The Rise of Boron-Containing Compounds: Advancements in Synthesis, Medicinal Chemistry, and Emerging Pharmacology
Boron-containing compounds (BCC) have emerged as important pharmacophores. To date,
five BCC drugs (including boronic acids and boroles) have been approved by the FDA for …
five BCC drugs (including boronic acids and boroles) have been approved by the FDA for …
The versatility of boron in biological target engagement
DB Diaz, AK Yudin - Nature Chemistry, 2017 - nature.com
Boron-containing molecules have been extensively used for the purposes of chemical
sensing, biological probe development and drug discovery. Due to boron's empty p orbital, it …
sensing, biological probe development and drug discovery. Due to boron's empty p orbital, it …
AKIRIN2 controls the nuclear import of proteasomes in vertebrates
M de Almeida, M Hinterndorfer, H Brunner… - Nature, 2021 - nature.com
Protein expression and turnover are controlled through a complex interplay of
transcriptional, post-transcriptional and post-translational mechanisms to enable spatial and …
transcriptional, post-transcriptional and post-translational mechanisms to enable spatial and …
[HTML][HTML] Boron chemicals in drug discovery and development: Synthesis and medicinal perspective
BC Das, NK Nandwana, S Das, V Nandwana… - Molecules, 2022 - mdpi.com
A standard goal of medicinal chemists has been to discover efficient and potent drug
candidates with specific enzyme-inhibitor abilities. In this regard, boron-based bioactive …
candidates with specific enzyme-inhibitor abilities. In this regard, boron-based bioactive …
Design and discovery of boronic acid drugs
J Plescia, N Moitessier - European journal of medicinal chemistry, 2020 - Elsevier
Research related to boronic acids, from synthetic development to materials to drug
discovery, has skyrocketed in the past 20 years. In terms of drug discovery, the incorporation …
discovery, has skyrocketed in the past 20 years. In terms of drug discovery, the incorporation …
The structural modification of natural products for novel drug discovery
Introduction: Throughout history, natural products (NPs) have provided a rich source of
compounds that have wide applications in the fields of medicine, health sciences, pharmacy …
compounds that have wide applications in the fields of medicine, health sciences, pharmacy …
Drug development targeting the ubiquitin–proteasome system (UPS) for the treatment of human cancers
X Zhang, S Linder, M Bazzaro - Cancers, 2020 - mdpi.com
Cancer cells are characterized by a higher rate of protein turnover and greater demand for
protein homeostasis compared to normal cells. In this scenario, the ubiquitin–proteasome …
protein homeostasis compared to normal cells. In this scenario, the ubiquitin–proteasome …
Structure, dynamics and function of the 26S proteasome
Y Mao - Macromolecular protein complexes III: structure and …, 2021 - Springer
The 26S proteasome is the most complex ATP-dependent protease machinery, of~ 2.5 MDa
mass, ubiquitously found in all eukaryotes. It selectively degrades ubiquitin-conjugated …
mass, ubiquitously found in all eukaryotes. It selectively degrades ubiquitin-conjugated …
Integration of mass spectrometry data for structural biology
Mass spectrometry (MS) is increasingly being used to probe the structure and dynamics of
proteins and the complexes they form with other macromolecules. There are now several …
proteins and the complexes they form with other macromolecules. There are now several …
Prospects and limitations of high-resolution single-particle cryo-electron microscopy
A Chari, H Stark - Annual Review of Biophysics, 2023 - annualreviews.org
Single particle cryo-electron microscopy (cryo-EM) has matured into a robust method for the
determination of biological macromolecule structures in the past decade, complementing X …
determination of biological macromolecule structures in the past decade, complementing X …