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PROTAC Synthesis and Screening for Targeted Protein Degradation

We offer expertise in the synthesis of PROTACs and partial PROTACs for targeted protein degradation & integrated drug discovery even on the multi-gram scale.

Description

PROteolysis – TArgeting Chimeras (PROTACs) are a series of hetero-bifunctional molecules that hijack the body’s own natural disposal system to initiate selective degradation of the protein of interest (POI). PROTACs have the potential to overcome most of the limitations of small molecule inhibitors, and they offer several advantages of the traditional concepts of drug discovery. Aurigene offers expertise in the synthesis of PROTACs and partial PROTACs for targeted protein degradation & integrated drug discovery even on the multi-gram scale.      

We have extensive experience in not only the synthesis and purification of PROTACs, but also the capability of extensively profiling our synthesized PROTACs including various Biological assays, DMPK and Toxicology support. We are uniquely poised in the Indian CRO market not only as a key player with extensive knowledge in small molecule-based Drug Discovery research, but also can offer our significant experience on the PROTAC-related domain to any potential collaborators.      

We are well versed in the synthesis and functionalization of various E3-ligase ligands such as CRBN, VHL, MDM2, and cIAP1 (in multi-gram scale) and in the synthesis of commercially available ligands, as well as in developing novel structural analogues as per custom requests. We also have significant experience in the niche fields of Targeted Protein Degradation (TPD) like molecular glues and ATTECs.
 

  • Synthesis of common E3-Ligase ligands (CRBN, VHL, cIAP and MDM-2) and their structural analogues from milligram to gram scale and beyond
  • Capability to develop novel flexible or rigid linkers for novel discovery needs
  • Experience in the synthesis of molecular glues and monovalent protein degraders
  • In-house library of >300 partial PROTACs and linkers for rapid target engagement
  • Flexible business models including stand-alone and various integrated services
  • Stand-alone biology support including in vitro and in vivo profiling, DMPK, or toxicology