OBJECTIVETo measure imaging data of occipitocervical angle in healthy people at different ages by X-ray.METHODSOne hundred and fifty asymptomatic volunteers(75 males and 75 females) aged from 20 and 70 years old with an average of(44.83±13.88) years old were divided into 5 groups according to different ages(20 to 29 years old, 30 to 39 years old, 40 to 49 years old, 50 to 59 years old and 60 to 70 years old), and 30 people in each group. All people underwent lateral radiography of neck on neutral position. McGregor line (the lowest connection line between upper margin of hard palate and occipital scales of plating), occipitocervical angle(OCA) formed by edge of C2 vertebral body, takami's occipitocervical angle formed between connection line of posterior marginal of C2 vertebral body and parallel lines of hard palate were collected. The data were performed statistical analysis according to gender and different ages, and analyzed correlation between OCA and TOCA.RESULTSOCA of 75 males at different ages were (14.71±3.09)° and(14.22±4.27)° in 75 females. TOCA of 75 males at different ages were (90.50±4.63)° and (90.57±6.67) ° in 75 females. There were no statistical difference in OCA and TOCA in people at different ages(P<0.05). There were no significant meaning among 5 groups at different ages in OCA and TOCA(P>0.05). The relation analysis results showed positive correlation between OCA and TOCA(r=0.454, P<0.01).CONCLUSIONSThe paper provided normal values for occipitocervical angle in population of southwestern China between 20 and 70 years old, and results may be useful for posterior occipitocervical fixation and fusion.

01 Jan 2002·European Journal of Nuclear Medicine and Molecular ImagingQ1 · MEDICINE

Comparison of radioiodinated TOC, TOCA and Mtr-TOCA: the effect of carbohydration on the pharmacokinetics

Q1 · MEDICINE

Article

Author: Ingo Wolf ; Hans-Jürgen Wester ; Jean-Claude Reubi ; Margret Schottelius ; Klemens Scheidhauer ; Markus Schwaiger

Although somatostatin-based peptide receptor imaging (sst-PRI) and peptide receptor radiotherapy (sst-PRRT) of human endocrine tumours and their metastases has become a valuable method, the experience with radiohalogenated sst-directed peptides has so far been disappointing. To extend the broad spectrum of radiohalogens with suitable radionuclide properties for sst-PRI and PRRT, new strategies in ligand development are required. The major drawbacks to be overcome include fast hepatic uptake, high abdominal background activity and low tumour uptake. Recently we introduced radiolabelled glycated octreotides as a new series of sst-binding radiotracers with excellent physicochemical characteristics. In this study we compared [(125)I]Tyr(3)-octreotide ([(125)I]TOC, ( 1)), [(125)I]Tyr(3)-octreotate ([(125)I]TOCA, ( 2)) and a carbohydrated octreotide derivative, maltotriose-[(125)I]Tyr(3)-octreotate ([(125)I]Mtr-TOCA, ( 3)) to evaluate the effect of single C-terminal oxidation and simultaneous N-terminal carbohydration. The biodistribution was compared in nude mice bearing AR42J tumour xenografts. Compared with ( 1), activity uptake of ( 2) and ( 3) at 1 h was decreased in intestine [36% ( 2), 72% ( 3)], liver [62% ( 2), 79% ( 3)] and kidney [34% ( 2), 41% ( 3)], respectively. Blood clearance was fast for all compounds investigated. Using ( 1) as reference, tumour uptake of ( 2) and ( 3) was 3.8- and 4.3-fold higher at 1 h p.i. At 1 h the tumour-to-blood ratio of ( 3) was 28.2+/-7.3, and the tumour-to-muscle ratio, 147+/-48. Specificity of tumour uptake was demonstrated in AR42J tumour-bearing mice by pretreatment with 0.8 mg TOC/kg 5 min prior to injection of ( 3). In cells transfected with sst1-sst5, the binding profile of I-Mtr-TOCA revealed a very high affinity and selectivity for sst2. In a first scintigraphic [(123)I]Mtr-TOCA study of a patient with a carcinoid of the small intestine with known peritoneal carcinomatosis and a solitary liver metastasis, all tumour tissues, including the liver metastasis, were well defined and clearly visible as soon as 30 min p.i. Based on these encouraging findings we conclude that carbohydration is a powerful strategy for the development of new radiolabelled sst-binding peptides and may represent a general method to improve pharmacokinetics of other peptide radioligands. [(123)I]Mtr-TOCA is a very promising new candidate for sst-directed PRI.

01 Jan 2001·Free Radical Research

α-Tocopherol, but notγ-tocopherol inhibits 7β-hydroxycholesterol-induced apoptosis in human U937 cells

Article

Author: N.M. Lyons ; J.A. Woods ; N.M. O'Brien

Oxysterols, particularly those oxidised at position 7, are toxic to cells in culture and have been shown to induce apoptosis in cell types such as vascular endothelial cells, smooth muscle cells and monocytes. The precise mechanism by which oxysterols induce apoptosis is unknown but may involve the generation of oxidative stress. In the present study we examined the ability of alpha-TOC, alpha-TOC acetate (alpha-TOCA) and gamma-TOC to protect against 7 beta-hydroxycholesterol (7 beta-OHC)-induced apoptosis of human monocytic U937 cells. 7 beta-OHC is one of the most commonly detected oxysterols in foods and its level in plasma has been positively associated with an increased risk of atherosclerosis. The present study demonstrates a significant decrease in cell membrane integrity and cellular glutathione levels when U937 cells were treated with 30 microM 7 beta-OHC. DNA fragmentation also occurred, as measured by agarose gel electrophoresis, and the number of apoptotic cells increased as assessed by nuclear morphology. Analysis by HPLC showed that there was a greater incorporation of gamma-TOC into U937 cells after a 48 h incubation, than either alpha-TOC or alpha-TOCA. However, despite the increased uptake of gamma-TOC, only alpha-TOC, and not gamma-TOC or alpha-TOCA was effective at inhibiting 7 beta-OHC-induced apoptosis in U937 cells.

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Indication	Highest Phase	Country/Location	Organization	Date
Melanoma	Phase 1	US	Forte Biosciences, Inc.	12 Mar 2020

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ASCO2016 Manual	Phase 1	Glioblastoma	-	Toca511/Toca-FC	(ogqdhlrvba) = kdcitdzwsq mvungkfsmn (ttraygfjai )	Positive	20 May 2016
				lomustine	(ogqdhlrvba) = xvizofflub mvungkfsmn (ttraygfjai )

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