PubMed Health⌕ Search

Biomedical subjects

M Sobocińska

Publications and source records attributed to M Sobocińska.

4 recordsLinked to original sources

Analogues of arginine vasopressin modified in position 2 or 3 with naphthylalanine: selective antagonists of oxytocin in-vitro.

In this study we describe the synthesis and some pharmacological properties of six new analogues of arginine vasopressin (AVP). Five of the peptides were substituted in position 2 with L-1-naphthylalanine (L-1-Nal) or D-1-naphthylalanine (D-1-Nal); one had D-1-Nal in position 3. All analogues were tested in bioassays for pressor and antidiuretic activity. We also tested the uterotonic activity of the peptides in-vitro. Two of the new peptides were moderately potent V1a and oxytocin antagonists. The modifications proposed resulted in a drop or the removal of antidiuretic activity and in the removal of pressor activity, or conversion into moderate antagonists. Two peptides ([Mpa1, (L-1-Nal)2]AVP and [Mpal, (D-1-Nal)2]AVP) which appear not to interact with V1a and V2 receptors were exceptionally selective oxytocin antagonists in vitro. These compounds with selective oxytocin antagonistic activity may be promising candidates for the development of potential tocolytic agents for the prevention of pre-term labour.

Animals↗

Conformational role of His-12 in C-peptide of ribonuclease A.

Possible interactions of the His-12 ring with other side chain and backbone groups of C-peptide lactone (CPL) are discussed. The works published so far are critically reviewed and compared with the latest results obtained by the authors. The main new conclusion is that in the helical conformation of CPL, the Phe-8 and His-12 rings are clustered together. Studies of Phe-8----Ala analogs of CPL and calculations of ring current effects satisfactorily explain the observed environmental shifts of Phe-8 and His-12 protons in NMR spectra of CPL. Interaction between both rings is favorable for alpha-helix formation, but cannot explain an increase in helix stability related with protonation of His-12. This effect arises from favorable interactions of the charged His+-12 ring with the helix backbone.

Histidine↗

Conformational study of two synthetic peptides with sequence analogies to the N-terminal fragment of RNase A.

The conformational properties of two synthetic model peptides, AEAAHAAEAAHMG (PA) and AEAAHAFEAAHMG (PF), have been studied using CD and 1H-NMR methods. In both peptides, glutamate and histidine residues are situated in such a way that two salt bridges between Glu- (i) and His+ (i + 3) can be formed. A salt bridge of this type (Glu- 9-His+ 12) was postulated previously to stabilize, to a great extent, the alpha-helical conformation of isolated N-terminal fragments of RNase A: C-peptide and S-peptide (A. Bierzyński, P.S. Kim and R.L. Baldwin, Proc. Natl. Acad. Sci. U.S.A. 79 (1982) 2470). Although in both PA and PF salt bridges between glutamates and histidines are formed, as demonstrated by the pH-titration curves of the glutamate gamma-proton signals, no traces of helical conformation have been detected. Evidently, the Glu- (i)-His+ (i + 3) salt bridges do not stabilize the alpha-helical conformation. A comparative analysis of PA and PF NMR spectra provides strong evidence that the phenylalanyl ring in PF interacts not only with the hydrophobic methyl groups of almost all alanine residues but also with the histidine rings and the glutamate side chains in their protonated as well as deprotonated forms. Similar interactions, involving Phe 8, can be expected in the N-terminal fragments of RNase and should be taken into account as an important factor determining the conformational properties of C- and S-peptides.

Amino Acid Sequence↗

[Dermatoses in tapestry workers].

From among 810 persons subjected to a medical examination, skin lesions were found in 33.3%. These were mostly: seborrhea (89 cases), occupational naevi (55 cases), dermatomycosis (49 cases), urticaria (21 cases), eczema (12 cases). Other dermatoses were found in 44 workers, however, in a small percentage, not greater than in other non-industrial populations. No occupational dermatoses resulting from exposure to fundamental materials or dyes used in production were found.

Adolescent↗