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serin protease inhibitor

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https://www.readbyqxmd.com/read/28088469/estrogen-induced-expression-of-tissue-factor-pathway-inhibitor-2-in-mcf7-cells-involves-lysine-specific-demethylase-1
#1
Marianne S Andresen, Huda Omar Ali, Christiane Filion Myklebust, Per Morten Sandset, Benedicte Stavik, Nina Iversen, Grethe Skretting
Hormone-sensitive cancers can be influenced by estrogens, a process usually mediated through the estrogen receptor (ER). Tissue factor pathway inhibitor type 2 (TFPI-2) is a Kunitz-type serine protease inhibitor involved in regulating the extracellular matrix. The present study demonstrates that the expression of TFPI-2 can be induced by estrogens. Breast cancer data from GOBO displayed increased levels of TFPI-2 and increased survival in patients with ERα+ tumors. Treatment of MCF7 cells (ERα+) with 17β-estradiol (E2) or 17α-ethinyl estradiol (EE2) increased TFPI-2 mRNA and protein levels...
January 11, 2017: Molecular and Cellular Endocrinology
https://www.readbyqxmd.com/read/28087168/synthesis-structure-activity-relationships-studies-of-benzoxazinone-derivatives-as-%C3%AE-chymotrypsin-inhibitors
#2
Bishnu P Marasini, Fazal Rahim, Shahnaz Perveen, Aneela Karim, Khalid Mohammed Khan, Atta-Ur-Rahman, M Iqbal Choudhary
A series of benzoxazinones 1-28 were synthesized via reaction of anthranilic acid with various substituted benzoyl chlorides in the presence of triethylamine in chloroform. Compounds 1-18 showed a good inhibition of α-chymotrypsin with IC50±SEM values between 6.5 and 341.1μM. Preliminary structure-activity relationships studies indicated that the presence of substituents on benzene ring reduces the inhibitory potential of benzoxazinone. Also the increased inhibitory potential due to fluoro group at phenyl substituent was observed followed by chloro and bromo substituents...
January 4, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28069642/alpha-1-antitrypsin-enhances-islet-engraftment-by-suppression-of-instant-blood-mediated-inflammatory-reaction
#3
Jingjing Wang, Zhen Sun, Wenyu Gou, David B Adams, Wanxing Cui, Katherine A Morgan, Charlie Strange, Hongjun Wang
Islet cell transplantation has limited effectiveness because of an instant blood-mediated inflammatory reaction (IBMIR) that occurs immediately after cell infusion and leads to dramatic β cell death. In intraportal islet transplantation models using mouse and human islets, we demonstrated that alpha-1 antitrypsin (AAT, Prolastin-C), a serine protease inhibitor used for the treatment of AAT deficiency, inhibits IBMIR and cytokine-induced inflammation in islets. In mice, more diabetic recipients reached normoglycemia after intraportal islet transplantation when they were treated with AAT compared to mice treated with saline...
January 9, 2017: Diabetes
https://www.readbyqxmd.com/read/28067849/pnserpin-a-novel-serine-protease-inhibitor-from-extremophile-pyrobaculum-neutrophilum
#4
Huan Zhang, Rui Fei, Baigong Xue, Shanshan Yu, Zuoming Zhang, Sheng Zhong, Yuanqi Gao, Xiaoli Zhou
Serine protease inhibitors (serpins) are native inhibitors of serine proteases, constituting a large protein family with members spread over eukaryotes and prokaryotes. However, only very few prokaryotic serpins, especially from extremophiles, have been characterized to date. In this study, Pnserpin, a putative serine protease inhibitor from the thermophile Pyrobaculum neutrophilum, was overexpressed in Escherichia coli for purification and characterization. It irreversibly inhibits chymotrypsin-, trypsin-, elastase-, and subtilisin-like proteases in a temperature range from 20 to 100 °C in a concentration-dependent manner...
January 7, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28065272/activity-assays-for-rhomboid-proteases
#5
E Arutyunova, K Strisovsky, M J Lemieux
Rhomboids are ubiquitous intramembrane serine proteases that are involved in various signaling pathways. This fascinating class of proteases harbors an active site buried within the lipid milieu. High-resolution structures of the Escherichia coli rhomboid GlpG with various inhibitors revealed the catalytic mechanism for rhomboid-mediated proteolysis; however, a quantitative characterization was lacking. Assessing an enzyme's catalytic parameters is important for understanding the details of its proteolytic reaction and regulatory mechanisms...
2017: Methods in Enzymology
https://www.readbyqxmd.com/read/28065267/mechanism-and-inhibition-of-rhomboid-proteases
#6
K Strisovsky
Intramembrane serine proteases of the rhomboid family are widespread, and their gradually uncovered functions in different organisms already suggest medical relevance for infectious diseases and cancer. However, selective inhibitors that could serve as research tools for rhomboids, for validation of their disease relevance, or as templates for drug development are lacking. Here I summarize the current knowledge about rhomboid protease mechanism and specificity, overview the currently used inhibitors, and conclude by proposing avenues for future development of rhomboid protease inhibitors...
2017: Methods in Enzymology
https://www.readbyqxmd.com/read/28064070/maspin-inhibits-macrophage-phagocytosis-and-enhances-inflammatory-cytokine-production-via-activation-of-nf-%C3%AE%C2%BAb-signaling
#7
Yimeng Wang, Luguo Sun, Zhenbo Song, Danfeng Wang, Yongli Bao, Yuxin Li
Maspin (mammary serine protease inhibitor) is a non-inhibitory member of the serine protease inhibitor superfamily and a tumor suppressor in several cancers due to its ability to inhibit cell invasion, angiogenesis, and promote apoptosis. However, its immunomodulatory function remains largely unexplored. Thus, we explored the potential link between Maspin and macrophage function, first evaluating the regulatory effects of conditioned medium (CM) of a Maspin-overexpressing CHO cell strain on mouse peritoneal macrophage phagocytosis and cytokine secretion...
January 5, 2017: Molecular Immunology
https://www.readbyqxmd.com/read/28060882/secretion-of-proteases-by-an-opportunistic-fungal-pathogen-scedosporium-aurantiacum
#8
Zhiping Han, Liisa Kautto, Helena Nevalainen
Scedosporium aurantiacum is an opportunistic filamentous fungus increasingly isolated from the sputum of cystic fibrosis patients, and is especially prevalent in Australia. At the moment, very little is known about the infection mechanism of this fungus. Secreted proteases have been shown to contribute to fungal virulence in several studies with other fungi. Here we have compared the profiles of proteases secreted by a clinical isolate Scedosporium aurantiacum (WM 06.482) and an environmental strain (WM 10...
2017: PloS One
https://www.readbyqxmd.com/read/28059686/the-role-of-spinal-thrombin-through-protease-activated-receptor-1-in-hyperalgesia-after-neural-injury
#9
Jenell R Smith, Beth A Winkelstein
OBJECTIVE Painful neuropathic injuries induce blood-spinal cord barrier (BSCB) breakdown, allowing pro-inflammatory serum molecules to cross the BSCB, which contributes to nociception. The goal of these studies was to determine whether the blood-borne serine protease thrombin also crosses a permeable BSCB, contributing to nociception through its activation of protease-activated receptor-1 (PAR1). METHODS A 15-minute C-7 nerve root compression, which induces BSCB breakdown and painful behaviors by Day 1, was administered in the rat (n = 10); sham operation (n = 11) and a 3-minute compression (n = 10) that does not induce sensitivity were administered as controls...
January 6, 2017: Journal of Neurosurgery. Spine
https://www.readbyqxmd.com/read/28058009/visceral-hypersensitivity-in-inflammatory-bowel-diseases-and-irritable-bowel-syndrome-the-role-of-proteases
#10
REVIEW
Hannah Ceuleers, Hanne Van Spaendonk, Nikita Hanning, Jelena Heirbaut, Anne-Marie Lambeir, Jurgen Joossens, Koen Augustyns, Joris G De Man, Ingrid De Meester, Benedicte Y De Winter
Proteases, enzymes catalyzing the hydrolysis of peptide bonds, are present at high concentrations in the gastrointestinal tract. Besides their well-known role in the digestive process, they also function as signaling molecules through the activation of protease-activated receptors (PARs). Based on their chemical mechanism for catalysis, proteases can be classified into several classes: serine, cysteine, aspartic, metallo- and threonine proteases represent the mammalian protease families. In particular, the class of serine proteases will play a significant role in this review...
December 21, 2016: World Journal of Gastroenterology: WJG
https://www.readbyqxmd.com/read/28051346/a-conjugate-of-two-tpa-binding-rna-aptamers-efficiently-inhibits-fibrinolysis
#11
Nils Bjerregaard, Daniel M Dupont, Peter A Andreasen
Uncontrolled bleeding is a major cause of mortality. Lysine analogues are routinely used in the management of bleeding, but several studies indicate a risk of serious detrimental effects upon their administration. In this study, we report a bivalent conjugate "3218" of two RNA aptamers selected for binding to the serine protease tissue-type plasminogen activator (tPA), the principal initiator of fibrinolysis in mammals. The constituent monomeric aptamers, K32v2 and K18v2, were previously demonstrated to weakly inhibit fibrinolysis...
January 4, 2017: Nucleic Acid Therapeutics
https://www.readbyqxmd.com/read/28045523/design-of-potent-and-selective-cathepsin-g-inhibitors-based-on-the-sunflower-trypsin-inhibitor-1-scaffold
#12
Joakim Erik Swedberg, Choi Yi Li, Simon J de Veer, Conan K Wang, David J Craik
Neutrophils are directly responsible for destroying invading pathogens via reactive oxygen species, antimicrobial peptides and neutrophil serine proteases (NSPs). Imbalance between NSP activity and endogenous protease inhibitors is associated with chronic inflammatory disorders and engineered inhibitors of NSPs is a potential therapeutic pathway. In this study we characterised the extended substrate specificity (P4-P1) of the NSP cathepsin G using a peptide substrate library. Substituting preferred cathepsin G substrate sequences into the sunflower trypsin inhibitor-1 (SFTI-1) produced a potent cathepsin G inhibitor (Ki = 0...
January 3, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28045393/recombinant-hepatocyte-growth-factor-activator-inhibitor-1-expression-in-drosophila-s2-cells-purification-and-crystallization
#13
Min Liu, Cai Yuan, Yunbin Jiang, Longguang Jiang, Mingdong Huang
Hepatocyte growth factor activator inhibitor 1 (HAI-1) is a multi-domain membrane-associated protease inhibitor that potently inhibits a variety of serine proteases such as hepatocyte growth factor activator and matriptase. Different truncates of HAI-1 show varying potencies for inhibition of target proteases, suggesting that the domain organization of HAI-1 plays a critical role in its function. Here, the soluble full-length extracellular part of HAI-1 (sHAI-1) was expressed using the Drosophila S2 insect-cell expression system...
January 1, 2017: Acta Crystallographica. Section F, Structural Biology Communications
https://www.readbyqxmd.com/read/28043634/mycobacterial-excretory-secretory-31-protein-with-serine-protease-and-lipase-activities-an-immunogen-and-drug-target-against-tuberculosis-infection
#14
Bhaskar C Harinath
OBJECTIVE/BACKGROUND: Tuberculosis (TB) has been declared as a global emergency by the World Health Organization in 1993 and still remains one of the world's biggest threats. Worldwide, 9.6 million people have been estimated to have fallen ill with TB in 2014: 5.4 million men, 3.2 million women, and 1.0 million children. To reduce this burden, detection and treatment gaps must be addressed and new tools developed (Global TB report 2015). METHODS: Seroreactivity of the purified excretory secretory (ES) antigens ES-31, ES-43, ES-41, and ES-6 have been assessed in pulmonary TB (fresh, relapse, chronic, and latent), extrapulmonary TB, and in human immunodeficiency virus-TB coinfection...
December 2016: International Journal of Mycobacteriology
https://www.readbyqxmd.com/read/28043383/the-putative-serine-protease-inhibitor-serpin-genes-encoded-on-echinococcus-multilocularis-genome-and-their-expressions-in-metacestodal-stage
#15
Mizuki Sasaki, Yasuhito Sako
Two putative serpin genes were identified in Echinococcus multilocularis, in addition to the already reported serpinEmu, and were designated as serpin2Emu and serpin3Emu. Western blot analysis using polyclonal antibodies against serpinEmu, putative serpin2Emu protein, and putative serpin3Emu protein indicated that all three proteins were localized in both intracellular and excretory-secretory (ES) fractions of E. multilocularis metacestodes. In addition, immune staining of parasite tissue indicated that all three proteins were localized at the germinal layer...
January 15, 2017: Veterinary Parasitology
https://www.readbyqxmd.com/read/28034741/identification-of-novel-small-molecule-inhibitors-against-ns2b-ns3-serine-protease-from-zika-virus
#16
Hyun Lee, Jinhong Ren, Salvatore Nocadello, Amy J Rice, Isabel Ojeda, Samuel Light, George Minasov, Jason Vargas, Dhanapalan Nagarathnam, Wayne F Anderson, Michael E Johnson
Zika flavivirus infection during pregnancy appears to produce higher risk of microcephaly, and also causes multiple neurological problems such as Guillain-Barré syndrome. The Zika virus is now widespread in Central and South America, and is anticipated to become an increasing risk in the southern United States. With continuing global travel and the spread of the mosquito vector, the exposure is expected to accelerate, but there are no currently approved treatments against the Zika virus. The Zika NS2B/NS3 protease is an attractive drug target due to its essential role in viral replication...
December 26, 2016: Antiviral Research
https://www.readbyqxmd.com/read/28019718/excretions-secretions-from-medicinal-larvae-lucilia-sericata-inhibit-complement-activation-by-two-mechanisms
#17
Tetsuro Tamura, Gwendolyn Cazander, Suzan H M Rooijakkers, Leendert A Trouw, Peter H Nibbering
Larvae of the blowfly Lucilia sericata facilitate wound healing by removing dead tissue and biofilms from non-healing and necrotic wounds. Another beneficial action of larvae and their excretions/secretions (ES) is down-regulation of excessive inflammation. As prolonged complement activation is key to excessive inflammation, the aim of this study was to elucidate the mechanisms underlying the anti-complement activities of ES. Results revealed that heat sensitive serine proteases in ES degrade multiple complement proteins in all steps of the three complement activation pathways...
December 26, 2016: Wound Repair and Regeneration
https://www.readbyqxmd.com/read/28019702/alkaline-serine-proteases-from-helicoverpa-armigera-potential-candidates-for-industrial-applications
#18
Shaik Mohammad Akbar, Hari Chand Sharma
We characterized trypsin- and chymotrypsin-like serine alkaline proteases from cotton bollworm, Helicoverpa armigera, for their probable potential application as additives in various bio-formulations. Purification was achieved by using hydroxylapatite, DEAE sephadex and CM sephadex columns, which resulted in increased enzyme activity by 13.76- and 14.05-fold for trypsin and chymotrypsin, respectively. Michaelis-Menten constants (Km ) for substrates of trypsin and chymotrypsin, BApNA and SAAPFpNA, were found to be 1...
December 26, 2016: Archives of Insect Biochemistry and Physiology
https://www.readbyqxmd.com/read/28011221/structure-activity-relationships-of-4-hydroxy-4-biaryl-proline-acylsulfonamide-tripeptides-a-series-of-potent-ns3-protease-inhibitors-for-the-treatment-of-hepatitis-c-virus
#19
Alan Xiangdong Wang, Jie Chen, Qian Zhao, Li-Qiang Sun, Jacques Friborg, Fei Yu, Dennis Hernandez, Andrew C Good, Herbert E Klei, Ramkumar Rajamani, Kathy Mosure, Jay O Knipe, Danshi Li, Jialong Zhu, Paul C Levesque, Fiona McPhee, Nicholas A Meanwell, Paul M Scola
The design and synthesis of a series of tripeptide acylsulfonamides as potent inhibitors of the HCV NS3/4A serine protease is described. These analogues house a C4 aryl, C4 hydroxy-proline at the S2 position of the tripeptide scaffold. Information relating to structure-activity relationships as well as the pharmacokinetic and cardiovascular profiles of these analogues is provided.
December 9, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28008946/htra2-suppresses-autoimmune-arthritis-and-regulates-activation-of-stat3
#20
Seung Hoon Lee, Young-Mee Moon, Hyeon-Beom Seo, Se-Young Kim, Eun-Kyung Kim, Junyeong Yi, Min-Kyung Nam, Jun-Ki Min, Sung-Hwan Park, Hyangshuk Rhim, Mi-La Cho
Rheumatoid arthritis (RA) is an autoimmune disease that is related to the induction of T helper (Th)17 cells, which secrete interleukin-17, and activation of the signal transducer and activator of transcription (STAT) 3. The expression of high-temperature requirement protein A (HtrA) 2, a serine protease involved in apoptosis, was decreased in RA patients nonresponsive to drug treatment of RA. The aim of this study was to determine whether overexpression of HtrA2 has a therapeutic effect on RA. Th17 differentiation, osteoclastogenesis, and lymphocyte activation are increased in motor neuron degeneration (mnd)2 mice, which lack HtrA2 activity because of a missense mutation (Ser276Cys) in the protease domain of HtrA2...
December 23, 2016: Scientific Reports
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