Search results for "Inhibition"
showing 10 items of 590 documents
Sugar specific cellular lectins of Phallusia mamillata hemocytes: Purification, characterization and evidence for cell surface localization
1989
Cellular lectins (CLs) of Phallusia mamillata were demonstrated in protein preparations obtained by salt fractionation from hemocytes sonicated in a suitable medium. Since the lectins from the precipitated fraction bind sugars containing D-galactosyl groups, they were purified by affinity chromatography on Sepharose. SDS-PAGE under reducing conditions showed that CLs are formed of two components of apparent MWs approximately 36,900 and 35,090 and thus differ from serum lectins (SLs) (MW about 62,200). The "shrinkage" observed when SLs were examined under nonreducing conditions suggest the presence of intrachain disulphide bonds which can affect the molecular structure of the SLs. CL-SL diff…
The action of iontophoretically applied acetylcholine and dopamine on single claustrum neurones in the cat.
1981
Abstract The effects of iontophoretically applied acetyl-choline (ACh) and dopamine (DA) on spontaneously active claustral neurones, in chloralose-anaesthetised cats, have been investigated. Acetylcholine had both facilitatory and inhibitory effects in almost the same proportions. The action of DA was prevalently inhibitory. Two types of inhibitory response to ACh and DA are described: short-lasting inhibition and long-lasting inhibition. The excitatory response always outlasted the period of drug application.
Single-digit nanomolar inhibitors lock the aromatase active site via a dualsteric targeting strategy
2022
The most frequently diagnosed breast cancer (BC) type in women expresses estrogen receptor (ER) , depends on estrogens for its growth, being classified as ER positive (ER+). The gold standard therapy for the treatment of this tumor relies on the inhibition of the aromatase enzyme, which catalyzes estrogen biosynthesis. Despite the clinical success of current aromatase inhibitors (AIs), after prolonged therapeutic regimens, BC ER + patients experience acquired resistance and disease relapse. This points up the urgent need for a newer generation of AIs able to overcome resistance issues, while mitigating toxicity and side effects of current therapies. Here we performed the synthesis, biologic…
2,3,7,8-Tetrachlorodibenzo-p-dioxin-Dependent Release from Contact Inhibition in WB-F344 Cells: Involvement of Cyclin A
2002
2,3,7,8-Tetrachlorodibenzo-p-dioxin (TCDD) is the most potent tumor promoter ever tested in rodents. Although it is known that most of TCDD actions are mediated by binding to the aryl hydrocarbon receptor (AhR), the mechanisms leading to tumor promotion still remain to be elucidated. Loss of contact inhibition is one characteristic hallmark in tumorigenesis. In rat liver epithelial WB-F344 cells, TCDD induces a release from contact inhibition, which is manifested by a twofold increase in cell number when TCDD (1 nM for 48 h) is added to confluent cells in the presence of serum, but not when given to exponentially growing or subconfluent, serum-deprived WB-F344 cells. Loss of G1 arrest was a…
Manipulation of glycolysis in malignant tumors: fantasy or therapy?
2009
After Warburg stated his hypothesis on tumor cell metabolism about 80 years ago, the field of carbohydrate metabolism of cancer cells and solid tumors is experiencing a boom for the past few years. Numerous studies have been focused on the characteristics of cancer metabolism and its accessibility to novel therapeutic interventions. Malignant transformation is associated with an increase in glycolytic flux, mainly caused by an upregulation of numerous glycolysis-related genes in the majority of human cancers. As a consequence of these alterations, tumor cells are producing lactate at higher levels compared to non-malignant tissue, even in the presence of oxygen, a phenomenon termed “aerobic…
Fluorescence induction kinetics as a tool to detect a chlororespiratory activity in the prasinophycean alga, Mantoniella squamata
1990
Abstract Pulse-modulated fluorescence measuring systems were used to study the fluorescence induction kinetics of the primitive prasinophycean alga, Mantoniella squamata . DCMU-treated cells show a very strong non-photochemical quenching which is insensitive to uncouplers and can not be attributed to state transitions or photoinhibition. In order to analyze the origin for this quenching, different inhibitors of the photosynthetic electron flow were applied. It was found that DCCD, an inhibitor of the ATP-synthase as well as of the cytochrome- c oxidase, enhances the fluorescence quenching, whereas antimycin A, which blocks the cyclic electron flow around PS I, stimulates it. The effect of b…
Photosynthesis of the red alga Gracilaria chilensis under natural solar radiation in an estuary in southern Chile
2005
The photosynthetic performance and pigment content of Gracilaria chilensis Bird, McLachlan, and Oliveira were measured under natural solar radiation in the Quempillen river estuary (southern Chile) in order to assess the short-term acclimation of this species to the current levels of ultraviolet (UV) radiation during midsummer. The effect of the tidal fluctuation was evaluated in algae exposed for 3 days to two light climates in cages suspended at two depths (0.5 and 1.5 m from the bottom). Responses to high solar radiation at noon were also assessed to gain insights into rapid photochemical kinetics and the degree of photoinhibition. Results indicated that G. chilensis is a shade-adapted s…
The Effect of Temperature and Radical Protection on the Photoinhibition of Spinach Thylakoids
1992
Photoinhibition of spinach thylakoids was studied by examination the inactivation of different parts of the electron transport chain, the decline of the variable fluorescence and the loss of atrazine binding sites. The results obtained after photoinhibition at 20° C and 0° C revealed an inactivation at the QB-site of the D1-protein as the first event in the course of photoinhibition. The natural antioxidants glutathione and ascorbate as well as the enzymes SOD and catalase diminished photoinhibition to similar extents. Further protection was achieved through combination of both radical defense systems. In addition to the radical scavenging properties glutathione and ascorbate have reducing …
Studies on the mechanism of photosystem II photoinhibition I. A two-step degradation of D1-protein
1990
The role of D1-protein in photoinhibition was examined. Photoinhibition of spinach thylakoids at 20°C caused considerable degradation of D1-protein and a parallel loss of variable fluorescence, QB-independent electron flow and QB-dependent electron flow. The breakdown of D1-protein as well as the loss of variable fluorescence and QB-independent electron flow were largely prevented when thylakoids were photoinhibited at 0°C. The QB-dependent electron flow markedly decreased under the same conditions. This inactivation may represent the primary event in photoinhibition and could be the result of some modification at the QB-site of D1-protein. Evidence for this comes from fluorescence relaxati…
Studies on the mechanism of photosystem II photoinhibition II. The involvement of toxic oxygen species.
1990
In a previous paper it was shown that photoinhibition of reaction centre II of spinach thylakoids was predominantly caused by the degradation of D1-protein. An initial inactivation step at the QB-site was distinguished from its breakdown. The present paper deals with the question as to whether this loss of QB-function is caused by oxygen radical attack. For this purpose the photoinhibition of thylakoids was induced at 20°C in the presence of either superoxide dismutase and catalase or the antioxidants glutathione and ascorbic acid. This resulted in comparable though not total protection of D1-protein, photochemistry and fluorescence from photoinhibition. The combined action of both the enzy…