Proteolysis-targeting chimeras (PROTACs) and targeted covalent inhibitors (TCIs) are
currently two exciting strategies in the fields of chemical biology and drug discovery …

Ground‐breaking research in disease biology and continuous efforts in method
development have uncovered a range of potential new drug targets. Increasingly, the drug …

The Plasmodium falciparum proteasome constitutes a promising antimalarial target, with
multiple chemotypes potently and selectively inhibiting parasite proliferation and synergizing …

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 …

The nucleus controls cell growth and division through coordinated interactions between
nuclear proteins and chromatin. Mutations that impair nuclear protein association with …

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 …

Macrocyclic peptides are attractive for chemoproteomic applications due to their modular
synthesis and potential for high target selectivity. We describe a solid phase synthesis …

There has been tremendous progress in covalent inhibitors as evidenced by the ascent of
innovative electrophilic warheads with suppressed non‐specific reactivity but enhanced …

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 …

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 …