PROTAC, a revolutionary technology developed in 2001, uses the cell's "cleaner"—the ubiquitin-proteasome system—to selectively destroy harmful proteins in order to treat cancer and other difficult-to-treat disorders, which has risen to prominence among the growing number of new therapies in recent years. Creative Biolabs has been exploring relevant subjects and is fully capable of assisting related research projects with PROTAC molecule design, development, and evaluation solutions. —
PROTAC, a heterobifunctional small molecule, is made up of a chemical linker and two ligands of different binding objectives, of which the discovery workflow initiates with determining the ligands for the target protein and E3 ligase. For the target protein, Creative Biolabs helps design the ligand after taking into account binding interaction patterns and ubiquitination propensity of the target protein or existing small molecule inhibitors.
"Our service covers comprehensive target proteins, including those found in the cytosol, nucleus, and transmembrane," according to a technician, "and if the target proteins of interest are documented transcription factors, non-enzymatic proteins, scaffold proteins, kinases, receptors, or bromodomains, we can provide ready-for-use ligand products based on current research, as well as ligand design services to meet specific demands."
* Nuclear receptors (e.g., AR, ER, RAR)
* Protein kinases (e.g., Akt, BCR, c-Abl, BTK, ALK, CDK9, RIPK2, DAPK1, PSD-95)
* Transcriptional regulatory proteins (e.g., BRD4, Sirt2, HDAC6, TRIM24, IKZF1/3, Smad3)
* Regulatory proteins (e.g., CRABP-I/II, TACC3, AHR, FKBP12, ERRα, X-protein)
* Neurodegenerative-related proteins (e.g., Huntingtin, Tau, α-synuclein)
* Cellular metabolic enzymes (e.g., MetAP-2, DHODH)
For typical research targets, Creative Biolabs established diverse platforms to meet the project needs.
* CLIPTAC: a functional PROTAC molecule formed in the cell via click chemistry.
* Homo-PROTAC: a bivalent small molecule that is designed to dimerize an E3 ligase and subsequently promote its self-degradation.
* HaloPROTAC: bind to and bio-orthogonally label HaloTag fusion proteins in vivo.
* ATTEC: a linker molecule that can interact with both the disease-causing protein and the phagophore protein LC3.
* Trivalent PROTACs: novel PROTAC compounds with longer half-life and acceptable permeability.
Visit https://www.creative-biolabs.com/protac/ to explore more.
Creative Biolabs has been in the industry for over 15 years and has established a specialized research team committed to drug discovery. Following years of research, the company has established one-stop PROTAC-based drug development solutions ranging from early discovery to pre-clinical evaluation, which are well acknowledged by researchers in relevant fields.
Release ID: 89066136