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PROTEOLYSIS TARGETING CHIMERAS (PROTAC)

PROTEOLYSIS TARGETING CHIMERAS (PROTAC)

Extensive experience in the synthesis of active PROTAC molecules for wide range of biological targets, from kinases to nuclear hormone receptors.
Active anchors could be selected from the literature or discovered through HTS and optimization discovery program

Hands on experience in synthesis and selection of E3 ligase recruiters, e.g. VHL, CRBN, IAP, and others.
Large selection of pre-synthesized ligase recruiters is in stock and available for development program.

Hands on experience in synthesis and selection of active small molecule anchor and E3 ligase recruiter linkers.
Small molecule library is available for CADD evaluation against selected target and for further screening and discovery program.

Hands on experience in synthesis and selection of anchor-recruiter linkers.
Large selection of pre-synthesized linkers is in stock and available for development program.

Discovery and optimization of active small molecules anchors for PROTAC’s:
Protein or ligand based CADD design of active molecules
Small molecules library selection and screening
Computer based modeling studies for PROTAC active anchor exit vector selection
Computer based modeling studies for PROTAC linker selection
Chemistry optimization for linker type and size, linker-anchor or linker-recruiter connection

In vitro biology platform for PROTAC evaluation
Biochemical or cell-based assays for target active small molecules discovery
Protein Simple Jess high throughput capillary Wester blotting system for PROTAC induced protein degradation
– Multiple readouts
– Up to 24 runs in parallel
Selection of suitable cell-based biology platform for PROTAC evaluation:
– Selected ligases expression levels
– Target expression level
Downstream targets or substrates expression levels
In house capabilities for ADME properties of synthesized PROTAC’s evaluation, including animal studies.

We will be happy to hear your requests, comments or questions at
sb@chemdiv.com or chemdiv@chemdiv.com

March 26, 2021 / Blog
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