Discovery, synthesis and biological characterization of a series of N-(1-(1,1-dioxidotetrahydrothiophen-3-yl)-3-methyl-1H-pyrazol-5-yl)acetamide ethers as novel GIRK1/2 potassium channel activators

2021 ◽  
Author(s):  
Swagat Sharma ◽  
Lauren Lesiak ◽  
Christopher D. Aretz ◽  
Yu Du ◽  
Sushil Kumar ◽  
...  
Keyword(s):  
Potassium Channel ◽  
Biological Characterization ◽  
Sulfone Group ◽  
Potassium Channel Activators

We report the synthesis, biological characterization, and in vitro PK properties of a new ether series of compounds that incorporate the sulfone group while maintaining potency and stability. 11a was identified as a new GIRK1/2 activator with suitable properties.

scholarly journals Physical and Biological Characterization of Ferromagnetic Fiber Networks: Effect of Fibrin Deposition on Short-Term In Vitro Responses of Human Osteoblasts

2015 ◽  
Vol 21 (3-4) ◽  
pp. 463-474 ◽  
Author(s):  
Rose L. Spear ◽  
Brajith Srigengan ◽  
Suresh Neelakantan ◽  
Wolfram Bosbach ◽  
Roger A. Brooks ◽  
...  
Keyword(s):  
Biological Characterization ◽  
Fibrin Deposition ◽  
Short Term ◽  
Human Osteoblasts ◽  
Fiber Networks

scholarly journals In Vitro Biological Characterization of DCUN1D5 in DNA Damage Response

2012 ◽  
Vol 13 (8) ◽  
pp. 4157-4162 ◽  
Author(s):  
Wei Guo ◽  
Guo-Jun Li ◽  
Hong-Bo Xu ◽  
Jie-Shi Xie ◽  
Tai-Ping Shi ◽  
...  
Keyword(s):  
Dna Damage ◽  
Dna Damage Response ◽  
Biological Characterization ◽  
Damage Response

Preparation and Biological Evaluation of Si-Substituted HA Ceramics with Controlled Composition

2007 ◽  
Vol 361-363 ◽  
pp. 1059-1062
Author(s):  
Mickael Palard ◽  
J. Combes ◽  
Eric Champion ◽  
Didier Bernache-Assollant
Keyword(s):  
Thermal Treatment ◽  
Biological Evaluation ◽  
Precipitation Process ◽  
Biological Characterization ◽  
Hydroxyapatite Ceramics

This work aimed at preparing dense and monophasic silicated hydroxyapatite ceramics over the range 0 ≤ x ≤ 1.0 mol of silicon. The synthesis of the powder via an aqueous precipitation process followed by an adapted thermal treatment showed that it was possible to obtain dense single-phased apatite ceramics containing up to 0.6 mol of silicon. The in vitro biological characterization of these materials was performed.

Biological characterization of charge isomers of human growth hormone

1988 ◽  
Vol 118 (1) ◽  
pp. 14-21 ◽  
Author(s):  
A. Skottner ◽  
A. Forsman ◽  
B. Skoog ◽  
J. L. Kostyo ◽  
C. M. Cameron ◽  
...  
Keyword(s):  
Biological Activity ◽  
Biological Activities ◽  
Human Growth ◽  
Proteolytic Processing ◽  
Biological Characterization ◽  
Growth Promoting ◽  
Rat Adipose Tissue ◽  
Insulin Like Activity

Abstract. Since deamidation of the human GH molecule may alter the manner and extent to which the hormone is cleaved by proteases, and since it has been repeatedly suggested that proteolytic processing is required for the expression of certain of the activities of GH, the present study was conducted to determine whether the biological activity profiles of more acidic forms of human GH are altered. Three charge isomers, GH-b, GH-c and GH-d, representing primarily deamidated forms, were isolated from a native human GH preparation (Crescormon®) in amounts adequate for characterization of their biological activities. All three were essentially equipotent in a radioimmunoassay for human GH. When assessed for growth-promoting activity in the hypophysectomized rat, the isomers were again equipotent with each other and with the GH preparation from which they were derived. The charge isomers also had significant in vitro insulin-like activity on isolated rat adipose tissue and diabetogenic activity in the ob/ob mouse. Thus, the biological activity profiles of these charge isomers of human GH do not differ greatly from one another.

In vitro biological characterization of macroporous 3D Bonelike® structures prepared through a 3D machining technique

2009 ◽  
Vol 29 (3) ◽  
pp. 930-935 ◽  
Author(s):  
M.S. Laranjeira ◽  
A.G. Dias ◽  
J.D. Santos ◽  
M.H. Fernandes
Keyword(s):  
Biological Characterization

scholarly journals Endobrevin, a Novel Synaptobrevin/VAMP-Like Protein Preferentially Associated with the Early Endosome

1998 ◽  
Vol 9 (6) ◽  
pp. 1549-1563 ◽  
Author(s):  
Siew Heng Wong ◽  
Tao Zhang ◽  
Yue Xu ◽  
V. Nathan Subramaniam ◽  
Gareth Griffiths ◽  
...  
Keyword(s):  
Synaptic Vesicles ◽  
Early Endosome ◽  
Biological Characterization ◽  
Binding Assays ◽  
Indirect Immunofluorescence Microscopy ◽  
General Importance ◽  
Vitro Binding ◽  
Main Components

Synaptobrevins/vesicle-associated membrane proteins (VAMPs) together with syntaxins and a synaptosome-associated protein of 25 kDa (SNAP-25) are the main components of a protein complex involved in the docking and/or fusion of synaptic vesicles with the presynaptic membrane. We report here the molecular, biochemical, and cell biological characterization of a novel member of the synaptobrevin/VAMP family. The amino acid sequence of endobrevin has 32, 33, and 31% identity to those of synaptobrevin/VAMP-1, synaptobrevin/VAMP-2, and cellubrevin, respectively. Membrane fractionation studies demonstrate that endobrevin is enriched in membrane fractions that are also enriched in the asialoglycoprotein receptor. Indirect immunofluorescence microscopy establishes that endobrevin is primarily associated with the perinuclear vesicular structures of the early endocytic compartment. The preferential association of endobrevin with the early endosome was further established by electron microscopy (EM) immunogold labeling. In vitro binding assays show that endobrevin interacts with immobilized recombinant α-SNAP fused to glutathioneS-transferase (GST). Our results highlight the general importance of members of the synaptobrevin/VAMP protein family in membrane traffic and provide new avenues for future functional and mechanistic studies of this protein as well as the endocytotic pathway.

In vitro and in vivo biological characterization of the anti-proliferative potential of a cyclic trinuclear organotin(iv) complex

2016 ◽  
Vol 12 (3) ◽  
pp. 1015-1023 ◽  
Author(s):  
Marta Martins ◽  
Pedro V. Baptista ◽  
Ana Soraia Mendo ◽  
Claudia Correia ◽  
Paula Videira ◽  
...  
Keyword(s):  
Tumor Cells ◽  
Proliferative Potential ◽  
Biological Characterization ◽  
Growth Of Tumor

Identification of novel molecules that can selectively inhibit the growth of tumor cells, is of utmost importance.

scholarly journals Phylogenetic Analysis of Nucleotide Sequences from the ITS Region and Biological Characterization of Nematophagous Fungi from Morelos, Mexico

2016 ◽  
Vol 2016 ◽  
pp. 1-13
Author(s):  
Gloria Sarahí Castañeda-Ramírez ◽  
Pedro Mendoza-de-Gives ◽  
Liliana Aguilar-Marcelino ◽  
María Eugenia López-Arellano ◽  
Jesús Hernández-Romano
Keyword(s):  
Biological Function ◽  
Its Region ◽  
Nematophagous Fungi ◽  
Biological Characterization ◽  
High Identity ◽  
Predatory Activity ◽  
Infective Larvae ◽  
Morphological Taxonomy

We determined the morphological taxonomy of eighteen nematophagous fungi (NF), as well as their in vitro predatory activity against Haemonchus contortus infective larvae (L3). Fungi were classified into six genera and three species, the most common of which were Monacrosporium eudermatum and Arthrobotrys oligospora. We then sequenced five NF isolates using ITS4 and ITS5 primers. These sequences showed high identity with sequences from the NCBI database (98-99%). In contrast, alignments among the same genera and species demonstrated 83–97% identity. Polymorphisms observed between Arthrobotrys and Monacrosporium appear to be associated with differences in biological function, nonspecific mutations, evolutionary processes, feeding behaviour, predatory activity, and microecosystems.

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