Enhanced Electrocatalytic Activities of Perovskite Electrocatalysts for the Oxidation of Small Molecules By Active Site Variation

2017 ◽  
Keyword(s):  
Small Molecules ◽  
Active Site ◽  
Site Variation

Tuning the Electrocatalytic Activity of Perovskites through Active Site Variation and Support Interactions

2014 ◽  
Vol 26 (11) ◽  
pp. 3368-3376 ◽  
Author(s):  
William G. Hardin ◽  
J. Tyler Mefford ◽  
Daniel A. Slanac ◽  
Bijal B. Patel ◽  
Xiqing Wang ◽  
...  
Keyword(s):  
Active Site ◽  
Electrocatalytic Activity ◽  
Site Variation

An alternative strategy for inhibiting multidrug-resistant mutants of the dimeric HIV-1 protease by targeting the subunit interface

2007 ◽  
Vol 35 (3) ◽  
pp. 551-554 ◽  
Author(s):  
L. Bannwarth ◽  
M. Reboud-Ravaux
Keyword(s):  
Small Molecules ◽  
Protein Interactions ◽  
Active Site ◽  
Multidrug Resistant ◽  
Cross Resistance ◽  
Mechanism Of Inhibition ◽  
Therapeutic Molecules ◽  
Β Sheet ◽  
Hiv 1

Mutations that occur in response to the HIV-1 protease inhibitors are responsible for the development of multidrug cross-resistance to these antiproteases in AIDS treatment. One alternative to inhibiting the active site of HIV-1 protease is to target the dimer interface of the homodimeric enzyme at the antiparallel β-sheet formed by the interdigitation of the C- and N-ends of each monomer. This region is highly conserved and is responsible for approx. 75% of the dimer-stabilization energy. The strategies that have been used to design small molecules to target the interface antiparallel β-sheet have produced lipopeptides, guanidinium derivatives and peptides (or peptidomimetics) cross-linked with spacers. The mechanism of inhibition was determined using a combination of kinetic and biophysical methods. These dimerization inhibitors proved equally active in vitro against both wild-type and mutated proteases. They are therefore promising alternatives to active-site-directed inhibitors in AIDS therapy. Disruption of protein–protein interactions by small molecules is a new way to obtain potentially therapeutic molecules.

scholarly journals Solving an X-Ray Structure of a Bio-Artificial Neurotransmitter Receptor Designed for the Naked-Eye Recognition of Dopamine

2020 ◽  
Author(s):  
Thibaud Rossel ◽  
Bing Zhang ◽  
Raphael Gobat
Keyword(s):  
Chemical Synthesis ◽  
Small Molecules ◽  
Active Site ◽  
Chemical Sensor ◽  
Selective Detection ◽  
Neurotransmitter Receptor ◽  
X Ray ◽  
Naked Eye ◽  
Coordination Spheres ◽  
Eye Recognition

The literature is constellated with a wide variety of chemosensors against a plethora of analytes. This seminal library is used to inspire chemists to improve them using chemical synthesis. However, their optimization via chemical synthesis is a difficult task which takes time without the guarantee of final success.We show here that combinatorial chemistry,the use of first and second coordination spheres and the displacement of indicators united within a protein cavity offers an easy-to-assemble colorimetric bio-chemical sensor. It consists only of commercial chemicals. This colorimetric sensor is highly modular, cheap and evolvable. Its X-ray structure reveals the composition of its active site. This allows to design it rationally for the recognition of dopamine with the naked eye. Our bio-sensor therefore resembles a biological receptor for the recognition of neurotransmitters. Its immediate high adaptability and ability to be evolved can be useful for the selective detection of a wide variety of analytes going from small molecules to microorganisms. This discovery therefore makes it possible to dream of new biotechnological or new immunotherapeutic applications.<br>

scholarly journals Discovery of Small Molecules that Activate RNA Methylation through Cooperative Binding to the METTL3-14-WTAP Complex Active Site

Cell Reports ◽  
2019 ◽  
Vol 26 (13) ◽  
pp. 3762-3771.e5 ◽  
Author(s):  
Simona Selberg ◽  
Daria Blokhina ◽  
Maria Aatonen ◽  
Pertti Koivisto ◽  
Antti Siltanen ◽  
...  
Keyword(s):  
Small Molecules ◽  
Active Site ◽  
Cooperative Binding ◽  
Rna Methylation

The catalytic mechanism of the hairpin ribozyme

2002 ◽  
Vol 30 (6) ◽  
pp. 1109-1115 ◽  
Author(s):  
M. J. Fedor
Keyword(s):  
Small Molecules ◽  
Active Site ◽  
Catalytic Mechanism ◽  
Structural Features ◽  
Hairpin Ribozyme ◽  
Bivalent Cation ◽  
Activity Loss ◽  
New Perspective ◽  
Catalytic Chemistry ◽  
Hairpin Ribozymes

Evidence that hairpin ribozymes function in the absence of bivalent cation cofactors suggests that active site nucleobases might participate directly in catalytic chemistry. We have adopted an abasic ribozyme rescue strategy to begin to dissect the roles of specific nucleobases in hairpin ribozyme activity. Loss of one active site nucleobase, G8, could be compensated by providing certain nucleobases and nucleobase analogues in solution. Comparison of the biochemical and structural features that are shared among small molecules that mediate rescue provides a new perspective on potential mechanisms of hairpin ribozyme catalysis.

Spectroscopic discernibility of dopants and axial ligands in pyridinic FeN4 environments relevant to single-atom catalysts for the oxygen reduction reaction

2020 ◽  
Author(s):  
Charlotte Gallenkamp ◽  
Ulrike Ingrid Kramm ◽  
Vera Krewald
Keyword(s):  
Oxygen Reduction Reaction ◽  
Small Molecules ◽  
Oxygen Reduction ◽  
Active Site ◽  
Reduction Reaction ◽  
Single Atom ◽  
Axial Ligands

Single-atom catalysts (SACs) activate small molecules, e.g. the oxygen reduction reaction is catalysed by FeNC materials. Because the nature of active site(s) in SACs is unclear, spectroscopic and computational insights...

Progress in targeting RAS with small molecule drugs

2019 ◽  
Vol 476 (2) ◽  
pp. 365-374 ◽  
Author(s):  
Frank McCormick
Keyword(s):  
Clinical Trials ◽  
Drug Discovery ◽  
Small Molecules ◽  
Active Site ◽  
Biochemical Properties ◽  
Ras Proteins ◽  
Oncogenic Ras ◽  
Small Molecule Drugs ◽  
Related Proteins ◽  
Effector Binding

Abstract RAS proteins have traditionally been deemed undruggable, as they do not possess an active site to which small molecules could bind but small molecules that target one form of oncogenic RAS, KRAS G12C, are already in preclinical and clinical trials, and several other compounds that bind to different RAS proteins at distinct sites are in earlier stage evaluation. KRAS is the major clinical target, as it is by far the most significant form of RAS in terms of cancer incidence. Unfortunately, KRAS exists in two isoforms, each with unique biochemical properties. This complicates efforts to target KRAS specifically. KRAS is also a member of a family of closely related proteins, which share similar effector-binding regions and G-domains, further increasing the challenge of specificity. Nevertheless, progress is being made, driven by new drug discovery technologies and creative science.

scholarly journals Enzyvitands: evolvable biosynthetic and colorimetric chalices

2020 ◽  
Author(s):  
Thibaud Rossel ◽  
Bing Zhang ◽  
Raphael Gobat
Keyword(s):  
Chemical Synthesis ◽  
Small Molecules ◽  
Active Site ◽  
Chemical Sensor ◽  
Colorimetric Sensor ◽  
Selective Detection ◽  
X Ray ◽  
Naked Eye ◽  
Coordination Spheres

The literature is constellated with a wide variety of chemosensors against a plethora of analytes. This seminal library is used to inspire chemists to improve them using chemical synthesis. However, their optimization via chemical synthesis is a difficult task which takes time without the guarantee of final success.We show here that combinatorial chemistry,the use of first and second coordination spheres and the displacement of indicators united within a protein cavity offers an easy-to-assemble colorimetric bio-chemical sensor. It consists only of commercial chemicals. This colorimetric sensor is highly modular, cheap and evolvable. Its X-ray structure reveals the composition of its active site. This allows to design it rationally for the recognition of dopamine with the naked eye. Our bio-sensor therefore resembles a biological receptor for the recognition of neurotransmitters. Its immediate high adaptability and ability to be evolved can be useful for the selective detection of a wide variety of analytes going from small molecules to microorganisms. This discovery therefore makes it possible to dream of new biotechnological or new immunotherapeutic applications.<br>

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