Success examples
A cathepsin C-like protease mediates the post-translation modification of Toxoplasma gondii secretory proteins for optimal invasion and egress

Thornton L. B., Key M., Micchelli C., Stasic A. J., Kwain S., Floyd K., Moreno S. N. J., Dominy B. N., Whitehead D. C., Dou Z.

mBio 2023, e0017423. Epub 2023 Jun 16.

DPAP1 Inhibitor
DOI
PubMed
Success examples
Canonical BAF complex activity shapes the enhancer landscape that licenses CD8+ T cell effector and memory fates

McDonald B., Chick B. Y., Ahmed N. S., Burns M., Ma S., Casillas E., Chen D., Mann T. H., O'Connor C., Hah N., Hargreaves D. C., Kaech S. M.

Immunity 2023, 56(6):1303-1319.e5.

SMARCA2/4 PROTAC
DOI
PubMed
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