Phosphonate and bisphosphonate inhibitors of farnesyl pyrophosphate synthases: A structure-guided perspective

J Park, VR Pandya, SJ Ezekiel, AM Berghuis - Frontiers in Chemistry, 2021 - frontiersin.org
Phosphonates and bisphosphonates have proven their pharmacological utility as inhibitors
of enzymes that metabolize phosphate and pyrophosphate substrates. The blockbuster …

Emergence of terpene chemical communication in insects: Evolutionary recruitment of isoprenoid metabolism

Z Rebholz, L Shewade, K Kaler, H Larose… - Protein …, 2023 - Wiley Online Library
Insects have evolved a chemical communication system using terpenoids, a structurally
diverse class of specialized metabolites, previously thought to be exclusively produced by …

Electrochemically induced Markovnikov-type selective hydro/deuterophosphonylation of electron-rich alkenes

W Deng, Y Hu, J Hu, X Li, Y Li, Y Huang - Chemical Communications, 2022 - pubs.rsc.org
The regioselective hydro/deuterophosphonylation of electron-rich alkenes with P (O) H
compounds has been realized via a metal-free electrochemically induced strategy …

Synthesis and evaluation of structurally diverse C-2-substituted thienopyrimidine-based inhibitors of the human geranylgeranyl pyrophosphate synthase

HF Lee, CM Lacbay, R Boutin, AN Matralis… - Journal of Medicinal …, 2022 - ACS Publications
Novel analogues of C-2-substituted thienopyrimidine-based bisphosphonates (C2-ThP-BPs)
are described that are potent inhibitors of the human geranylgeranyl pyrophosphate …

Copper (i)-catalysed intramolecular hydroarylation-redox cross-dehydrogenative coupling of N-propargylanilines with phosphites

G Li, G Yu, C Wang, T Morita, X Zhang… - Organic & Biomolecular …, 2022 - pubs.rsc.org
Intramolecular hydroarylation-redox cross-dehydrogenative coupling of N-propargylanilines
with phosphite diesters proceeded in the presence of Cu (I)-catalysts (20 mol%) to …

Synthesis of β‐Aryl‐α, β‐Dehydroaminophosphonates by Pd‐Catalyzed Fujiwara–Moritani C− C Coupling

J Sáez, D Dalmau, FJ Sayago… - European Journal of …, 2024 - Wiley Online Library
The treatment of diethyl α, β‐dehydroaminophosphonate 1 with various arenes (ArH=
toluene 2 a, benzene 2 b, anisole 2 c, bromobenzene 2 d, chlorobenzene 2 e, benzyl …

Inhibition of human mevalonate kinase by allosteric inhibitors of farnesyl pyrophosphate synthase

S Salari, HF Lee, YS Tsantrizos, J Park - FEBS Open Bio, 2024 - Wiley Online Library
Mevalonate kinase is a key regulator of the mevalonate pathway, subject to feedback
inhibition by the downstream metabolite farnesyl pyrophosphate. In this study, we validated …

Rh (I)-catalyzed asymmetric transfer hydrogenation of α-enamidophosphonates to α-aminophosphonates

Y Feng, P Viereck, SG Li, YS Tsantrizos - Tetrahedron, 2022 - Elsevier
An asymmetric Rh-catalyzed transfer hydrogenation was developed for the conversion of α-
enamidophosphonates to α-aminophosphonates (α-APs) using isopropanol as the hydride …

[HTML][HTML] Multiplexed experimental strategies for fragment library screening against challenging drug targets using SPR biosensors

EA FitzGerald, D Vagrys, G Opassi, HF Klein… - SLAS Discovery, 2024 - Elsevier
Surface plasmon resonance (SPR) biosensor methods are ideally suited for fragment-based
lead discovery. However, generally applicable experimental procedures and detailed …

Access to α-Aminophosphonic Acid Derivatives and Phosphonopeptides by [Rh (P–OP)]-Catalyzed Stereoselective Hydrogenation

H Fernández-Pérez, P Lenartowicz… - The Journal of …, 2020 - ACS Publications
The hydrogenation of N-substituted vinylphosphonates using rhodium complexes derived
from P–OP ligands L1, ent-L1, or (R, R)-Me-DuPHOS as catalysts has been successfully …