Inhibition studies of some serine and thiol proteinases by new leupeptin analogs

1993 ◽  
Vol 36 (8) ◽  
pp. 1084-1089 ◽  
Author(s):  
Rose M. McConnell ◽  
J. Lyndal York ◽  
Donna Frizzell ◽  
Carole Ezell
Keyword(s):  
Inhibition Studies ◽  
Thiol Proteinases

scholarly journals Inhibition studies of an intracellular inhibitor on thiol proteinases

FEBS Letters ◽  
1978 ◽  
Vol 91 (2) ◽  
pp. 355-359 ◽  
Author(s):  
M. Kopitar ◽  
J. Brzin ◽  
T. Zvonar ◽  
P. Ločnikar ◽  
I. Kregar ◽  
...  
Keyword(s):  
Inhibition Studies ◽  
Thiol Proteinases

Difference of [Ca2+]i Movements in Platelets Stimulated by Thrombin and TRAP: the Involvement of αIIbβ3-Mediated TXA2 Synthesis

1998 ◽  
Vol 79 (06) ◽  
pp. 1184-1190 ◽  
Author(s):  
Yoshiaki Tomiyama ◽  
Shigenori Honda ◽  
Kayoko Senzaki ◽  
Akito Tanaka ◽  
Mitsuru Okubo ◽  
...  
Keyword(s):  
Platelet Aggregation ◽  
Fibrinogen Binding ◽  
Adp Release ◽  
The Difference ◽  
Txa2 Receptor Antagonist ◽  
High Level ◽  
Inhibition Studies ◽  
Peak Increase ◽  
Second Peak ◽  
Assay Conditions

SummaryThis study investigated the difference of [Ca2+]i movement in platelets in response to thrombin and TRAP. The involvement of αIIbβ3 in this signaling was also studied. Stimulation of platelets with thrombin at 0.03 U/ml caused platelet aggregation and a two-peak increase in [Ca2+]i. The second peak of [Ca2+]i, but not the first peak was abolished by the inhibition of platelet aggregation with αIIbβ3 antagonists or by scavenging endogenous ADP with apyrase. A cyclooxygenase inhibitor, aspirin, and a TXA2 receptor antagonist, BM13505, also abolished the second peak of [Ca2+]i but not the first peak, although these regents did not inhibit aggregation. Under the same assay conditions, measurement of TXB2 demonstrated that αIIbβ3 antagonists and aspirin almost completely inhibited the production of TXB2. In contrast to thrombin-stimulation, TRAP caused only a single peak of [Ca2+]i even in the presence of platelet aggregation, and a high level of [Ca2+]i increase was needed for the induction of platelet aggregation. The inhibition of aggregation with αIIbβ3 antagonists had no effect on [Ca2+]i change and TXB2 production induced by TRAP. Inhibition studies using anti-GPIb antibodies suggested that GPIb may be involved in the thrombin response, but not in the TRAP. Our findings suggest that low dose thrombin causes a different [Ca2+]i response and TXA2 producing signal from TRAP. Endogenous ADP release and fibrinogen binding to αIIbβ3 are responsible for the synthesis of TXA2 which results in the induction of the second peak of [Ca2+]i in low thrombin- but not TRAP-stimulated platelets.

Isolation and Characterization of Plasminogen Activator from Pig Leucocytes

1974 ◽  
Vol 31 (01) ◽  
pp. 072-085 ◽  
Author(s):  
M Kopitar ◽  
M Stegnar ◽  
B Accetto ◽  
D Lebez
Keyword(s):  
Molecular Weight ◽  
Plasminogen Activator ◽  
Gel Electrophoresis ◽  
Gel Filtration ◽  
Ph Optimum ◽  
Isolation And Characterization ◽  
Ph Range ◽  
Inhibition Studies ◽  
Final Purification

SummaryPlasminogen activator was isolated from disrupted pig leucocytes by the aid of DEAE chromatography, gel filtration on Sephadex G-100 and final purification on CM cellulose, or by preparative gel electrophoresis.Isolated plasminogen activator corresponds No. 3 band of the starting sample of leucocyte cells (that is composed from 10 gel electrophoretic bands).pH optimum was found to be in pH range 8.0–8.5 and the highest pH stability is between pH range 5.0–8.0.Inhibition studies of isolated plasminogen activator were performed with EACA, AMCHA, PAMBA and Trasylol, using Anson and Astrup method. By Astrup method 100% inhibition was found with EACA and Trasylol and 30% with AMCHA. PAMBA gave 60% inhibition already at concentration 10–3 M/ml. Molecular weight of plasminogen activator was determined by gel filtration on Sephadex G-100. The value obtained from 4 different samples was found to be 28000–30500.

Mycobacterial DNA GyrB Inhibitors: Ligand Based Pharmacophore Modelling and In Vitro Enzyme Inhibition Studies

2014 ◽  
Vol 14 (17) ◽  
pp. 1990-2005 ◽  
Author(s):  
Shalini Saxena ◽  
Janupally Renuka ◽  
Variam Jeankumar ◽  
Perumal Yogeeswari ◽  
Dharmarajan Sriram
Keyword(s):  
Enzyme Inhibition ◽  
Pharmacophore Modelling ◽  
Inhibition Studies

Synthesis, Characterization and Cholinesterase Inhibition Studies of New Arylidene Aminothiazolylethanone Derivatives

2017 ◽  
Vol 13 (7) ◽  
Author(s):  
Pervaiz A. Channar ◽  
Muhammad S. Shah ◽  
Aamer Saeed ◽  
Shafi U. Khan ◽  
Fayaz A. Larik ◽  
...  
Keyword(s):  
Cholinesterase Inhibition ◽  
Inhibition Studies

Synthesis and Photoproperties of a Substituted Zinc(II) Phthalocyanine-N-(2-hydroxypropyl)methacrylamide Copolymer Conjugate

1993 ◽  
Vol 58 (10) ◽  
pp. 2321-2336 ◽  
Author(s):  
Zhong-wei Gu ◽  
John D. Spikes ◽  
Pavla Kopečková ◽  
Jindřich Kopeček
Keyword(s):  
Organic Solvents ◽  
Water Soluble ◽  
Lower Probability ◽  
Hpma Copolymer ◽  
Polymeric Derivative ◽  
Oxygen Generation ◽  
Hpma Copolymers ◽  
Hydroxypropyl Methacrylamide ◽  
Polymeric Carriers ◽  
Thiol Proteinases

In cancer photodynamic therapy (PDT), improved efficiency of photosensitizer delivery to tumors may be obtained by binding them to targetable water soluble polymeric carriers. However, attachment of photosensitizers to Macromolecular carriers may alter their spectral and photosensitizing properties. In this study, a new monosubstituted phthalocyanine derivative, N-glycyl zinc(II) 4,9,16,23-tetraaminophthalocyanine (G-TAPC-Zn) was synthesized by the reaction of zinc(II) 4,9,16,23-tetraaminophthalocyanine (TAPC-Zn) with N-tert-butoxycarbonyl-glycine N'-hydroxybenzotriazole ester followed by deprotection of the tert-butoxycarbonyl (BOC) group. G-TAPC-Zn contains an aliphatic amino group suitable for attachment to water soluble polymeric carriers. By aminolysis of a polymeric precursor, an N-(2-hydroxypropyl)methacrylamide (HPMA) copolymer containing oligopeptide (GFLG) side-chains terminated in p-nitrophenyl ester groups, with G-TAPC-Zn a polymeric derivative of the latter (P-GFLGG-TAPC-Zn) was synthesized. Spectral data indicated that in aqueous solutions P-GFLGG-TAPC-Zn formed aggregates. The degree of aggregation decreased with increasing concentration of detergents or organic solvents in buffer solutions. Consequently, the release of the drug from carrier catalyzed by thiol proteinases, papain or cathepsin B, took place only in the presence of detergents or organic solvents, i.e., under conditions with a lower probability of aggregate formation. Binding of G-TAPC-Zn to HPMA copolymers decreased the quantum yield of singlet oxygen generation from 0.24 to 0.063 and significantly increased its resistance to photobleaching.

scholarly journals Substrate specificity and inhibition studies of human serotonin N-acetyltransferase.

2000 ◽  
Vol 275 (50) ◽  
pp. 39799
Author(s):  
Gilles Ferry ◽  
Armelle Loynel ◽  
Nathalie Kucharczyk ◽  
Sophie Bertin ◽  
Marianne Rodriguez ◽  
...  
Keyword(s):  
Substrate Specificity ◽  
Inhibition Studies
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