scholarly journals Development of a hydrolysis-based small-molecule hydrogen selenide (H2Se) donor

2019 ◽  
Vol 10 (46) ◽  
pp. 10723-10727 ◽  
Author(s):  
Turner D. Newton ◽  
Michael D. Pluth
Keyword(s):  
Small Molecule ◽  
Hydrogen Selenide ◽  
Chemical Tools

Hydrolysis-based H2Se donors provide new chemical tools for investigating biological H2Se.

Small-molecule degraders of cyclin-dependent kinase protein: a review

2021 ◽  
Author(s):  
Bin Yu ◽  
Zekun Du ◽  
Yuming Zhang ◽  
Zhiyu Li ◽  
Jinlei Bian
Keyword(s):  
Cell Cycle ◽  
Drug Resistance ◽  
Protein Degradation ◽  
Small Molecule ◽  
Small Molecule Inhibitors ◽  
Structural Characteristics ◽  
Protein A ◽  
Cyclin Dependent Kinase ◽  
Chemical Tools ◽  
Potential Therapeutics

Proteolysis-targeting chimeras are a new modality of chemical tools and potential therapeutics involving the induction of protein degradation. Cyclin-dependent kinase (CDK) protein, which is involved in cycles and transcription cycles, participates in regulation of the cell cycle, transcription and splicing. Proteolysis-targeting chimeras targeting CDKs show several advantages over traditional CDK small-molecule inhibitors in potency, selectivity and drug resistance. In addition, the discovery of molecule glues promotes the development of CDK degraders. Herein, the authors describe the existing CDK degraders and focus on the discussion of the structural characteristics and design of these degraders.

scholarly journals AD Informer Set: Chemical tools to facilitate Alzheimer's disease drug discovery

2021 ◽  
Author(s):  
Frances M Potjewyd ◽  
Joel K Annor-Gyamfi ◽  
Jeffrey Aube ◽  
Shaoyou Chu ◽  
Ivie L Conlon ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Small Molecules ◽  
Small Molecule ◽  
Positive Control ◽  
Target Validation ◽  
Protein Targets ◽  
Novel Targets ◽  
Chemical Tools ◽  
Small Molecule Modulators

Introduction: The portfolio of novel targets to treat Alzheimer's disease (AD) has been enriched by the AMP-AD program. Methods: A cheminformatics-driven effort enabled identification of existing small molecule modulators for many protein targets nominated by AMP-AD and suitable positive control compounds to be included in the set. Results: We have built an annotated set of 171 small molecule modulators, including mostly inhibitors, targeting 98 unique proteins that have been nominated by AMP-AD consortium members as novel targets for AD treatment. These small molecules vary in their quality and should be considered chemical tools that can be used in efforts to validate therapeutic hypotheses, but which would require further optimization. A physical copy of the AD Informer Set can be ordered via the AD Knowledge Portal. Discussion: Small molecule tools that enable target validation are important tools for the translation of novel hypotheses into viable therapeutic strategies for AD.

Developing Chemical Tools to Study Hydrogen Selenide in a Biological Setting

2020 ◽  
Vol 159 ◽  
pp. S30
Author(s):  
Turner Newton ◽  
Arman Garcia ◽  
Sarah Bolton ◽  
Michael Pluth
Keyword(s):  
Hydrogen Selenide ◽  
Chemical Tools

scholarly journals A small molecule that displays marked reactivity toward copper– versus zinc–amyloid-β implicated in Alzheimer's disease

2014 ◽  
Vol 50 (40) ◽  
pp. 5301-5303 ◽  
Author(s):  
Masha G. Savelieff ◽  
Yuzhong Liu ◽  
Russell R. P. Senthamarai ◽  
Kyle J. Korshavn ◽  
Hyuck Jin Lee ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Small Molecule ◽  
Amyloid Β ◽  
Chemical Tools

A small molecule was designed for reactivity toward Cu(ii)–amyloid-β over Zn(ii)–amyloid-β, which will expand on the development of chemical tools to uncover the role of metal–Aβ species in Alzheimer's disease.

Protein-recruiting synthetic molecules targeting the Golgi surface

2020 ◽  
Vol 56 (98) ◽  
pp. 15422-15425
Author(s):  
Shunsuke Sawada ◽  
Akinobu Nakamura ◽  
Tatsuyuki Yoshii ◽  
Keiko Kuwata ◽  
Fubito Nakatsu ◽  
...  
Keyword(s):  
Small Molecule ◽  
Living Cells ◽  
Target Proteins ◽  
Synthetic Molecules ◽  
Chemical Tools ◽  
Small Molecule Ligand

Synthetic molecules consisting of a small-molecule ligand and a tri-N-methylated myristoyl-Gly-Cys lipopeptide serve as chemical tools to rapidly recruit their target proteins from the cytoplasm to the Golgi surface in living cells.

scholarly journals Small molecule screening in zebrafish: an in vivo approach to identifying new chemical tools and drug leads

2010 ◽  
Vol 8 (1) ◽  
pp. 11 ◽  
Author(s):  
Kerrie L Taylor ◽  
Nicola J Grant ◽  
Nicholas D Temperley ◽  
E. Elizabeth Patton
Keyword(s):  
Small Molecule ◽  
Small Molecule Screening ◽  
Chemical Tools ◽  
Drug Leads

Hydrolysis-Based Small-Molecule Hydrogen Selenide (H2Se) Donors for Intracellular H2Se Delivery

2021 ◽  
Author(s):  
Turner D. Newton ◽  
Sarah G. Bolton ◽  
Arman C. Garcia ◽  
Julie E. Chouinard ◽  
Stephen L. Golledge ◽  
...  
Keyword(s):  
Small Molecule ◽  
Hydrogen Selenide
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