Pyrrolidine, also known as tetrahydropyrrole, is a saturated five-membered heterocyclic ring, which is miscible with water. Pyrrolidine exists in many alkaloids and drug molecules, such as kappa opioids, antagonists of dopamine D4 receptors, and HIV reverse transcriptase inhibitors.
Pyrrole is a five membered heterocyclic compound with the molecular formula of C4H5N. Pyrrole has a ring composed of four carbon atoms and one nitrogen atom. Pyrrole is easy to polymerize in the air. Pyrrole is the parent compound of many important biological substances (such as bile pigment, porphyrin and chlorophyll). Pyrrole scaffolds are widely used in biological and pharmaceutical fields. Pyrrole is a special heterocyclic scaffold, which exists in many natural products, drug molecules and pesticides, and has shown its application in materials science.
Existing BTK inhibitors directly bind to the active site of BTK and face challenges such as acquired resistance or incomplete responses over time. PROTAC-induced BTK degradation works as a novel alternative therapy for drug-resistant cancers. The latest journal Science publishes the identification of BTK mutations that are susceptible to clinical-stage BTK and IKZF1/3 degrader NX-2127.
Nurix Therapeutics’ TPD compound NX-2127 is a first-in-class, dual-function small-molecule protein degrader. It drives targeted BTK and transcription factor IKAROS (IKZF1/3) degradation through ubiquitination and proteasomal degradation, adding combined benefit. NX-2127 is under development of phase I clinical trials that shows promising results and a manageable safety profile for the treatment of relapsed/ refractory B-cell malignancies.