scholarly journals Design, Synthesis, and Characterization of Small-Molecule Reagents That Cooperatively Provide Dual Readouts for Triaging and, When Necessary, Quantifying Point-of-Need Enzyme Assays

2015 ◽  
Vol 80 (21) ◽  
pp. 10437-10445 ◽  
Author(s):  
Adam D. Brooks ◽  
Hemakesh Mohapatra ◽  
Scott T. Phillips
Keyword(s):  
Small Molecule ◽  
Synthesis And Characterization ◽  
Enzyme Assays ◽  
Design Synthesis

scholarly journals Bifunctional Small Molecule Ligands of K-Ras Induce Its Association with Immunophilin Proteins

2019 ◽  
Author(s):  
Ziyang Zhang ◽  
Kevan M. Shokat
Keyword(s):  
Small Molecule ◽  
Therapeutic Strategy ◽  
Cyclophilin A ◽  
Synthesis And Characterization ◽  
Design Synthesis ◽  
Biochemical Assays ◽  
Intracellular Proteins ◽  
Small Molecule Ligands ◽  
Ligand Scaffolds

AbstractHere we report the design, synthesis and characterization of bifunctional chemical ligands that induce the association of Ras with ubiquitously expressed immunophilin proteins such as FKBP12 and cyclophilin A. We show this approach is applicable to two distinct Ras ligand scaffolds, and that both the identity of the immunophilin ligand and the linker chemistry affect compound efficacy in biochemical and cellular contexts. These ligands bind to Ras in an immunophilin-dependent fashion and mediate the formation of tripartite complexes of Ras, immunophilin and the ligand. The recruitment of cyclophilin A to GTP-bound Ras blocks its interaction with B-Raf in biochemical assays. Our study demonstrates the feasibility of ligand-induced association of Ras with intracellular proteins and suggests it as a promising therapeutic strategy for Rasdriven cancers.

scholarly journals Structure-Based Design, Synthesis, and Characterization of Dual Hotspot Small-Molecule HIV-1 Entry Inhibitors

2012 ◽  
Vol 55 (9) ◽  
pp. 4382-4396 ◽  
Author(s):  
Judith M. LaLonde ◽  
Young Do Kwon ◽  
David M. Jones ◽  
Alexander W. Sun ◽  
Joel R. Courter ◽  
...  
Keyword(s):  
Small Molecule ◽  
Synthesis And Characterization ◽  
Design Synthesis ◽  
Entry Inhibitors ◽  
Hiv 1

scholarly journals Design of an n-type low glass transition temperature radical polymer

2021 ◽  
Author(s):  
Teng Chi ◽  
Siddhartha Akkiraju ◽  
Zihao Liang ◽  
Ying Tan ◽  
Ho Joong Kim ◽  
...  
Keyword(s):  
Glass Transition ◽  
Transition Temperature ◽  
Glass Transition Temperature ◽  
Synthesis And Characterization ◽  
Design Synthesis

We document the design, synthesis, and characterization of the first low glass transition temperature, n-type (i.e., preferentially-reduced) radical polymer.

Design, Synthesis, and Characterization of Novel CXCR4 Antagonists Featuring Cyclic Amines

ChemMedChem ◽  
2020 ◽  
Vol 15 (13) ◽  
pp. 1150-1162
Author(s):  
Yu Lin ◽  
Zhanhui Li ◽  
Haikuo Ma ◽  
Yujie Wang ◽  
Xu Wang ◽  
...  
Keyword(s):  
Synthesis And Characterization ◽  
Design Synthesis ◽  
Cyclic Amines ◽  
Cxcr4 Antagonists

HYDRAmers: design, synthesis and characterization of different generation novel Hydra-like dendrons based on multifunctionalized adamantane

2011 ◽  
Vol 47 (31) ◽  
pp. 8955 ◽  
Author(s):  
Giuseppe Lamanna ◽  
Julie Russier ◽  
Cécilia Ménard-Moyon ◽  
Alberto Bianco
Keyword(s):  
Synthesis And Characterization ◽  
Design Synthesis

scholarly journals Design, synthesis and characterization of peptidomimetic conjugate of BODIPY targeting HER2 protein extracellular domain

2013 ◽  
Vol 65 ◽  
pp. 60-69 ◽  
Author(s):  
Sashikanth Banappagari ◽  
Alecia McCall ◽  
Krystal Fontenot ◽  
M. Graca H. Vicente ◽  
Amit Gujar ◽  
...  
Keyword(s):  
Extracellular Domain ◽  
Synthesis And Characterization ◽  
Design Synthesis ◽  
Her2 Protein

DESIGN, SYNTHESIS, AND CHARACTERIZATION OF THE SOME NOVEL 2‐AMINO-PYRIDINE‐3‐ CARBONITRILE AND 2‐AMINO-4H-PYRAN‐3‐CARBONITRILE DERIVATIVES AGAINST ANTIMICROBIAL ACTIVITY AND ANTIOXIDANT ACTIVITY

2020 ◽  
pp. 125-134
Author(s):  
SURENDRA BABU LAGU ◽  
RAJENDRA PRASAD YEJELLA
Keyword(s):  
Antimicrobial Activity ◽  
Antioxidant Activity ◽  
Antimicrobial Activities ◽  
Docking Studies ◽  
Synthesis And Characterization ◽  
Zone Of Inhibition ◽  
Design Synthesis ◽  
Instrumental Methods ◽  
Objective Investigation

Objective: Investigation, the series of newer 2‐amino-pyridine‐3‐carbonitrile and 2‐amino-4H-pyran‐3‐carbonitrile derivative were synthesized and evaluated antimicrobial activities and antioxidant activity. Methods: Novel synthesized chalcones were further condensation to give 2-amino-3-cyanopyridine and 2-amino-3-cyanopyrans in the presence of malononitrile, pyridine, and ammonia acetate. The product is characterized by conventional and instrumental methods. Pyridine and 4-H-Pyran and their analogs occupy prime position due to their diverse applications. Results: The compounds A3C and B3C exhibited marked zone of inhibition with 30.02±0.02 mm and 29.06±0.01 mm, respectively. Docking studies suggested possible interactions with dihydrofolic reductase 4 with 9.15 and −9.67 kcal/mol, respectively. The IC50 30.28±0.01 exhibited A3C by 2,2-diphenylpicrylhydrazyl methods which is better among the series. The 2-amino-3-cyanopyridine derivatives were found good activity than 2-amino-3-cyanopyrane derivative. Among all synthesized compounds few having potent activity and some are near to the standard. Conclusion: Antimicrobial activity and antioxidant of the newly synthesized pyrans and pyridines derivatives will definitely inspire future researchers for the preparation of new analogs.

scholarly journals Design, Synthesis, and Characterization of a Fluorescence Polarization Pan-BET Bromodomain Probe

2018 ◽  
Vol 9 (12) ◽  
pp. 1223-1229 ◽  
Author(s):  
Carolyn N. Paulson ◽  
Xianghong Guan ◽  
Alex M. Ayoub ◽  
Alice Chan ◽  
Rezaul M. Karim ◽  
...  
Keyword(s):  
Fluorescence Polarization ◽  
Synthesis And Characterization ◽  
Design Synthesis
Sign in / Sign up

Export Citation Format

Share Document