Chemical Synthesis of an Erythropoietin Glycoform Having a Triantennary N-Glycan: Significant Change of Biological Activity of Glycoprotein by Addition of a Small Molecular Weight Trisaccharide

2020 ◽  
Vol 142 (49) ◽  
pp. 20671-20679
Author(s):  
Yuta Maki ◽  
Ryo Okamoto ◽  
Masayuki Izumi ◽  
Yasuhiro Kajihara
Keyword(s):  
Molecular Weight ◽  
Biological Activity ◽  
Chemical Synthesis ◽  
Small Molecular Weight ◽  
Significant Change

The biological assay of human somatomedin A: improvement by small molecular weight natural molecules

1984 ◽  
Vol 106 (1) ◽  
pp. 43-51 ◽  
Author(s):  
Marie-Hélène Heulin ◽  
Michèle Artur ◽  
Colette Geschier ◽  
Jean Straczek ◽  
Guy Vescovi ◽  
...  
Keyword(s):  
Molecular Weight ◽  
Biological Activity ◽  
Chick Embryo ◽  
Incubation Medium ◽  
Normal Serum ◽  
Optimal Concentration ◽  
Biological Assay ◽  
Small Molecular Weight ◽  
Proper Action

Abstract. Somatomedin activity is often measured by 35SO4 uptake in pelvic chick embryo cartilage. This assay gives good results when the somatomedin activity is measured in serum, but often gives uninterpretable results for purified somatomedin. An ultrafiltrate (UF 1000) obtained from human normal serum, added to the incubation medium allows measurement of biological somatomedin activity even when somatomedin is highly purified. UF 1000 contains some compounds of molecular weight lower than 1000 daltons. UF 1000 acts either when used simultaneously with somatomedin or in pre-incubation with cartilage before testing biological activity. So, we chose to use it in pre-incubation (1 h) at the optimal concentration of 10% (v/v), the standard curves being realized with normal serum retentates. In these conditions, the proper action of UF 1000 does not interfere with calculation of somatomedin activity. This method has enabled us to show that a diminution of serum somatomedin activity can be linked either to an anomaly of UF 1000 or to a somatomedin deficiency.

Molecular Docking, Synthesis and anti-HIV-1 Protease Activity of Novel Chalcones

2020 ◽  
Vol 26 (8) ◽  
pp. 802-814 ◽  
Author(s):  
Nemanja Turkovic ◽  
Branka Ivkovic ◽  
Jelena Kotur-Stevuljevic ◽  
Milica Tasic ◽  
Bojan Marković ◽  
...  
Keyword(s):  
Molecular Weight ◽  
Molecular Docking ◽  
Chemical Synthesis ◽  
Protease Activity ◽  
Molecular Mechanisms ◽  
Replication Cycle ◽  
Low Molecular Weight ◽  
Chalcone Derivatives ◽  
Anti Hiv ◽  
Hiv 1

Background: Since the beginning of the HIV/AIDS epidemic, 75 million people have been infected with the HIV and about 32 million people have died of AIDS. Investigation of the molecular mechanisms critical to the HIV replication cycle led to the identification of potential drug targets for AIDS therapy. One of the most important discoveries is HIV-1 protease, an enzyme that plays an essential role in the replication cycle of HIV. Objective: The aim of the present study is to synthesize and investigate anti-HIV-1 protease activity of some chalcone derivatives with the hope of discovering new lead structure devoid drug resistance. Methods: 20 structurally similar chalcone derivatives were synthesized and their physico-chemical characterization was performed. Binding of chalcones to HIV-1 protease was investigated by fluorimetric assay. Molecular docking studies were conducted to understand the interactions. Results: The obtained results revealed that all compounds showed anti-HIV-1 protease activity. Compound C1 showed the highest inhibitory activity with an IC50 value of 0.001 μM, which is comparable with commercial product Darunavir. Conclusion: It is difficult to provide general principles of inhibitor design. Structural properties of the compounds are not the only consideration; ease of chemical synthesis, low molecular weight, bioavailability, and stability are also of crucial importance. Compared to commercial products the main advantage of compound C1 is the ease of chemical synthesis and low molecular weight. Furthermore, compound C1 has a structure that is different to peptidomimetics, which could contribute to its stability and bioavailability.

Synthesis and Biological Activity Study of Tanshinone Derivatives: A Literature and Patent Review

2020 ◽  
Vol 20 (28) ◽  
pp. 2520-2534
Author(s):  
He Huang ◽  
Chuanjun Song ◽  
Junbiao Chang
Keyword(s):  
Biological Activity ◽  
Herbal Medicine ◽  
Chemical Synthesis ◽  
Bioactive Compounds ◽  
Chinese Herbal Medicine ◽  
Salvia Miltiorrhiza ◽  
Salvia Miltiorrhiza Bunge ◽  
Chinese Herbal ◽  
Patent Review

: Tanshinones are a class of bioactive compounds present in the Chinese herbal medicine Danshen (Salvia miltiorrhiza Bunge), containing among others, abietane diterpene quinone scaffolds. Chemical synthesis and biological activity studies of natural and unnatural tanshinone derivatives have been reviewed in this article.

Hemostatically potent small molecular weight serine protease from Maclura spinosa (Roxb. ex Willd.) accelerates healing of subcutaneous dermal wounds in Swiss albino mice

Biologia ◽  
2019 ◽  
Vol 75 (1) ◽  
pp. 139-149
Author(s):  
Venkatesh Bommalapura Kulkarni ◽  
Raghu Ram Achar ◽  
Maheshwari Mahadevappa ◽  
Dinesh Sosalagere Manjegowda ◽  
Priya Babu Shubha ◽  
...  
Keyword(s):  
Molecular Weight ◽  
Serine Protease ◽  
Small Molecular Weight ◽  
Swiss Albino Mice ◽  
Albino Mice

scholarly journals Enantioselective Catalytic C-H Amidations: An Highlight

Catalysts ◽  
2021 ◽  
Vol 11 (4) ◽  
pp. 471
Author(s):  
Eleonora Tosi ◽  
Renata Marcia de Figueiredo ◽  
Jean-Marc Campagne
Keyword(s):  
Biological Activity ◽  
Chemical Synthesis ◽  
Crucial Role ◽  
Medicinal Chemistry ◽  
Life Sciences ◽  
Biological Processes ◽  
Chiral Molecules ◽  
Material Sciences ◽  
Innovative Approaches

The crucial role played by compounds bearing amide functions, not only in biological processes but also in several fields of chemistry, life polymers and material sciences, has brought about many significant discoveries and innovative approaches for their chemical synthesis. Indeed, a plethora of strategies has been developed to reach such moieties. Amides within chiral molecules are often associated with biological activity especially in life sciences and medicinal chemistry. In most of these cases, their synthesis requires extensive rethinking methodologies. In the very last years (2019–2020), enantioselective C-H functionalization has appeared as a straightforward alternative to reach chiral amides. Therein, an overview on these transformations within this timeframe is going to be given.

scholarly journals Cordycepin analogues of 2-5A and its derivatives. Chemical synthesis and biological activity.

1983 ◽  
Vol 258 (3) ◽  
pp. 1671-1677
Author(s):  
H Sawai ◽  
J Imai ◽  
K Lesiak ◽  
M I Johnston ◽  
P F Torrence
Keyword(s):  
Biological Activity ◽  
Chemical Synthesis
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