Success examples
Combining BET inhibition with SMAC mimetics restricts tumor growth and triggers immune surveillance in preclinical cancer models

Slavic Obradovic K., Ebner F., Artemov A. V., Miotto M., Traexler P-E., Jacob R., Thanh H. P. T., Ruzicka R., Wernitznig A., Baumann I., Gerlach D., Impagnatiello M-A., Siena S., Murphy M., House R., Reiser U., Santoro V., Popow J., Carotta S., Baum A., Lipp J., Bardelli A., Tontsch-Grunt U., Russo M., Aichinger M.

Cell Rep Med. 2025, 6(9):102313.

Orally bioavailable BET inhibitor
DOI
PubMed
Success examples
A Gold-PROTAC Degrades the Oncogenic Tyrosine Kinase MERTK: Insights into the Degradome from a Steady-State System

Thomas S. R., Iellici T., Park M., Klaus E., Bileck A., Gerner C., Meier-Menches S. M., Casini A.

ACS Chem Biol. 2026, 21(1):170-186.

SMARCA2 PROTAC
DOI
PubMed
Success examples
FAK inhibition disrupts tumor growth, apoptosis, and transcriptional regulation in GI-NETs

Toffoli L., Ditsiou A., Triboli L., Hamm V., Moschioni E., D'Este F., Gagliano T.

Endocr Oncol. 2025, 5(1):e250052.

PTK2 PROTAC
DOI
PubMed
Success examples
Curcumin monoglucuronide protects cartilage from progressive degeneration by blocking MMP-13

Roy H. S., Kulkarni C., Neethu K. M., Babu A., Arora M., Jayamurugan G., Mandal D., Guha R., Chattopadhyay N., Ghosh D.

Arch Pharm Res. 2025, 48(7-8):765-781.

MMP-13 antagonist
DOI
PubMed
Success examples
CDK8 Inhibition Releases the Muscle Differentiation Block in Fusion-driven Alveolar Rhabdomyosarcoma

Zhang S., Engel K., Fahs A., Malone C. F., Ross K., Just M., Guedes B., Granum D., Oristian K. M., Kovach A., Alexe G., Digiovanni G., Barbar L., Bentley R., Cerda-Smith C., Le Roux O., Mendes E., Zimmerman S. P., Rees M., Roth J., Shern J. F., Wood K. C., Counter C. M., Linardic C. M., Stegmaier K.

bioRxiv. 2025, 2025.07.14.663986.

CDK8 inhibitor
DOI
PubMed
Success examples
Chemical Control of Protease Activity and Gene Expression Using a Biotin-Released Inhibitory Domain

Van Keuren A. M., Simoes C. T., Tucker C. L.

ACS Synth Biol. 2025, 14(8):3065-3077.

BCL6 degrader
DOI
PubMed