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Arun Kumar Singh et al.
International journal of infectious diseases : IJID : official publication of the International Society for Infectious Diseases, 16(5), e375-e381 (2012-03-14)
Staphylococcus aureus has emerged as a major drug-resistant pathogen in hospital- and community-acquired infections. Leucine aminopeptidase (LAP) is known to be essential for survival of the bacteria; however the LAP of S. aureus has not been extensively characterized. In this
Sebastian D Parlee et al.
PloS one, 7(12), e51072-e51072 (2012-12-12)
Chemerin is a leukocyte chemoattractant and adipokine with important immune and metabolic roles. Chemerin, secreted in an inactive form prochemerin, undergoes C-terminal proteolytic cleavage to generate active chemerin, a ligand for the chemokine-like receptor-1 (CMKLR1). We previously identified that adipocytes
Michael B Harbut et al.
Proceedings of the National Academy of Sciences of the United States of America, 108(34), E526-E534 (2011-08-17)
Malaria causes worldwide morbidity and mortality, and while chemotherapy remains an excellent means of malaria control, drug-resistant parasites necessitate the discovery of new antimalarials. Peptidases are a promising class of drug targets and perform several important roles during the Plasmodium
Daniela P Alves et al.
Pharmacology, 89(1-2), 22-28 (2012-01-13)
The aim of the present study was to investigate the mechanisms underlying the endogenous control of nociception at a peripheral level during inflammation. Using a pharmacological approach and the rat paw pressure test, we assessed the effect of an intraplantar
Xiaopan Zhang et al.
Journal of enzyme inhibition and medicinal chemistry, 28(3), 545-551 (2012-03-03)
Aminopeptidase N (APN/CD13) over expressed on tumour cells, plays a critical role in tumour invasion, metastasis and tumour angiogenesis. In this article, we described the design, synthesis and preliminary activity studies of novel 3-amino-2-hydroxyl-3-phenylpropanoic acid derivatives as APN inhibitors. The
ChuanYun Dai et al.
Science China. Life sciences, 56(1), 51-58 (2013-01-15)
To design a releasable PEGylated TNF-α (rPEG-TNF-α), a cathepsin B-sensitive dipeptide (Val-Cit moiety) was inserted into conventional PEG-modified TNF-α (PEG-TNF-α), facilitating its clinical use for anti-tumor therapy. Comparative pharmacokinetic and pharmacodynamic studies showed that the half-lives of both PEGylated forms
Jung-Mi Kang et al.
Molecular and biochemical parasitology, 182(1-2), 17-26 (2011-12-14)
Leucine aminopeptidases (LAP; EC 3.4.11.1) are a group of metalloexopeptidases, which catalyze the sequential removal of leucine amino acids from the N-termini of the polypeptides or proteins. In this study, we identified two novel genes that encode LAPs of Clonorchis
Atsushi Wakita et al.
International journal of hematology, 96(1), 84-93 (2012-05-29)
We conducted a multicenter prospective randomized study to compare a fixed-scheduled induction therapy with a response-oriented individualized induction therapy for elderly patients with acute myeloid leukemia (AML). Newly diagnosed AML patients, aged between 65 and 80, were randomly assigned to
Yanna Zhu et al.
Peptides, 33(2), 265-271 (2012-01-26)
Bestatin, a dipeptide, a low molecular weight aminopeptidase inhibitor, has been demonstrated to be an immunomodulator with an antitumor activity. However, the transporter-mediated renal excretion of bestatin is not fully understood. The purpose of this study was to elucidate the
Yekaterina Poloz et al.
Eukaryotic cell, 11(4), 545-557 (2012-02-22)
Bestatin methyl ester (BME) is an inhibitor of Zn(2+)-binding aminopeptidases that inhibits cell proliferation and induces apoptosis in normal and cancer cells. We have used Dictyostelium as a model organism to study the effects of BME. Only two Zn(2+)-binding aminopeptidases
Kanghui Yang et al.
Journal of enzyme inhibition and medicinal chemistry, 27(2), 302-310 (2011-07-21)
A series of novel L-isoserine derivatives were synthesised and evaluated for their ability to inhibit aminopeptidase N (APN)/CD13. In our preliminary biological results, some of these compounds possessed a potent inhibitory activity against the APN. Within this series, compound 14b
Florian Veillard et al.
The Journal of biological chemistry, 286(43), 37158-37167 (2011-09-08)
Human endostatin, a potent anti-angiogenic protein, is generated by release of the C terminus of collagen XVIII. Here, we propose that cysteine cathepsins are involved in both the liberation and activation of bioactive endostatin fragments, thus regulating their anti-angiogenic properties.
Kunio Fujiwara et al.
Journal of molecular histology, 42(6), 589-596 (2011-10-19)
The in vivo role of transporters in drug disposition, in the context of other transporters, and metabolism has not been established. We prepared an anti-bestatin serum against bestatin conjugated to albumin with glutaraldehyde (GA). The antiserum was specific for GA-conjugated
Magdalena Lis et al.
Pharmacological reports : PR, 63(6), 1481-1490 (2012-02-24)
The low-molecular weight dipeptide bestatin is a potent inhibitor of aminopeptidase N and has been demonstrated to have antitumor and immunomodulatory effects. The effects of bestatin on interleukin (IL)-1β synthesis and release by peritoneal macrophages stimulated in vitro with lipopolysaccharide
Florian Veillard et al.
Biological chemistry, 393(12), 1471-1476 (2013-05-15)
Bestatin, a specific inhibitor of metalloaminopeptidases,inhibits the growth of Porphyromonas gingivalis. To identify its target enzyme, a library of fluorescent substrates was used but no metalloaminopeptidase activity was found. The aminopeptidase activity of P. gingivalis was bestatin-insensitive and directed exclusively
Zeng Wang et al.
Sichuan da xue xue bao. Yi xue ban = Journal of Sichuan University. Medical science edition, 43(4), 609-611 (2012-09-25)
To establish a liquid chromatography tandem mass spectrometry method for the determination of ubenimex in human plasma. The essay was conducted with an API 3000 HPLC-MS/MS system consisted of a Ultimate C18 column (50 mm x 4.6 mm, 5 microm).
K Ota
Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie, 45(2-3), 55-60 (1991-01-01)
An immunomodulating agent, ubenimex (Bestatin) has low toxicity even after long-term oral administration and brings about significant modifications in immunological response. In a cooperative randomized controlled study of Bestatin immunotherapy for adult acute nonlymphocytic leukemia, prolongation of remission duration and
Mohammed Alamgir Sarker et al.
Bioscience, biotechnology, and biochemistry, 75(6), 1154-1159 (2011-06-15)
A novel aminopeptidase, Aminopeptidase T (APase T), was purified from porcine skeletal muscle following successive column chromatography: twice on DEAE-cellulose, hydroxyapatite, and Sephacryl S-200 HR using Leu-β-naphthylamide (LeuNap) as a substrate. The molecular mass of the enzyme was 69 kDa
Alan H M Wong et al.
The Journal of biological chemistry, 287(44), 36804-36813 (2012-08-31)
Human aminopeptidase N (hAPN/hCD13) is a dimeric membrane protein and a member of the M1 family of zinc metallopeptidases. Within the rennin-angiotensin system, its enzymatic activity is responsible for processing peptide hormones angiotensin III and IV. In addition, hAPN is
M Lis et al.
Polish journal of veterinary sciences, 14(3), 393-403 (2011-10-01)
Bestatin, a low-molecular weight dipeptide, is a potent inhibitor of aminopeptidase N which has been demonstrated to have antitumor and immunomodulatory effects. The effects of bestatin (10, 1 and 0.1 mg/kg) administered intraperitoneally once, five or ten times to mice
Ching-Feng Huang et al.
International archives of allergy and immunology, 158(2), 142-150 (2012-01-31)
DNA vaccines encoding allergens have been developed to prevent or to treat specific IgE responses. To evaluate the potential preventive and therapeutic effect of DNA vaccines encoding Cyn d 1 alone or combined with different adjuvants on specific allergies. Recombinant
Jian-Wei Xu et al.
Asian Pacific journal of cancer prevention : APJCP, 12(4), 985-987 (2011-07-28)
To evaluate the effect of ubenimex capsule on general performance and chemotherapy related toxicity in patients with advanced gastric cancer undergoing chemotherapy. Patients with advanced gastric cancer were randomly divided into two groups: with or without ubenimex. All received the
Magdalena Lis et al.
Immunopharmacology and immunotoxicology, 35(1), 133-138 (2012-09-11)
The effects of bestatin on humoral immune response to sheep erythrocytes (SRBC) and restoration of the response impaired by a single cyclophosphamide dose (350 mg/kg) were tested on mice. Bestatin (at doses of 10, 1, and 0.1 mg/kg) was administered intraperitoneally (i.p.)
Xi-Jun Qian et al.
Zhongguo shi yan xue ye xue za zhi, 19(5), 1125-1128 (2011-11-02)
This study was purposed to investigate the effect of aminopeptidase N/CD13 on bestatin enhancing all-trans-retinoic acid (ATRA)-inducing differentiation in NB4 cells. The nitroblue-tetrazolium (NBT) reduction assay was performed to determine the differentiation of NB4 cells, MR2 cells and primary APL
Pain inhibition by blocking leukocytic and neuronal opioid peptidases in peripheral inflamed tissue.
Anja Schreiter et al.
FASEB journal : official publication of the Federation of American Societies for Experimental Biology, 26(12), 5161-5171 (2012-08-28)
Inflammatory pain can be controlled by endogenous opioid peptides. Here we blocked the degradation of opioids in peripheral injured tissue to locally augment this physiological system. In rats with hindpaw inflammation, inhibitors of aminopeptidase N (APN; bestatin) or neutral endopeptidase
Ines Martin-Padura et al.
Laboratory investigation; a journal of technical methods and pathology, 92(7), 952-966 (2012-05-02)
Hepatocellular carcinoma (HCC) is the fifth most common solid tumor and the third leading cause of cancer-related deaths. Currently available chemotherapeutic options are not curative due in part to tumor resistance to conventional therapies. We generated orthotopic HCC mouse models
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