possibilities to study protein-binding events. Keywords: glycopeptide binding; glycopeptides; glycoprotein synthesis; solid-phase peptide synthesis; synthetic vaccines; Introduction The majority of human proteins are co- or post-translationally modified by mono
- - or oligosaccharides. The glycoprotein saccharides contribute physiochemical properties, influencing protein conformation or increasing stability against proteolytic activity. With their unique structural diversity and complexity, carbohydrates attached on proteins or lipids are involved in numerous
- techniques for glycoprotein synthesis by preparation of a number of GalNAc containing O-glycoproteins, such as the antimicrobial protein diptericin, the cytokine lymphotactin and the leukocyte adhesion molecule ligand GlyCAM-1 [46][47][48]. By repeated NCL couplings of mucin tandem repeats, MUC2 and MUC1
Metathesis access to monocyclic iminocyclitol-based therapeutic agents
Beilstein J. Org. Chem. 2011, 7, 699–716, doi:10.3762/bjoc.7.81
- glycoprotein biosynthesis. Derivatives of this class bearing hydroxymethyl groups at C-6 have been shown to inhibit powerfully lysosomal α-mannosidase while displaying varying potencies toward α-1,6-mannosidase. On the other hand, N-alkylated polyhydroxylated azepanes with the D-glucose or L-idose
Preparation of aminoethyl glycosides for glycoconjugation
Beilstein J. Org. Chem. 2010, 6, 699–703, doi:10.3762/bjoc.6.81
- important component of glycoprotein glycans and also a substrate for sialyltransferases to generate biologically important sialyllactosides. The aminoethyl lactoside 16 was prepared in greatest yield from the bromide and attempts to prepare 16 directly from the acetate using BF3·Et2O as the activator only
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