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The esterification of 2-chlorotrityl chloride resin with Fmoc-amino acids in the presence of DIEA is studied under various conditions. High esterification yields are obtained using 0.6 equiv. Fmoc-amino acid/mmol resin in DCM or DCE, in 25 min, at room temperature. The reaction proceeds without by product formation even in the case of Fmoc-Asn and Fmoc-Gln.(More)
The reaction between Arg-Gly-Asp (RGD) and Lys-Gly-Asp (KGD) derivatives with 3,4',5-trihydroxy-trans-stilbene (resveratrol) was investigated. Knowing that resveratrol, RGD as well as KGD analogues inhibit human platelet aggregation in vitro, it was tempting for us to examine whether their coupling products present enhanced biological activity. Here, we(More)
A novel, real-time and robust occupancy extraction system is going to be presented in this paper. The main contribution of the paper is to introduce a novel camera calibration algorithm to a multi-space area. The proposed calibration method is accurate, efficient and free of any error propagation among cameras' calibrations, without usage of overlapping(More)
Analogues of [Orn6]-SP6-11 have been synthesized in which the CH2SCH3 group of Met11 is replaced by a COOCH3 or a COOBzl group. These analogues, which were tested for agonist and antagonist activity in three in vitro preparations representative of NK-1, NK-2 and NK-3 receptor types, were full agonists at NK-1 receptors, showed very weak agonist activity at(More)
The in vitro chemosensitivity of three cancer cell lines [HT29 (colon), HeLa (cervical) and T47D (breast)] to eight synthetic tetrapeptides, analogs of AS-I toxin, with phytotoxic effect on a series of plants was studied. Mouse fibroblast L929 cell line was also tested for chemosensitivity to these peptides. All cell lines were especially sensitive to(More)
Factor VIII, a human blood plasma protein, plays an important role during the intrinsic pathway of blood coagulation cascade after its activation by thrombin. The activated form of FVIII acts as cofactor to the serine protease Factor IXa, in the conversion of the zymogen Factor X to the active enzyme Factor Xa. The Ser558–Gln565 region of the A2 subunit of(More)
A series of di- and tripeptides containing aspartic or asparagine as N-terminal or intermediate amino acid were synthesized and tested for their effect on human platelet aggregation in vitro. It was found that only Met-Asp(or Asn)-Phe-NH2 inhibited platelet aggregation induced by collagen, ADP or adrenaline. Asn-Phe-NH2 and to a small extent Asp-Phe-NH2(More)
Novel anticoagulant therapies target specific clotting factors in blood coagulation cascade. Inhibition of the blood coagulation through Factor VIII–Factor IX interaction represents an attractive approach for the treatment and prevention of diseases caused by thrombosis. Our research efforts are continued by the synthesis and biological evaluation of(More)
A series of Leu-(Asp, Asn, Glu, Gln) dipeptides were synthesized and tested for their effect on human platelet aggregation in vitro induced by collagen, ADP, or adrenaline. It was found that only Leu-Asp-NH2 and Leu-Asn-NH2 inhibit rather strongly platelet aggregation, whereas a small inhibition was observed with Leu-Glu-NH2 and Leu-Gln-NH2, respectively.
We have investigated the effects of the substance P C-terminal octapeptide analogues [Pro4, Glu (OBzl)11] SP4-11, [Hyp4, Glu(OBzl)11] SP4-11, [cHyp4, Glu(OBzl)11] SP4-11 and [kPro4, Glu(OBzl)11] SP4-11 on the constitutive and/or lipopolysaccharide (LPS)-induced expression of tumor necrosis factor (TNF-alpha) in both freshly isolated human blood monocytes(More)