Rational design of multitarget-directed ligands: strategies and emerging paradigms
J Zhou, X Jiang, S He, H Jiang, F Feng… - Journal of medicinal …, 2019 - ACS Publications
Due to the complexity of multifactorial diseases, single-target drugs do not always exhibit
satisfactory efficacy. Recently, increasing evidence indicates that simultaneous modulation …
satisfactory efficacy. Recently, increasing evidence indicates that simultaneous modulation …
Rational multitargeted drug design strategy from the perspective of a medicinal chemist
X Li, X Li, F Liu, S Li, D Shi - Journal of Medicinal Chemistry, 2021 - ACS Publications
The development of multitarget-directed ligands (MTDLs) has become a widely focused
research topic, but rational design remains as an enormous challenge. This paper reviews …
research topic, but rational design remains as an enormous challenge. This paper reviews …
Polypharmacology by design: a medicinal chemist's perspective on multitargeting compounds
Multitargeting compounds comprising activity on more than a single biological target have
gained remarkable relevance in drug discovery owing to the complexity of multifactorial …
gained remarkable relevance in drug discovery owing to the complexity of multifactorial …
Polypharmacology: The science of multi-targeting molecules
Polypharmacology is a concept where a molecule can interact with two or more targets
simultaneously. It offers many advantages as compared to the conventional single-targeting …
simultaneously. It offers many advantages as compared to the conventional single-targeting …
Recent developments on 1, 2, 4-triazole nucleus in anticancer compounds: a review
R Kaur, A Ranjan Dwivedi, B Kumar… - Anti-Cancer Agents in …, 2016 - ingentaconnect.com
1, 2, 4-triazole is an important nucleus present in a large number of compounds. More than
thirty-five compounds containing this nucleus are introduced into the market. 1, 2, 4-triazole …
thirty-five compounds containing this nucleus are introduced into the market. 1, 2, 4-triazole …
Designing multi-targeted agents: An emerging anticancer drug discovery paradigm
R Fu, Y Sun, W Sheng, D Liao - European journal of medicinal chemistry, 2017 - Elsevier
The dominant paradigm in drug discovery is to design ligands with maximum selectivity to
act on individual drug targets. With the target-based approach, many new chemical entities …
act on individual drug targets. With the target-based approach, many new chemical entities …
[HTML][HTML] The structural biology of oestrogen metabolism
MP Thomas, BVL Potter - The Journal of steroid biochemistry and …, 2013 - Elsevier
Many enzymes catalyse reactions that have an oestrogen as a substrate and/or a product.
The reactions catalysed include aromatisation, oxidation, reduction, sulfonation …
The reactions catalysed include aromatisation, oxidation, reduction, sulfonation …
Sulfate metabolites provide an intracellular pool for resveratrol generation and induce autophagy with senescence
KR Patel, C Andreadi, RG Britton… - Science translational …, 2013 - science.org
The phytochemical resveratrol has been shown to exert numerous health benefits in
preclinical studies, but its rapid metabolism and resulting poor bioavailability may limit …
preclinical studies, but its rapid metabolism and resulting poor bioavailability may limit …
Quinazolinone-based anticancer agents: synthesis, antiproliferative SAR, antitubulin activity, and tubulin co-crystal structure
W Dohle, FL Jourdan, G Menchon… - Journal of medicinal …, 2018 - ACS Publications
Quinazolinone-based anticancer agents were designed, decorated with functional groups
from a 2-methoxyestradiol-based microtubule disruptor series, incorporating the aryl …
from a 2-methoxyestradiol-based microtubule disruptor series, incorporating the aryl …
Steroid sulphatase and its inhibitors: past, present, and future
PA Foster - Molecules, 2021 - mdpi.com
Steroid sulphatase (STS), involved in the hydrolysis of steroid sulphates, plays an important
role in the formation of both active oestrogens and androgens. Since these steroids …
role in the formation of both active oestrogens and androgens. Since these steroids …