scholarly journals Chemical Diversity in a Stingless Bee–Plant Symbiosis

ACS Omega ◽  
2019 ◽  
Vol 4 (12) ◽  
pp. 15208-15214
Author(s):  
Eduardo A. Silva-Junior ◽  
Camila R. Paludo ◽  
Juliano G. Amaral ◽  
Marília E. Gallon ◽  
Leonardo Gobbo-Neto ◽  
...  
Keyword(s):  
Stingless Bee ◽  
Chemical Diversity ◽  
Bee Plant

scholarly journals Lessons from Exploring Chemical Space and Chemical Diversity of Propolis Components

2020 ◽  
Vol 21 (14) ◽  
pp. 4988 ◽  
Author(s):  
Trong D. Tran ◽  
Steven M. Ogbourne ◽  
Peter R. Brooks ◽  
Norberto Sánchez-Cruz ◽  
José L. Medina-Franco ◽  
...  
Keyword(s):  
Honey Bee ◽  
Broad Spectrum ◽  
Chemical Space ◽  
Biological Activities ◽  
Stingless Bee ◽  
Chemical Diversity ◽  
Commercial Interest ◽  
Compound Database ◽  
Ancient Times ◽  
Unique Compound

Propolis is a natural resinous material produced by bees and has been used in folk medicines since ancient times. Due to it possessing a broad spectrum of biological activities, it has gained significant scientific and commercial interest over the last two decades. As a result of searching 122 publications reported up to the end of 2019, we assembled a unique compound database consisting of 578 components isolated from both honey bee propolis and stingless bee propolis, and analyzed the chemical space and chemical diversity of these compounds. The results demonstrated that both honey bee propolis and stingless bee propolis are valuable sources for pharmaceutical and nutraceutical development.

What can phylogeny tell us about chemical diversity?

Planta Medica ◽  
2011 ◽  
Vol 77 (12) ◽  
Author(s):  
N Rønsted ◽  
GI Stafford ◽  
AW Meerow ◽  
G Petersen ◽  
J Van Staden ◽  
...  
Keyword(s):  
Chemical Diversity

Exploration of apoptotic effect in cancer cells treated with stingless bee Trigona incisa propolis native to East Kalimantan, Indonesia

Planta Medica ◽  
2015 ◽  
Vol 81 (16) ◽  
Author(s):  
PM Kustiawan ◽  
ET Arung ◽  
P Phuwapraisirisan ◽  
S Puthong ◽  
T Palaga ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Stingless Bee ◽  
East Kalimantan ◽  
Apoptotic Effect

High throughput screening to investigate Brazilian Cerrado biome plant extract bank chemical diversity

Planta Medica ◽  
2016 ◽  
Vol 81 (S 01) ◽  
pp. S1-S381
Author(s):  
LS Espindola ◽  
RG Dusi ◽  
KR Gustafson ◽  
J McMahon ◽  
JA Beutler
Keyword(s):  
High Throughput ◽  
Plant Extract ◽  
High Throughput Screening ◽  
Chemical Diversity ◽  
Brazilian Cerrado ◽  
Cerrado Biome

Rapid Elaboration of Fragments into Leads Applied to Bromodomain-3 Extra Terminal Domain

2020 ◽  
Author(s):  
Luke Adams ◽  
Lorna E. Wilkinson-White ◽  
Menachem J. Gunzburg ◽  
Stephen J. Headey ◽  
Martin J. Scanlon ◽  
...  
Keyword(s):  
Binding Site ◽  
Systematic Approach ◽  
Structural Information ◽  
Peptide Binding ◽  
Chemical Diversity ◽  
Chemical Probes ◽  
Protein Targets ◽  
Structure Activity ◽  
Peptide Binding Site ◽  
Selection Of

The development of low-affinity fragment hits into higher affinity leads is a major hurdle in fragment-based drug design. Here we demonstrate an approach for the Rapid Elaboration of Fragments into Leads (REFiL) applying an integrated workflow that provides a systematic approach to generate higher-affinity binders without the need for structural information. The workflow involves the selection of commercial analogues of fragment hits to generate preliminary structure-activity relationships. This is followed by parallel microscale chemistry using chemoinformatically designed reagent libraries to rapidly explore chemical diversity. Upon completion of a fragment screen against Bromodomain-3 extra terminal (BRD3-ET) domain we applied the REFiL workflow, which allowed us to develop a series of tetrahydrocarbazole ligands that bind to the peptide binding site of BRD3-ET. With REFiL we were able to rapidly improve binding affinity >30-fold. The REFiL workflow can be applied readily to a broad range of protein targets without the need of a structure, allowing the efficient evolution of low-affinity fragments into higher affinity leads and chemical probes.<br>

Oxazole-Based Compounds As Anticancer Agents

2020 ◽  
Vol 26 (41) ◽  
pp. 7337-7371 ◽  
Author(s):  
Maria A. Chiacchio ◽  
Giuseppe Lanza ◽  
Ugo Chiacchio ◽  
Salvatore V. Giofrè ◽  
Roberto Romeo ◽  
...  
Keyword(s):  
Cancer Research ◽  
Drug Discovery ◽  
Anticancer Agents ◽  
Heterocyclic Compounds ◽  
Chemical Diversity ◽  
Biologically Active ◽  
New Drugs ◽  
The Core ◽  
Anti Cancer ◽  
Biologically Active Derivatives

: Heterocyclic compounds represent a significant target for anti-cancer research and drug discovery, due to their structural and chemical diversity. Oxazoles, with oxygen and nitrogen atoms present in the core structure, enable various types of interactions with different enzymes and receptors, favoring the discovery of new drugs. Aim of this review is to describe the most recent reports on the use of oxazole-based compounds in anticancer research, with reference to the newly discovered iso/oxazole-based drugs, to their synthesis and to the evaluation of the most biologically active derivatives. The corresponding dehydrogenated derivatives, i.e. iso/oxazolines and iso/oxazolidines, are also reported.

Creating Chemical Diversity to Target Protein Kinases

2004 ◽  
Vol 7 (5) ◽  
pp. 453-472 ◽  
Author(s):  
B. Li ◽  
Y. Liu ◽  
T. Uno ◽  
N. Gray
Keyword(s):  
Protein Kinases ◽  
Chemical Diversity ◽  
Target Protein
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