Oligopeptides

Publication Title: 
Biotechnology and Applied Biochemistry

Angiotensin-I-converting enzyme (ACE) plays an important role in blood pressure regulation. In this study, an ACE-hexapeptide inhibitor (Asp-Glu-Asn-Ser-Lys-Phe) designated as chebulin was produced from the fruit protein of Terminalia chebula Retz. by pepsin digestion, ultrafiltrated through a 3 KDa cut-off membrane, a reverse-phase high-performance liquid chromatography, and nano-liquid chromatography tandem mass spectrometry analysis. Chebulin was found to inhibit ACE in a noncompetitive manner, as supported by the structural model.

Author(s): 
Sornwatana, Thakorn
Bangphoomi, Kunan
Roytrakul, Sittiruk
Wetprasit, Nuanchawee
Choowongkomon, Kiattawee
Ratanapo, Sunanta
Publication Title: 
Cell Metabolism

Changes in fat content have been associated with dietary restriction (DR), but whether they play a causal role in mediating various responses to DR remains unknown. We demonstrate that upon DR, Drosophila melanogaster shift their metabolism toward increasing fatty-acid synthesis and breakdown, which is required for various responses to DR. Inhibition of fatty-acid synthesis or oxidation genes specifically in the muscle tissue inhibited life-span extension upon DR. Furthermore, DR enhances spontaneous activity of flies, which was found to be dependent on the enhanced fatty-acid metabolism.

Author(s): 
Katewa, Subhash D.
Demontis, Fabio
Kolipinski, Marysia
Hubbard, Alan
Gill, Matthew S.
Perrimon, Norbert
Melov, Simon
Kapahi, Pankaj
Publication Title: 
Molecular and Biochemical Parasitology

Efforts to move from malaria control to eradication will require new approaches to block malaria transmission, such as the development of anti-malarial drugs with gametocytocidal activity. Here fluorescent oxidoreduction indicator alamarBlue is used to develop a screen for gametocyte viability. The fluorescent signal increases linearly with gametocyte number (R(2)=0.99) and determination of the IC(50) of epoxomicin demonstrated the assay was reproducible and sensitive (IC(50) 2.16±0.57 nM, Z'-factor 0.81±0.01).

Author(s): 
Tanaka, Takeshi Q.
Williamson, Kim C.
Publication Title: 
Antimicrobial Agents and Chemotherapy

Despite declining numbers of cases and deaths, malaria remains a major public health problem in many parts of the world. Today, case management relies heavily on a single class of antimalarial compounds: artemisinins. Hence, development of resistance against artemisinins may destroy current malaria control strategies. Beyond malaria control are elimination and eradication programs that will require drugs with good activity against acute infection but also with preventive and transmission-blocking properties.

Author(s): 
Tschan, Serena
Brouwer, Arwin J.
Werkhoven, Paul R.
Jonker, Anika M.
Wagner, Lena
Knittel, Sarah
Aminake, Makoah Nigel
Pradel, Gabriele
Joanny, Fanny
Liskamp, Rob M. J.
Mordmüller, Benjamin
Publication Title: 
Circulation

BACKGROUND: Developmentally regulated endothelial locus-1 (Del-1) is an extracellular matrix protein that is expressed by endothelial cells during embryological vascular development. We speculated that Del-1 may be reexpressed in ischemia and may be involved in endogenous angiogenesis. METHODS AND RESULTS: Del-1 protein was detected by immunohistochemistry in murine ischemic hindlimb after femoral artery excision. To determine whether exogenous Del-1 would augment angiogenesis in vivo, Del-1 or vehicle was administered for 3 weeks by intramuscular injection of murine ischemic hindlimbs.

Author(s): 
Ho, Hoai-Ky V.
Jang, James J.
Kaji, Shuichiro
Spektor, Gary
Fong, Annie
Yang, Phillip
Hu, Bob S.
Schatzman, Randy
Quertermous, Thomas
Cooke, John P.
Publication Title: 
Drug Metabolism and Disposition: The Biological Fate of Chemicals

The effect of atazanavir on P-glycoprotein (P-gp) expression and activity, as well as its inhibitory potency against CYP3A activity, was evaluated in vitro. Induction of P-gp activity and expression was studied using LS180V cells. P-gp inhibition was studied using both LS180V cells and Caco-2 cells. P-gp activity was assessed by measuring P-gp-mediated rhodamine 123 (Rh123) transport, and P-gp expression was determined using SDS-polyacrylamide gel electrophoresis/Western blot analysis. CYP3A inhibition was tested using triazolam hydroxylation in human liver microsomes (HLM).

Author(s): 
Perloff, Elke S.
Duan, Su X.
Skolnik, Paul R.
Greenblatt, David J.
von Moltke, Lisa L.
Publication Title: 
Journal of Immunology (Baltimore, Md.: 1950)

Chronic neutrophilic inflammation is a manifestation of a variety of lung diseases including cystic fibrosis (CF). There is increasing evidence that fragments of extracellular matrix proteins, such as collagen and elastin, play an important role in inflammatory cell recruitment to the lung in animal models of airway inflammation. Unfortunately, the association of these peptides with human disease and the identification of therapeutic targets directed toward these inflammatory pathways have remained elusive.

Author(s): 
Gaggar, Amit
Jackson, Patricia L.
Noerager, Brett D.
O'Reilly, Philip J.
McQuaid, D. Brent
Rowe, Steven M.
Clancy, J. P.
Blalock, J. Edwin
Publication Title: 
The American Journal of Pathology

Matrix metalloproteinase (MMP)-8 and MMP-9 play several roles in inflammation, including degradation of extracellular matrix (ECM) components and regulation of cytokine activity. To determine the roles of MMP-8 and MMP-9 in a neutrophil-dependent inflammatory response, we used a murine model of corneal inflammation in which LPS is injected into the corneal stroma.

Author(s): 
Lin, Michelle
Jackson, Patricia
Tester, Angus M.
Diaconu, Eugenia
Overall, Christopher M.
Blalock, J. Edwin
Pearlman, Eric
Publication Title: 
Respiratory Research

BACKGROUND: Chronic obstructive pulmonary disease (COPD) is a common respiratory disorder for which new diagnostic and therapeutic approaches are required. Hallmarks of COPD are matrix destruction and neutrophilic airway inflammation in the lung. We have previously described two tri-peptides, N-alpha-PGP and PGP, which are collagen fragments and neutrophil chemoattractants. In this study, we investigate if N-alpha-PGP and PGP are biomarkers and potential therapeutic targets for COPD.

Author(s): 
O'Reilly, Philip
Jackson, Patricia L.
Noerager, Brett
Parker, Suzanne
Dransfield, Mark
Gaggar, Amit
Blalock, J. Edwin
Publication Title: 
Journal of Neuroimmunology

Prolyl endopeptidase (PE), a protease that cleaves after proline residues in oligopeptides, is highly active in brain and degrades neuropeptides in vitro. We have recently demonstrated that PE, in concert with MMP's, can generate PGP (proline-glycine-proline), a novel, neutrophil chemoattractant, from collagen. In this study, we demonstrate that human peripheral blood neutrophils contain PE, which is constitutively active, and can generate PGP de novo from collagen after activation with LPS.

Author(s): 
O'Reilly, Philip J.
Hardison, Matthew T.
Jackson, Patricia L.
Xu, Xin
Snelgrove, Robert J.
Gaggar, Amit
Galin, F. Shawn
Blalock, J. Edwin

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