Success examples
The bromodomain and extra-terminal domain degrader MZ1 exhibits preclinical anti-tumoral activity in diffuse large B-cell lymphoma of the activated B cell-like type

Tarantelli C., Cannas E., Ekeh H., Moscatello C., Gaudio E., Cascione L., Napoli S., Rech C., Testa A., Maniaci C., Rinaldi A., Zucca E., Stathis A., Ciulli A., Bertoni F.

Explor Target Antitumor Ther. 2021, 2:586-601.

BET PROTAC
DOI
Success examples
Characterizing PROTAC ternary complex formation using Biacore™ SPR systems

Zollman D., Shepherd C., Cytiva, Ciulli A.

Cytiva.

BET PROTAC
DOI
Success examples
Therapeutical interference with the epigenetic landscape of germ cell tumors: a comparative drug study and new mechanistical insights

Müller M. R., Burmeister A., Skowron M. A., Stephan A., Bremmer F., Wakileh G. A., Petzsch P., Köhrer K., Albers P., Nettersheim D.

Clin Epigenetics 2022, 14 (1):5.

BET PROTAC
DOI
PubMed
Success examples
Into Deep Water: Optimizing BCL6 Inhibitors by Growing into a Solvated Pocket

Lloyd M. G., Huckvale R., Cheung K-M. J., Rodrigues M. J., Collie G. W., Pierrat O. A., Iou M. G., Carter M., Davis O. A., McAndrew P. C., Gunnell E., Le Bihan Y-V., Talbot R., Henley A. T., Johnson L. D., Hayes A., Bright M. D., Raynaud F. I., Meniconi M., Burke R., van Montfort R. L. M., Rossanese O. W., Bellenie B. R., Hoelder S.

J Med Chem. 2021, 64, 23, 17079-17097.

BCL6 inhibitor
DOI
PubMed
Success examples
Frequent mutations of FBXO11 highlight BCL6 as a therapeutic target in Burkitt lymphoma

Pighi C., Cheong T.C., Compagno M., Patrucco E., Arigoni M., Olivero M., Wang Q., Lopez C., Bernhart S.H., Grande B.M., Poggio T., Langellotto F., Bonello L., Dall'Olio R., Martinez-Martin S., Molinaro L., Francia di Celle P., Whitfield J.R., Soucek L., Voena C., Calogero R.A., Morin R.D., Staudt L.M., Siebert R., Zamo A., Chiarle R.

Blood Adv 2021, 5(23):5239-5257.

BCL6 degrader BCL6 inhibitor BCL6 degrader
DOI
PubMed
Success examples
Label-free cell assays to determine compound uptake or drug action using MALDI-TOF mass spectrometry

Unger M. S., Blank M., Enzlein T., Hopf C.

Nat Protoc 2021, Nov 10.

FAS inhibitor
DOI
PubMed