ChemInform Abstract: Non-Classical Formation of Peptide Bonds by Oxaziridine-Amide Isomerization: Model Studies and a Formal Synthesis of Aspartame.

ChemInform ◽  
2010 ◽  
Vol 23 (21) ◽  
pp. no-no
Author(s):  
J.-C. PLAQUEVENT ◽  
D. BENARD ◽  
B. GOUMENT
1988 ◽  
Vol 66 (11) ◽  
pp. 2903-2913 ◽  
Author(s):  
Michael E. Moir ◽  
Robert J. Crawford

The processes of epimerization of individual peptide units in proteins and the concurrent cleavage of peptide bonds are modelled by heating some tetrapeptide and tetrapeptide derivatives to 148.5 °C in pH 6.8 phosphate buffer. An excess of D-proline was observed during the heating of L-prolyl-L-leucylglycylglycine. The D/L ratio of proline attains a maximum value of 2.1 after 90 minutes. The excess D-proline is attributed to the formation of a 2.3:1 mixture of diketopiperazines cyco-(D-prolyl-L-leucyl) and cyclo-(L-prolyl-L-leucyl). These two species account for most of the leucine and proline in the final mixture after the tetrapeptide is no longer detectable. Only small amounts of prolylleucine can be detected after 50 hours. It is suggested that the above tetrapeptide undergoes internal aminolysis. Leucine in the tetrapeptide glycyl-L-leucylglycylglycine racemizes three times faster than in L-prolyl-L-leucylglycylglycine. This demonstrates that an amino acid residue in a peptide chain does have an effect upon the rate of epimerization of a neighbouring peptide residue. A discussion of the geochemical implications of the results is included.


1995 ◽  
Vol 74 (03) ◽  
pp. 868-873 ◽  
Author(s):  
Silvana Arrighi ◽  
Roberta Rossi ◽  
Maria Giuseppina Borri ◽  
Vladimir Lesnikov ◽  
Marina Lesnikov ◽  
...  

SummaryTo improve the safety of plasma derived factor VIII (FVIII) concentrate, we introduced a final super heat treatment (100° C for 30 min) as additional virus inactivation step applied to a lyophilized, highly purified FVIII concentrate (100 IU/mg of proteins) already virus inactivated using the solvent/detergent (SID) method during the manufacturing process.The efficiency of the super heat treatment was demonstrated in inactivating two non-lipid enveloped viruses (Hepatitis A virus and Poliovirus 1). The loss of FVIII procoagulant activity during the super heat treatment was of about 15%, estimated both by clotting and chromogenic assays. No substantial changes were observed in physical, biochemical and immunological characteristics of the heat treated FVIII concentrate in comparison with those of the FVIII before heat treatment.


1966 ◽  
Vol 16 (03/04) ◽  
pp. 526-540 ◽  
Author(s):  
E. A Beck ◽  
D. P Jackson

SummaryThe effects of trypsin and plasmin on the functional and physicochemical properties of purified human fibrinogen were observed at various stages of proteolysis. Concentrations of plasmin and trypsin that produced fibrinogenolysis at comparable rates as measured in a pH stat produced, at similar rates, loss of precipitability of fibrinogen by heat and ammonium sulphate and alterations in electrophoretic mobility on starch gel. Trypsin produced a more rapid loss of clottability of fibrinogen and a more rapid appearance of inhibitors of the thrombin-fibrinogen clotting system than did plasmin. Consistent differences were noted between the effects of trypsin and plasmin on the immunoelectrophoretic properties of fibrinogen during the early stages of proteolysis.These results are consistent with the hypothesis that trypsin initially reacts with the same peptide bonds of fibrinogen that are split by thrombin, but these same bonds do not appear to be split initially by plasmin. Measurement of the various functional and physico-chemical changes produced by the action of trypsin and plasmin on fibrinogen can be used to recognize various stages of proteolysis.


2014 ◽  
Vol 59 (4) ◽  
pp. 971-986 ◽  
Author(s):  
Krzysztof Tajduś

Abstract The paper presents the analysis of the phenomenon of horizontal displacement of surface induced by underground mining exploitation. In the initial part, the basic theories describing horizontal displacement are discussed, followed by three illustrative examples of underground exploitation in varied mining conditions. It is argued that center of gravity (COG) method presented in the paper, hypothesis of Awierszyn and model studies carried out in Strata Mechanics Research Institute of the Polish Academy of Sciences indicate the proportionality between vectors of horizontal displacement and the vector of surface slope. The differences practically relate to the value of proportionality coefficient B, whose estimated values in currently realized design projects for mining industry range between 0.23r to 0.42r for deep exploitations, whereas in the present article the values of 0.33r and 0.47r were obtained for two instances of shallow exploitation. Furthermore, observations on changes of horizontal displacement vectors with face advancement indicated the possibility of existence of COG zones above the mined-out field, which proved the conclusions of hitherto carried out research studies (Tajduś 2013).


2020 ◽  
Author(s):  
Rui Guo ◽  
Xiaotian Qi ◽  
Hengye Xiang ◽  
Paul Geaneoates ◽  
Ruihan Wang ◽  
...  

Vinyl fluorides play an important role in drug development as they serve as bioisosteres for peptide bonds and are found in a range of biologically active molecules. The discovery of safe, general and practical procedures to prepare vinyl fluorides remains an important goal and challenge for synthetic chemistry. Here we introduce an inexpensive and easily-handled reagent and report simple, scalable, and metal-free protocols for the regioselective and stereodivergent hydrofluorination of alkynes to access both the E and Z isomers of vinyl fluorides. These conditions were suitable for a diverse collection of alkynes, including several highly-functionalized pharmaceutical derivatives. Mechanistic and DFT studies support C–F bond formation through a vinyl cation intermediate, with the (E)- and (Z)-hydrofluorination products forming under kinetic and thermodynamic control, respectively.<br>


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