The FDA approval of imatinib in 2001 was a breakthrough in molecularly targeted cancer
therapy and heralded the emergence of kinase inhibitors as a key drug class in the oncology …

Janus kinase (JAK) is a family of cytoplasmic non-receptor tyrosine kinases that includes
four members, namely JAK1, JAK2, JAK3, and TYK2. The JAKs transduce cytokine signaling …

Covalent inhibitors and other types of covalent modalities have seen a revival in the past two
decades, with a variety of new targeted covalent drugs having been approved in recent …

Targeted covalent inhibitors (TCIs) are designed to bind poorly conserved amino acids by
means of reactive groups, the so-called warheads. Currently, targeting noncatalytic cysteine …

Receptor tyrosine kinase signalling pathways have been successfully targeted to inhibit
proliferation and angiogenesis for cancer therapy. However, kinase deregulation has been …

Within druggable target space, new small-molecule modalities, particularly covalent
inhibitors and targeted degraders, have expanded the repertoire of medicinal chemists …

Over the past decade, covalent kinase inhibitors (CKI) have seen a resurgence in drug
discovery. Covalency affords a unique set of advantages as well as challenges relative to …

Accumulating data on cellular and molecular pathways help to develop novel therapeutic
strategies in skin inflammation and autoimmunity. Examples are psoriasis and atopic …

Small molecule degraders such as PROTACs (PROteolysis TArgeting Chimeras) have
emerged as new promising pharmacological modalities and the first PROTAC drug …

Small molecule covalent kinase inhibitors (CKIs) have entered a new era in drug discovery,
which have the advantage for sustained target inhibition and high selectivity. An increased …