Covalent inhibitors: an opportunity for rational target selectivity

R Lagoutte, R Patouret, N Winssinger - Current opinion in chemical biology, 2017 - Elsevier
There is a resurging interest in compounds that engage their target through covalent
interactions. Cysteine's thiol is endowed with enhanced reactivity, making it the nucleophile …

Orphan GPR52 as an emerging neurotherapeutic target

S Ali, P Wang, RE Murphy, JA Allen, J Zhou - Drug Discovery Today, 2024 - Elsevier
GPR52 is a highly conserved, brain-enriched, G s/olf-coupled orphan G protein-coupled
receptor (GPCR) that controls various cyclic AMP (cAMP)-dependent physiological and …

Chemoproteomic profiling by cysteine fluoroalkylation reveals Myrocin G as an inhibitor of the nonhomologous end joining DNA repair pathway

D Abegg, M Tomanik, N Qiu, D Pechalrieu… - Journal of the …, 2021 - ACS Publications
Chemoproteomic profiling of cysteines has emerged as a powerful method for screening the
proteome-wide targets of cysteine-reactive fragments, drugs, and natural products. Herein …

Cysteine-reactive probes and their use in chemical proteomics

DG Hoch, D Abegg, A Adibekian - Chemical Communications, 2018 - pubs.rsc.org
Proteomic profiling using bioorthogonal chemical probes that selectively react with certain
amino acids is now a widely used method in life sciences to investigate enzymatic activities …

Regio-and stereoselective divergent cross-coupling of alkynes and disubstituted alkenes via photoredox cobalt dual catalysis

SQ Zhang, YL Li, K Cui, C Chen, ZY Gu… - Organic Chemistry …, 2023 - pubs.rsc.org
Achieving divergent synthesis from the same substrates quickly to generate different
products remains an attractive objective in synthetic chemistry and the medicinal industry …

Elephantopinolide AP, germacrane-type sesquiterpene lactones from Elephantopus scaber induce apoptosis, autophagy and G2/M phase arrest in hepatocellular …

M Bai, JJ Chen, W Xu, SH Dong, QB Liu, B Lin… - European Journal of …, 2020 - Elsevier
Chromatographic purification of Elephantopus scaber led to 16 new germacrane-type
sesquiterpene lactones (1–16), named elephantopinolide AP, along with a known analogue …

Palladium‐Catalyzed Asymmetric Allylic Alkylation of 4‐Substituted Isoxazolidin‐5‐ones: Straightforward Access to β2,2‐Amino Acids

M Nascimento de Oliveira… - … –A European Journal, 2018 - Wiley Online Library
We report here an unprecedented and highly enantioselective palladium‐catalyzed allylic
alkylation applied to 4‐substituted isoxazolidin‐5‐ones. Ultimately, the process provides a …

A Two‐Phase Approach to Fusicoccane Synthesis To Uncover a Compound That Reduces Tumourigenesis in Pancreatic Cancer Cells

B Chen, Q Wu, D Xu, X Zhang, Y Ding… - Angewandte …, 2022 - Wiley Online Library
Abstract Alterbrassicicene D (1) and 3 (11)‐epoxyhypoestenone (2) were synthesised via a
two‐phase approach featuring concise construction of the 5‐8‐5 tricyclic intermediate and a …

A palladium-catalyzed asymmetric allylic alkylation approach to α-quaternary γ-butyrolactones

M Nascimento de Oliveira, J Fournier… - Organic …, 2017 - ACS Publications
The Pd-catalyzed asymmetric allylic alkylation (Pd-AAA) of enol carbonates derived from γ-
butyrolactones is reported, affording the corresponding enantioenriched α, α′-disubstituted …

Total Synthesis, Biological Evaluation, and Target Identification of Rare Abies Sesquiterpenoids

DC Davis, DG Hoch, L Wu, D Abegg… - Journal of the …, 2018 - ACS Publications
Abiespiroside A (1), beshanzuenone C (2), and beshanzuenone D (3) belong to the Abies
sesquiterpenoid family. Beshanzuenones C (2) and D (3) are isolated from the critically …