Applications of covalent chemistry in targeted protein degradation
Proteolysis-targeting chimeras (PROTACs) and targeted covalent inhibitors (TCIs) are
currently two exciting strategies in the fields of chemical biology and drug discovery …
currently two exciting strategies in the fields of chemical biology and drug discovery …
EFMC: trends in medicinal chemistry and chemical biology
YP Auberson, PB Arimondo, M Duca, S Essig… - …, 2023 - Wiley Online Library
Ground‐breaking research in disease biology and continuous efforts in method
development have uncovered a range of potential new drug targets. Increasingly, the drug …
development have uncovered a range of potential new drug targets. Increasingly, the drug …
[HTML][HTML] Mitigating the risk of antimalarial resistance via covalent dual-subunit inhibition of the Plasmodium proteasome
The Plasmodium falciparum proteasome constitutes a promising antimalarial target, with
multiple chemotypes potently and selectively inhibiting parasite proliferation and synergizing …
multiple chemotypes potently and selectively inhibiting parasite proliferation and synergizing …
[HTML][HTML] Docking and selectivity studies of covalently bound Janus kinase 3 inhibitors
HA Zhong, S Almahmoud - International Journal of Molecular Sciences, 2023 - mdpi.com
The Janus kinases (JAKs) are a family of non-receptor cytosolic protein kinases critical for
immune signaling. Many covalently bound ligands of JAK3 inhibitors have been reported. To …
immune signaling. Many covalently bound ligands of JAK3 inhibitors have been reported. To …
Profiling nuclear cysteine ligandability and effects on nuclear localization using proximity labeling-coupled chemoproteomics
Q Peng, E Weerapana - Cell Chemical Biology, 2024 - cell.com
The nucleus controls cell growth and division through coordinated interactions between
nuclear proteins and chromatin. Mutations that impair nuclear protein association with …
nuclear proteins and chromatin. Mutations that impair nuclear protein association with …
4‐O‐Substituted Glucuronic Cyclophellitols are Selective Mechanism‐Based Heparanase Inhibitors
V Borlandelli, Z Armstrong, A Nin‐Hill… - …, 2023 - Wiley Online Library
Degradation of the extracellular matrix (ECM) supports tissue integrity and homeostasis, but
is also a key factor in cancer metastasis. Heparanase (HPSE) is a mammalian ECM …
is also a key factor in cancer metastasis. Heparanase (HPSE) is a mammalian ECM …
Solid phase synthesis of fluorosulfate containing macrocycles for chemoproteomic workflows
FF Faucher, D Abegg, P Ipock… - Israel Journal of …, 2023 - Wiley Online Library
Macrocyclic peptides are attractive for chemoproteomic applications due to their modular
synthesis and potential for high target selectivity. We describe a solid phase synthesis …
synthesis and potential for high target selectivity. We describe a solid phase synthesis …
New Cysteine Covalent Modification Strategies Enable Advancement of Proteome‐wide Selectivity of Kinase Modulators
I Guan, K Williams, J Pan, X Liu - Asian Journal of Organic …, 2021 - Wiley Online Library
There has been tremendous progress in covalent inhibitors as evidenced by the ascent of
innovative electrophilic warheads with suppressed non‐specific reactivity but enhanced …
innovative electrophilic warheads with suppressed non‐specific reactivity but enhanced …
[HTML][HTML] Synthesis and Biological Evaluation of Chalconesulfonamides: En Route to Proapoptotic Agents with Antiestrogenic Potency
SK Krymov, DI Salnikova, LG Dezhenkova… - Pharmaceuticals, 2023 - mdpi.com
Breast and other estrogen receptor α-positive cancers tend to develop resistance to existing
drugs. Chalcone derivatives possess anticancer activity based on their ability to form …
drugs. Chalcone derivatives possess anticancer activity based on their ability to form …
[HTML][HTML] Drug Discovery Based on Oxygen and Nitrogen (Non-)Heterocyclic Compounds Developed @LAQV–REQUIMTE/Aveiro
JLC Sousa, HMT Albuquerque, AMS Silva - Pharmaceuticals, 2023 - mdpi.com
Artur Silva's research group has a long history in the field of medicinal chemistry. The
development of new synthetic methods for oxygen (mostly polyphenols, eg, 2-and 3 …
development of new synthetic methods for oxygen (mostly polyphenols, eg, 2-and 3 …