The Rise of Boron-Containing Compounds: Advancements in Synthesis, Medicinal Chemistry, and Emerging Pharmacology

RJ Grams, WL Santos, IR Scorei, A Abad-García… - Chemical …, 2024 - ACS Publications
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 …

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 …

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 …

[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 …

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 …

The structural modification of natural products for novel drug discovery

H Yao, J Liu, S Xu, Z Zhu, J Xu - Expert opinion on drug discovery, 2017 - Taylor & Francis
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 …

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 …

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 …

Integration of mass spectrometry data for structural biology

HM Britt, T Cragnolini, K Thalassinos - Chemical Reviews, 2021 - ACS Publications
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 …

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 …