There are over 500 human kinases ranging from very well-studied to almost completely
ignored. Kinases are tractable and implicated in many diseases, making them ideal targets …

Covalent fragment approaches combine advantages of covalent binders and fragment-
based drug discovery (FBDD) for target identification and validation. Although early …

Abstract To date, Proteolysis Targeting Chimera (PROTAC) technology has been
successfully applied to mediate proteasomal-induced degradation of several …

The scientific community has shown considerable interest in proteolysis-targeting chimeras
(PROTACs) in the last decade, indicating their remarkable potential as a means of achieving …

The Ataxia telangiectasia and RAD3-related (ATR) kinase is a key regulator of DNA
replication stress responses and DNA-damage checkpoints. Several potent and selective …

Proteolysis targeting chimera (PROTAC) technology has become a powerful strategy in drug
discovery, especially for undruggable targets/proteins. A typical PROTAC degrader consists …

G 1 to S phase transition 1 (GSPT1) is the requisite release factor for the translation
termination. GSPT1 is identified as an oncogenic driver of several types of cancer and …

Nuclear receptor-binding SET domain 3, otherwise known as NSD3, is a member of the
group of lysine methyltransferases and is involved in a variety of cellular processes …

Targeted protein degradation (TPD) is a promising approach that has the ability to address
disease-causing proteins. Compared to traditional inhibition, proteolysis targeting chimera …

Leukemia is a heterogeneous group of life‐threatening malignant disorders of the
hematopoietic system. Immunotherapy, radiotherapy, stem cell transplantation, targeted …