Non-peptide alpha(v)beta(3) antagonists. Part 3: identification of potent RGD mimetics incorporating novel beta-amino acids as aspartic acid replacements.

Potent non-peptidic alpha(v)beta(3) antagonists have been prepared incorporating various beta-amino acids as aspartic acid mimetics. Modification of the beta-alanine 3-substituents alters the potency and physicochemical properties of these receptor antagonists and in some cases provides orally bioavailable alpha(v)beta(3) inhibitors.     

Family resemblance for anthropometric and blood pressure measurements in Black Caribs and Creoles from St. Vincent Island

This paper examines family resemblance for five anthropometric measurements (height, weight, triceps skinfold, upper arm circumference relaxed [UACR] and flexed [UACF] and for systolic and diastolic blood pressure in a group of adult Caribbean islanders of primarily African ancestry. Six hypotheses about family resemblance are tested by using path analysis and likelihood ratios. Significant intergenerational transmission is found only for height and UACR. For weight, UACF, and diastolic blood pressure, non-transmissible sibling resemblance is the primary component of family resemblance, although significant marital resemblance exists for diastolic blood pressure. Triceps skinfold and systolic blood pressure show no evidence of any family resemblance. Although results for highly heritable traits such as height are comparable to reports from other populations, measurements with a large contribution from common family environment or residual environmental effects, such as triceps skinfold or blood pressure, have much lower family resemblance in this population than in other populations. We hypothesize that this difference is due to the fact that adult children and their parents do not share a common household in this culture and to the presence of major nonfamilial environmental factors contributing to obesity and hypertension in this population.     

Human fibroblast stromelysin catalytic domain: expression, purification, and characterization of a C-terminally truncated form.

Stromelysin-1 is a member of a tissue metalloproteinase family whose members are all capable of degrading extracellular matrix components. A truncated form of human fibroblast prostromelysin 1 lacking the C-terminal, hemopexin-like domain has been expressed in Escherichia coli and purified to homogeneity. Treatment of this short form of prostromelysin with (aminophenyl)mercuric acetate resulted in activation and loss of the propeptide in a manner identical with the wild-type, full-length protein. Kinetic comparisons using Nle11-substance P as a substrate showed that the wild-type stromelysin and the truncated form of the enzyme had similar kcat and Km values. Likewise, both enzymes displayed similar Ki values for a hydroxamate-containing peptide inhibitor. Taken together, these results indicate that the C-terminal portion of stromelysin is not required for proper folding of the catalytic domain, maintenance of the enzyme in a latent form, activation with an organomercurial, cleavage of a peptide substrate, or interaction with an inhibitor. Moreover, the active short form of stromelysin displayed a reduction in the C-terminal heterogeneity, a characteristic degradation of the full-length stromelysin, and thereby provides a more suitable protein for future structural studies.     

Stable isotope analyses of collagen in fish scales: limitations set by scale architecture

Comparisons between the stable isotope composition of carbon in collagen excized from juvenile (freshwater) and adult (marine) portions of scales from Atlantic salmon Salmo salar demonstrated that c. 75% of carbon analysed in the 'juvenile' portion of the scale derives from later formed collagen. Scale collagen analyses were effectively restricted to the last season of growth.     

Activities in Crude Porcine Pancreatic Lipase: Enantioselectivity in Hydrolysis of the Diacetate of 2-Phenylpropane-1,3-Diol

The hydrolysis of a prochiral diacetate by porcine pancreatic lipase is catalysed by the purified enzyme, not by an enzyme present in the crude enzyme but absent from the purified enzyme, as previously reported.