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T Vitali

Publications and source records attributed to T Vitali.

At least 19 recordsLinked to original sources

Premature termination mutations in exon 3 of the SMN1 gene are associated with exon skipping and a relatively mild SMA phenotype.

Autosomal recessive spinal muscular atrophy (SMA) is a common motor neuron disease caused by absence or mutation in the survival motor neuron (SMN1) gene. SNM1 and a nearly identical copy, SMN2, encode identical proteins, but SMN2 only produces a little full length protein due to alternative splicing. The level of functional SMN protein and the number of SMN2 genes correlate with the clinical phenotype ranging from severe to very mild. Here, we report on premature termination mutations in SMN1 exon 3 (425del5 and W102X) which induce skipping of the mutated exon. The novel nonsense mutation W102X was detected in two patients with a relatively mild phenotype who had only two copies of the SMN2 gene, a number that has previously been found associated with the severe form of SMA. We show that the shortened transcripts are translated into predicted in frame protein isoforms. Aminoglycoside treatment suppressed the nonsense mutation in cultured cells and abolished exon skipping. Fibroblasts from both patients show a high number of nuclear structures containing SMN protein (gems). These findings suggest that the protein isoform lacking the exon 3 encoded region contributes to the formation of the nuclear protein complex which may account for the milder clinical phenotype.

Adult↗

Detection of the survival motor neuron (SMN) genes by FISH: further evidence for a role for SMN2 in the modulation of disease severity in SMA patients.

Spinal muscular atrophy (SMA) is a common autosomal recessive neuromuscular disorder which presents with various clinical phenotypes ranging from severe to very mild. All forms are caused by the homozygous absence of the survival motor neuron ( SMN1 ) gene. SMN1 and a nearly identical copy ( SMN2 ) are located in a duplicated region at 5q13 and encode identical proteins. The genetic basis for the clinical variability of SMA remains unclear, but it has been suggested that the copy number of SMN2 could influence the disease severity. We have assessed the number of SMN2 genes in patients with different clinical phenotypes by fluorescence in situ hybridization (FISH) using as SMN probe a mixture of small specific DNA fragments. Gene copy number was established by FISH on interphase nuclei, but the presence of two SMN2 genes on the same chromosome could also be revealed by FISH on metaphase spreads. All patients had at least two SMN2 genes. We found two or three copies of SMN2 in severely affected type I patients, three copies in intermediately affected type II patients, generally four copies in mildly affected type III patients and four or eight copies in patients with very mild adult-onset SMA. No alterations of the genes were detected by Southern blot and sequence analysis, suggesting that all gene copies of SMN2 were intact. These data provide additional evidence that the SMN2 genes modulate the disease severity and suggest that knowledge of the gene copy number could be of some prognostic value.

Alleles↗

Construction of a 2.5-Mb integrated physical and gene map of distal 21q22.3.

The gene-rich telomeric region of 21q harbors several loci relevant to human diseases including autoimmune polyglandular disease type I, nonsyndromic deafness, Knobloch syndrome, holoprosencephaly, and bipolar affective disorder. A contig of genomic clones in this region would facilitate the isolation of these genes. However, distal 21q22.3 has yet been poorly mapped, presumably due to the presence of sequences that are underrepresented in yeast artificial chromosome (YAC) libraries. We generated a framework of YACs and used these clones as starting points for the isolation of a combination of bacterial artificial chromosome clones, P1-derived artificial chromosome clones, and cosmid clones by chromosome walking procedures. These studies resulted in the construction of a high-resolution contig map spanning the 2.5-Mb region from PFKL to the telomere, approximately 2 Mb of which are covered by ready-to-sequence contigs. Within this map we determined the location and relative distance of 21 markers. These include 9 established genetic markers, the order of which is cen-PFKL-D21S154-D21S170-D21S171-D21S1903- D21S1897- D21S112-D21S1446-D21S1575-tel. Moreover, we established the precise map position of 13 genes and 4 ESTs including the recently isolated genes C21ORF2, SMT3H1, RNA editing deaminase 1 (ADARB1), folate transporter (SLC19A1), COL18A1, lanosterol synthase (LSS-PEN), pericentrin (PCNT), and arginine methyltransferase (HRMT1L1). This integrated map provides a useful resource for the mapping and isolation of disease genes and for the construction of a complete transcription map of distal 21q as well as for large-scale sequencing efforts.

Chromosome Mapping↗

Ligands of the histamine H3-receptor: new potent antagonists of the 2-thioimidazole type.

An overview of H3-receptor ligands is presented, with particular attention to antagonists. The protein binding of the classical H3-receptor antagonist thioperamide and its effect on in vivo distribution are discussed. A series of H3-receptor antagonists characterised by the presence of an imidazole ring, a spacer (ethylthio-, ethylamino-, propylthio- or propylamino-chain), a second heterocycle nucleus and a lipophilic group is described. Their H3-receptor antagonist potency has been measured on electrically stimulated guinea-pig intestine, and their affinity for central H3-receptor has been determined by competitive inhibition of [3H]N alpha-methylhistamine binding to rat cortex. Biphasic inhibition curves have been observed in some cases. Compounds endowed with interesting activity belong mostly to the class of 2-[[2-[4(5)-imidazolyl]ethyl]thio]imidazole, having a phenyl or a cyclohexyl group.

Animals↗

QSAR study on H3-receptor affinity of benzothiazole derivatives of thioperamide.

Starting from the structure of thioperamide, a known H3-antagonist, a new series of compounds with a benzothiazole nucleus instead of the cyclohexylcarbothioamide moiety was synthesized. Various substituents, selected by experimental design, were introduced in position 6 of the benzothiazole nucleus, in order to change its physico-chemical characteristics. The lipophilicity of the synthesized compounds was measured by means of RP-HPLC, and their H3-receptor affinity was evaluated by competitive binding assays on rat cortex synaptosomes, with the labelled ligand N alpha-[3H]methylhistamine. A QSAR analysis was performed on the experimental data, using also substituent constants taken from the literature. The newly synthesized compounds showed lower H3-affinities than thioperamide; quantitative structure-activity relationships, described by models obtained with PLS and MRA techniques, were observed among benzothiazole derivatives. According to these relationships, any attempt to improve the potency of these compounds should involve the substitution of the benzothiazole moiety with less bulky and/or more flexible structures, which should also be less lipophilic and allow better electronic interactions with the binding site. 1-(Benzothiazol-2-yl)-4-[(1H)-imidazol-4-yl]piperidine represents a limit structure for H3-activity, since it seems impossible to improve its affinity by means of substitution in the studied position of the benzothiazole nucleus, as shown by predictions performed by a PLS model.

Animals↗

Anomalous responses to histamine stimulation of guinea-pig oesophageal muscularis mucosae.

The incomplete tachyphylaxis of the contractile response to the H1-stimulants observed on guinea-pig oesophageal muscularis mucosae seems to be H2- and H3-antagonist as well as atropine- and tetrodotoxin-resistant. Lidocaine and eserine partially prevented this process probably by a mechanism independent of their main activity. The dualistic antagonism exerted by mepyramine and methysergide on reproducible histamine responses could be explained by a kinetic condition of "hemi-equilibrium state" together with changes of drug-receptor interaction and by non-specific properties of methysergide. On the whole, the present data indicate that the role of histamine in this tissue has still to be defined.

Animals↗

Rotational disorders in intramedullary fixation of the lower limbs.

The routine employment of intramedullary fixation in fractures of the femur and tibia has led the authors to thoroughly evaluate malunions. With the aid of CT scan, precise multilevel quantification of residual rotational deformity was possible by comparison with the contralateral limb after fracture healing. The results of this study confirm the effectiveness of the method, filling an interpretative gap in the literature.

Adolescent↗

Influence of urea-equivalent groups in position 5 of 2-amino, 2-(1-aminoethylidenamino) and 2-guanidino thiazole derivatives on H2-receptor antagonist activity in gastric fistula cat.

A series of thiazole derivatives, in which a side-chain with different urea-equivalent groups was introduced in position 5 of the heterocycle, have been tested as inhibitors of dimaprit-induced gastric acid and pepsin secretion in the gastric fistula cat. By comparing the in vivo and the previously reported in vitro activity of these compounds, we can note a very close parallelism not only in the quality of their action but also in the estimates of pA2 values. These data support an interdependence between the molecular substructures and the affinity for the H2-receptor.

Animals↗

H2-receptor antagonist activity of N-methylthiourea, N-cyano-N'-methylguanidine, N-cyanoamidine, N-carbamoylamidine and N-sulfamoylamidine 5-substituted thiazole derivatives on guinea-pig atria.

The H2-antagonist activity of thiazole derivatives, substituted on position 5 with urea-equivalent groups, has been tested on guinea-pig isolated atria stimulated by dimaprit. By comparing the activities of the 2,5-disubstituted thiazole derivatives with those of the corresponding 2,4-disubstituted derivatives it can be seen that the side-chain position is critical to activity and differently influences activity in the various series. The heteroaromatic ring atom sequence N-C-S-C-side chain is always associated with a low antagonist activity.

Animals↗

[Thiazolylalkylamines: synthesis of analogs of imidazolylethylamines and their effect on gastric secretion].

As a part of a study on H2-agonists, the preparations and properties are reported for a representative group of 2-aminothiazolethylamine derivatives which contain the gastric secretion stimulating S-aminoalkylisothiourea moiety. The test compounds were obtained by known methods or from 2-(2-amino-5-thiazolyl)ethyl chloride and were tested for their possible histamine-like activities on different biological substrates. From the biological results it appears that the behaviour of the substances is rather complex, but the following general observations can be pointed out: the contracturant properties, sometimes quite marked, do not derive from direct H1-specific activities; the effects, particularly evident in stimulating in vitro or in vivo gastric secretion, in relaxing gall-bladder smooth muscle, on auriculae and/or on blood pressure, are not competitively antagonized by cimetidine; none of the tested compounds proved to be an antagonist of histamine H2-receptors, while one of them is found to inhibit competitively the H1-receptors. On the basis of structure-activity relationships it can be excluded that the iuxta-nuclear NH2 group of 2-aminothiazolethylamines reacts, in some way, with the H2-receptors, since, in this case, the 2-aminothiazole group is not a pharmacophore like the 2-aminoimidazole or isothiurea group. Consequently the hypotheses, that the flexibility of the molecule is a fundamental requirement for the H2-stimulating properties of S-(3-dimethylaminopropyl)isothiurea and that the different activities of 2-aminohistamine, in comparison with those of 2-methylhistamine, are due to the existence of a hydrophilic area suitable for the allocation of the iuxta-nuclear NH2 group in the H2-receptor, are strengthened.

Amines↗

[The value of xeroradiographic patterns in the diagnosis of breast diseases (author's transl)].

The purpose of this study was to establish the value of xeroradiographic patterns and their applicability in the automatic diagnosis of breast diseases. Such an evaluation is based on the comparison with the histologic examination, irrespective of the overall diagnostic judgement previously formulated. From an analysis of the material examined it was possible to ascertain the distribution frequency, the sensitivity, the specificity, the discriminating capacity, and finally the weight of each radiologic sign considered. There are xeroradiographic signs that are apparent almost exclusively in the malignant pathology and therefore can be considered as positive indices of the malignancy of the alteration. The specificity of the radiologic signs considered is very high, whereas the same cannot be said for the sensitivity. Moreover, a linear discriminating analysis made it possible to identify those semiologic elements which, with a minor probability of error, would attribute the pathologic process to the class verified histologically, for malignant neoplasms as well as benign tumors and dysplastic processes.

Breast Diseases↗

Biological properties of 3-benzyl-1,2-benzisothiazole compounds.

By reaction of 3-chloro-1,2-benzisothiazole with phenylacetonitrile, 3-benzyl-1,2-benzisothiazole derivatives can be obtained. These compounds seem to mimic the benzylisoquinoline structure so they can exhibit spasmolytic activities. Both antimuscarinic and direct muscle-relaxant properties have been found with N,N-dimethyl-3-phenyl-3-(1,2-benzisothiazol-3-yl) propylamine hydrochloride.

Acetylcholine↗

Diagnostic accuracy of xeromammography.

The analytical study of the case material has allowed a precise evaluation of the distribution by age groups of the different pathologic processes of the breast, of the localization and dimensions of malignant tumors, as well as the diagnostic accuracy for those cases histologically ascertained and those with a follow-up. The diagnostic accuracy and the consequent reliability of the xeroradiographic method for the diagnosis of breast cancer is distinctly superior to that reported in the literature for traditional mammography, whereas for the differential diagnosis between circumscribed dysplastic manifestations and benign tumors xeromammography is not sufficiently reliable. The authors critically discuss the results and in particular the problem of false positives, which also include diagnostic errors that cannot be avoided in that they directly derive from the pathologic morphology of the disease process (plasma cell mastitis and sclerosing adenosis). As regards the problem of false negatives, they can be reduced within certain limits by resorting to other instrumental investigations. However, there are cases (1% of the malignant neoplasias histologically ascertained) that present a completely negative xeroradiographic finding. There are the limits of the radiologic investigation which cannot in any way be surmounted.

Adolescent↗

[Imidazole H2-antagonists and H2-angonists: effects of 5-alkyl substitution].

The effects of some imidazole derivatives, H2-antagonists and H2-agonists, with different alkyl groups in 5-position (R = Me, Et, i.Pr), were studied comparatively on cat gastric secretion and guinea-pig gastric fundus. The antagonistic and agonistic activities decrease with increase in the substituent inductive effect, and, in particular, it should be noted that the cimetidine ethyl analog (compound V) is a competitive antagonist of H2-histamine receptors. More hypotheses on the H1- and H2-receptor surfaces are proposed.

Alkylation↗

Effects of alkyl analogs of histamine and metiamide on gastric acid secretion.

Histamine and metiamide analogs with alkyl, methyl, ethyl or isopropyl groups on the imidazole ring in position 5, not previously tested on an in vivo preparation, were studied for their effects on gastric acid secretion in cats with gastric fistulas. Our findings confirmed that the methyl group appears to be optimal for an effect on gastric acid secretion as regards both agonism and antagonism. Ethyl substitution apparently did not change the pharmacological activity of histamine but modified the inhibitory effect of metiamide from competitive to non-competitive kinetics. Isopropyl analogs were inactive on gastric secretion under our experimental conditions.

Animals↗