Success examples
Pan-KRAS inhibitor disables oncogenic signalling and tumour growth

Kim D., Herdeis L., Rudolph D., Zhao Y., Böttcher J., Vides A., Ayala-Santos C. I., Pourfarjam Y., Cuevas-Navarro A., Xue J. Y., Mantoulidis A., Bröker J., Wunberg T., Schaaf O., Popow J., Wolkerstorfer B., Kropatsch K. G., Qu R., de Stanchina E., Sang B., Li C., McConnell D. B., Kraut N., Lito P.

Nature 2023, 619(7968):160-166.

KRAS switch I/II pocket inhibitor
DOI
PubMed
Success examples
AMPK activation protects against prostate cancer by inducing a catabolic cellular state

Penfold L., Woods A., Pollard A. E., Arizanova J., Pascual-Navarro E., Muckett P. J., Dore M. H., Montoya A., Whilding C., Fets L., Mokochinski J., Constantin T. A., Varela-Carver A., Leach D. A., Bevan C. L., Nikitin A. Y., Hall Z., Carling D.

Cell Rep. 2023, 42(4):112396.

AMPK Activator
DOI
PubMed
Success examples
Transcriptional Antagonism by CDK8 Inhibition Improves Therapeutic Efficacy of MEK Inhibitors

Malone C. F., Kim M., Alexe G., Engel K., Forman A. B., Robichaud A., Saur Conway A., Goodale A., Meyer A., Khalid D., Thayakumar A., Hatcher J. M., Gray N. S., Piccioni F., Stegmaier K.

Cancer Res 2023, 83(2):285-300.

CDK8 inhibitor
DOI
PubMed
Success examples
Functional E3 ligase hotspots and resistance mechanisms to small-molecule degraders

Hanzl A., Casement R., Imrichova H., Hughes S. J., Barone E., Testa A., Bauer S., Wright J., Brand M., Ciulli A., Winter G. E.

Nat Chem Biol 2022, 61(2):599-618.

SMARCA2/4 PROTAC
DOI
PubMed
Success examples
Inhibition of RAS-driven signaling and tumorigenesis with a pan-RAS monobody targeting the Switch I/II pocket

Wallon L., Khan I., Teng K. W., Koide A., Zuberi M., Li J., Ketavarapu G., Traaseth N. J., O'Bryan J. P., Koide S.

Proc Natl Acad Sci U S A 2022, 119(43):e2204481119.

KRAS switch I/II pocket inhibitor
DOI
PubMed
Success examples
Functional genomic analysis of epithelioid sarcoma reveals distinct proximal and distal subtype biology

Rasmussen S. V., Jin J. X., Bickford L. R., Woods A. D., Sahm F., Crawford K. A., Nagamori K., Goto H., Torres K. E., Sidoni A., Rudzinski E. R., Thway K., Jones R. L., Ciulli A., Wright H., Lathara M., Srinivasa G., Kannan K., Huang P. H., Grünewald T. P. G., Berlow N. E., Keller C.

Clin Transl Med 2022, 12(7):e961. open access

BRD7/BRD9 PROTAC
DOI
PubMed