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  • peptide
  • It was attempted to achieve this goal by simple modifications of the molecular structure of the known inhibitors, with the focus on modifications of the peptide backbone. (uni-regensburg.de)
  • In this paper, we report lectin pathway-specific short peptide inhibitors developed by phage display against mannose-binding lectin-associated serine proteases (MASPs), MASP-1 and MASP-2. (jimmunol.org)
  • On the basis of the selected peptide sequences, two 14-mer peptides, designated as sunflower MASP inhibitor (SFMI)-1 and SFMI-2, were produced and characterized. (jimmunol.org)
  • Properties of signal peptide-specific systems are highlighted for the development of new therapeutic and antimicrobial applications, as compounds can target signal peptides from either host cells or pathogens and thereby selectively prevent translocation of those specific proteins. (springer.com)
  • Here we show the crystal structures of the prefusion MeV-F alone and in complex with the small compound AS-48 or a fusion inhibitor peptide. (pnas.org)
  • A peptide sequence containing only AA 28-79 retains substantial Kip1 cyclin A/CDK2 inhibitory activity. (rcsb.org)
  • inhibition
  • The structure of TAXI-I in complex with Aspergillus niger xylanase, illustrates the ability of tight binding and inhibition with subnanomolar affinity and indicates the importance of the C-terminal end for the differences in xylanase specificity among different TAXI-type inhibitors [ PMID: 15166216 ]. (ebi.ac.uk)
  • Sansen S, De Ranter CJ, Gebruers K, Brijs K, Courtin CM, Delcour JA, Rabijns A. Structural basis for inhibition of Aspergillus niger xylanase by triticum aestivum xylanase inhibitor-I. (ebi.ac.uk)
  • Inhibition of calcium/calmodulin-dependent protein kinase II (CaMKII), Janus kinase-3 (JAK-3), and IκB kinase (IKK) were identified to decrease the formation of MCF-7-derived CSCs in primary, secondary and tertiary mammosphere assay. (biomedcentral.com)
  • Broad inhibition of translocation is also an interesting target for the development of new anticancer drugs because cancer cells heavily depend on efficient protein translocation into the endoplasmic reticulum to support their fast growth. (springer.com)
  • The structures and accompanying cell-based fusion assays with inhibitors provide insight into the molecular mechanism for the inhibition of MeV-mediated fusion, which would help us conquer MeV-induced neurodegenerative diseases. (pnas.org)
  • For the discovery of phosphatase inhibitor classes by means of this approach, four natural product-derived or -inspired medium-sized compound collections were synthesized and investigated for inhibition of the tyrosine phosphatases VE-PTP, Shp-2, PTP1B, MptpA, and MptpB and the dual-specificity phosphatases Cdc25A and VHR. (pnas.org)
  • 9 Cholesteryl ester transfer protein (CETP) inhibition, however, offers the prospect of doubling HDL-C levels. (bjcardio.co.uk)
  • Inhibition of ErbB2 by either the HSP (heat shock protein) 90 inhibitor geldanamycin or the ErbB inhibitor ZD1839 in SKBR3 cells, a human breast cancer cell line overexpressing ErbB2 protein, induces a rapid and dramatic decrease in AKT activity. (aacrjournals.org)
  • An additional N‐terminal 12‐amino‐acid region (kinase inhibitory region) of JAB also contributes to high‐affinity binding to the JAK2 tyrosine kinase domain and is required for inhibition of JAK2 signaling and kinase activity. (embopress.org)
  • fusion proteins
  • ANV-KPI fusion proteins represent a new class of anticoagulants that specifically target the anionic membrane-associated coagulation enzyme complexes present at sites of thrombogenesis and are potentially useful as antithrombotic agents. (bloodjournal.org)
  • In experiments aiming to block the endogenous TNF production in arthritis, we and others showed that systemic administration of blocking Abs to TNF or of sTNFR:Fc fusion proteins after disease onset led to amelioration of joint disease in murine collagen-induced arthritis ( 12 , 13 , 14 ). (jimmunol.org)
  • specificity
  • Small-molecule modulators of phosphatase activity have proven to be powerful tools for the study of the chemical biology of these enzymes ( 3 ), and, in particular, protein tyrosine phosphatases (PTPs) ( 4 , 5 ) and dual-specificity phosphatases ( 6 ) have recently moved into the focus of a growing number of drug discovery programs, for instance in diabetes and anticancer research. (pnas.org)
  • membrane
  • The antiangiogenic properties and neurotrophic activities of the protein are due to peptides derived from the N-terminal region of this protein, while the C-terminal peptides interact with its membrane receptor [ 7 ]. (hindawi.com)
  • It consists of ∼30 proteins (circulating in the serum or membrane bound) forming a sophisticated molecular network capable of recognizing, tagging, and eliminating invading pathogen microorganisms and altered host cells (e.g., apoptotic and necrotic cells) via Ab-independent mechanisms ( 1 ). (jimmunol.org)
  • In general, translocation from the cytosol requires three key steps: (1) substrate recognition and targeting to the destination membrane, while maintaining the substrate in a translocation-competent state (2) translocation across or integration into that membrane, which usually requires energy expenditure in the form of GTP, ATP or proton motive force and (3) release, folding and maturation of the protein substrate. (springer.com)
  • Since then, p97 has been shown to play a critical role in the degradation of misfolded membrane and secretory proteins ( 4 ) and has also been linked to a broad array of cellular processes, including Golgi membrane reassembly ( 5 ), membrane transport ( 6 ), regulation of myofibril assembly ( 7 ), cell division ( 8 ), formation of protein aggregates ( 9 ), and autophagosome maturation ( 10 , 11 ). (pnas.org)
  • Endogenous F(1)F(o)-ATPase inhibitor limiting ATP depletion when the mitochondrial membrane potential falls below a threshold and the F(1)F(o)-ATP synthase starts hydrolyzing ATP to pump protons out of the mitochondrial matrix. (genecards.org)
  • The common and key step in the activation of all 3 Raf isoforms is membrane recruitment by a Ras family protein. (axonmedchem.com)
  • extracellular
  • It is an extracellular protein which shows the secondary and tertiary structure of serpin and binds to collagen-1 and heparin. (hindawi.com)
  • The most promiscuous of the 11 human MKPs is MKP-1, which can dephosphorylate p38, c-Jun NH 2 -terminal kinase and extracellular signaling-related protein kinase (Erk) 1/2 in vitro. (aspetjournals.org)
  • ATPase
  • A specific small-molecule inhibitor of p97 would provide an important tool to investigate diverse functions of this essential ATPase associated with diverse cellular activities (AAA) ATPase and to evaluate its potential to be a therapeutic target in human disease. (pnas.org)
  • The planar tri- and tetracyclic analogs inhibited KSP ATPase in an ATP-competitive manner just like biphenyl-type inhibitors. (nih.gov)
  • encodes
  • Here, we isolated and functionally characterized the pepper (Capsicum annuum L.) gene CaPMEI1, which encodes a pectin methylesterase inhibitor protein (PMEI), in pepper leaves infected by Xanthomonas campestris pv. (deepdyve.com)
  • This gene encodes a tumor suppressor protein that can induce cell growth arrest and apoptosis. (abnova.com)
  • Compound
  • In a continuing search for new protein phosphatase inhibitors from fungi, we have isolated a new compound, named penostatin J ( 1 ), together with three known ones, penostatin C ( 2 ), penostatin A ( 3 ), and penostatin B ( 4 ), from cultures of the entomogenous fungus Isaria tenuipes. (mdpi.com)
  • sequence
  • The SLAP-2 protein contains an NH 2 -terminal myristoylation consensus sequence and SH3 and SH2 Src homology domains, but lacks a tyrosine kinase domain. (rupress.org)
  • Sequence analysis and structural comparisons reveal that BVU2987 and other DUF2874 proteins are related to β-lactamase inhibitor protein, PepSY and SmpA_OmlA proteins and hence are likely to function as inhibitory proteins. (nih.gov)
  • The crystallized protein (including residues 20-145) was expressed with a tag that was removed during purification, leaving Gly0 followed by the target sequence (starting from residue 20). (nih.gov)
  • inhibits
  • DBeQ also potently inhibits cancer cell growth and is more rapid than a proteasome inhibitor at mobilizing the executioner caspases-3 and -7. (pnas.org)
  • We have recently identified a JAK‐binding protein (JAB) that inhibits JAK signaling in cells. (embopress.org)
  • substrates
  • Dual-reporter cell lines that simultaneously express p97-dependent and p97-independent proteasome substrates were used to stratify inhibitors that emerged from the screen. (pnas.org)
  • neuronal
  • We examined the endogenous expression of four members of the IAP family, X chromosome‐linked IAP (XIAP), rat IAP1 (RIAP1), RIAP2, and neuronal apoptosis inhibitory protein (NAIP), by semiquantitative reverse PCR and immunoblot analysis in cultured cerebellar granule neurons. (deepdyve.com)
  • Signaling
  • Despite its inhibitory effect on Gβγ-mediated signaling, Nb5 has no effect on Gα q -mediated and Gα s -mediated signaling events in living cells. (nih.gov)
  • XIAP
  • Cerebellar granule neurons express significant levels of RIAP2 mRNA and protein, but expression of RIAP1, NAIP, and XIAP was not detected. (deepdyve.com)