The versatility of boron in biological target engagement

Synthesis of Aminoboronic Acid Derivatives from Amines and Amphoteric Boryl Carbonyl Compounds

(2016) Diego B. Diaz et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Benzoxaborole as a new chemotype for carbonic anhydrase inhibition

(2016) Vincenzo Alterio et al.   CHEMICAL COMMUNICATIONS

Ixazomib: First Global Approval

(2016) Matt Shirley   DRUGS

When Does Chemical Elaboration Induce a Ligand To Change Its Binding Mode?

(2016) Shipra Malhotra et al.   JOURNAL OF MEDICINAL CHEMISTRY

Peptide–Boronic Acid Inhibitors of Flaviviral Proteases: Medicinal Chemistry and Structural Biology

(2016) Christoph Nitsche et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of the First Potent and Selective Inhibitors of Human dCTP Pyrophosphatase 1

(2016) Sabin Llona-Minguez et al.   JOURNAL OF MEDICINAL CHEMISTRY

Hydrogen Bonding of 1,2-Azaborines in the Binding Cavity of T4 Lysozyme Mutants: Structures and Thermodynamics

(2016) Hyelee Lee et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

The N–B Interaction through a Water Bridge: Understanding the Chemoselectivity of a Fluorescent Protein Based Probe for Peroxynitrite

(2016) Zhi-jie Chen et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Inhibition of Mcl-1 through covalent modification of a noncatalytic lysine side chain

(2016) Gizem Akçay et al.   Nature Chemical Biology

MIDA boronates are hydrolysed fast and slow by two different mechanisms

(2016) Jorge A. Gonzalez et al.   Nature Chemistry

Solid Phase Synthesis of C-Terminal Boronic Acid Peptides

(2016) Mira A. M. Behnam et al.   ORGANIC LETTERS

Crystal structure of Zika virus NS2B-NS3 protease in complex with a boronate inhibitor

(2016) Jian Lei et al.   SCIENCE

The inhibition mechanism of human 20Sproteasomes enables next-generation inhibitor design

(2016) Jil Schrader et al.   SCIENCE

Structural basis of metallo-β-lactamase, serine-β-lactamase and penicillin-binding protein inhibition by cyclic boronates

(2016) Jürgen Brem et al.   Nature Communications

Facile synthesis of borofragments and their evaluation in activity-based protein profiling

(2015) Shinya Adachi et al.   CHEMICAL COMMUNICATIONS

Covalent docking of selected boron-based serine beta-lactamase inhibitors

(2015) Jacopo Sgrignani et al.   JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN

Discovery of a Cyclic Boronic Acid β-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases

(2015) Scott J. Hecker et al.   JOURNAL OF MEDICINAL CHEMISTRY

Late-Stage Functionalization of 1,2-Dihydro-1,2-azaborines via Regioselective Iridium-Catalyzed C–H Borylation: The Development of a New N,N-Bidentate Ligand Scaffold

(2015) Andrew W. Baggett et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Toward Efficient Nucleophilic Azaborine Building Blocks for the Synthesis of B–N Naphthyl (Hetero)arylmethane Isosteres

(2015) Javad Amani et al.   ORGANIC LETTERS

Condensation-Driven Assembly of Boron-Containing Bis(Heteroaryl) Motifs Using a Linchpin Approach

(2015) Shinya Adachi et al.   ORGANIC LETTERS

Targeting bacteria via iminoboronate chemistry of amine-presenting lipids

(2015) Anupam Bandyopadhyay et al.   Nature Communications

n-Alkylboronic Acid Inhibitors Reveal Determinants of Ligand Specificity in the Quorum-Quenching and Siderophore Biosynthetic Enzyme PvdQ

(2014) Kenneth D. Clevenger et al.   BIOCHEMISTRY

Targeting Class A and C Serine β-Lactamases with a Broad-Spectrum Boronic Acid Derivative

(2014) Donatella Tondi et al.   JOURNAL OF MEDICINAL CHEMISTRY

The Active Site Sulfenic Acid Ligand in Nitrile Hydratases Can Function as a Nucleophile

(2014) Salette Martinez et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Covalent docking of large libraries for the discovery of chemical probes

(2014) Nir London et al.   Nature Chemical Biology

Glycerol as an Efficient Medium for the Petasis Borono-Mannich Reaction

(2014) Tomi Rosholm et al.   ChemistryOpen

Rational Design of a Transition State Analogue with Picomolar Affinity for Pseudomonas aeruginosa PvdQ, a Siderophore Biosynthetic Enzyme

(2013) Kenneth D. Clevenger et al.   ACS Chemical Biology

α-Boryl Isocyanides Enable Facile Preparation of Bioactive Boropeptides

(2013) Adam Zajdlik et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Discovery of a Novel Class of Boron-Based Antibacterials with Activity against Gram-Negative Bacteria

(2013) Vincent Hernandez et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Synthesis of quaternary α-amino acid-based arginase inhibitors via the Ugi reaction

(2013) Adam Golebiowski et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of (R)-2-Amino-6-borono-2-(2-(piperidin-1-yl)ethyl)hexanoic Acid and Congeners As Highly Potent Inhibitors of Human Arginases I and II for Treatment of Myocardial Reperfusion Injury

(2013) Michael C. Van Zandt et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure and Function of Non-Native Metal Clusters in Human Arginase I

(2012) Edward L. D’Antonio et al.   BIOCHEMISTRY

Boron-based phosphodiesterase inhibitors show novel binding of boron to PDE4 bimetal center

(2012) Yvonne R. Freund et al.   FEBS LETTERS

Iminoboronates: A New Strategy for Reversible Protein Modification

(2012) Pedro M. S. D. Cal et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

UV-Photoelectron Spectroscopy of 1,2- and 1,3-Azaborines: A Combined Experimental and Computational Electronic Structure Analysis

(2012) Anna Chrostowska et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Schiff base formation and recognition of amino sugars, aminoglycosides and biological polyamines by 2-formyl phenylboronic acid in aqueous solution

(2012) Nini J. Gutiérrez-Moreno et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Crystal Structures of Complexes with Cobalt-Reconstituted Human Arginase I

(2011) Edward L. D’Antonio et al.   BIOCHEMISTRY

Structure-Based Design of Novel Boronic Acid-Based Inhibitors of Autotaxin

(2011) Harald M. H. G. Albers et al.   JOURNAL OF MEDICINAL CHEMISTRY

Unexpected Tricovalent Binding Mode of Boronic Acids within the Active Site of a Penicillin-Binding Protein

(2011) Astrid Zervosen et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Structural basis of substrate discrimination and integrin binding by autotaxin

(2011) Jens Hausmann et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Ring Structure and Aromatic Substituent Effects on the pKa of the Benzoxaborole Pharmacophore

(2011) John W. Tomsho et al.   ACS Medicinal Chemistry Letters

Novel macrocyclic HCV NS3 protease inhibitors derived from α-amino cyclic boronates

(2010) Xianfeng Li et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Evaluation of the Proteasome Inhibitor MLN9708 in Preclinical Models of Human Cancer

(2010) E. Kupperman et al.   CANCER RESEARCH

Boron Mimetics: 1,2-Dihydro-1,2-azaborines Bind inside a Nonpolar Cavity of T4 Lysozyme

(2009) Lijun Liu et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Potent and Selective Peptidyl Boronic Acid Inhibitors of the Serine Protease Prostate-Specific Antigen

(2008) Aaron M. LeBeau et al.   CHEMISTRY & BIOLOGY