Proteomics

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PROTAC-triggered degradation of MYC

ABSTRACT: The oncogene MYC drives many cancers and is an outstanding therapeutic target. MYC is an intrinsically disordered protein, and therefore, targeting MYC remains a challenge. Here, we developed a proteolysis targeting chimera (PROTAC) degrading MYC: MDEG-541. The inhibitor is based on the MYC-MAX dimerization inhibitor 10058-F4 and Thalidomide. Mode of action depends on the proteasome and cereblon. MDEG-541 shows single digit mM activity in most sensitive colon and pancreatic cancer cell lines as well as gastrointestinal tumor organoids.

INSTRUMENT(S): Orbitrap Fusion Lumos

ORGANISM(S): Homo Sapiens (human)

DISEASE(S): Pancreatic Cancer

SUBMITTER: Stephanie Wilhelm  

LAB HEAD: Prof. Dr. Bernhard Kuster

PROVIDER: PXD018674 | Pride | 2022-05-12

REPOSITORIES: Pride

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3586_GA1_041875_S00_U01_TMT11_R1.raw Raw
3586_GA2_041875_S00_U16_TMT11_R1.raw Raw
3586_GA3_041875_S00_U17_TMT11_R1.raw Raw
3586_GA4_041875_S00_U32_TMT11_R1.raw Raw
3586_GA5_041875_S00_U33_TMT11_R1.raw Raw
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Publications

Targeted protein degradation offers new opportunities to inactivate cancer drivers and has successfully entered the clinic. Ways to induce selective protein degradation include proteolysis targeting chimera (PROTAC) technology and immunomodulatory (IMiDs) / next-generation Cereblon (CRBN) E3 ligase modulating drugs (CELMoDs). Here, we aimed to develop a MYC PROTAC based on the MYC-MAX dimerization inhibitor 10058-F4 derivative 28RH and Thalidomide, called MDEG-541. We show that a subgroup of gas  ...[more]

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