Success examples
KRAS is vulnerable to reversible switch-II pocket engagement in cells

Vasta J. D., Peacock D. M., Zheng Q., Walker J. A., Zhang Z., Zimprich C. A., Thomas M. R., Beck M. T., Binkowski B. F., Corona C. R., Robers M. B., Shokat K. M.

Nat Chem Biol 2022, 18(6):596-604. open access.

KRAS switch I/II pocket inhibitor
DOI
PubMed
Success examples
BAF complexes drive proliferation and block myogenic differentiation in fusion-positive rhabdomyosarcoma

Laubscher D., Gryder B. E., Sunkel B. D., Andresson T., Wachtel M., Das S., Roschitzki B., Wolski W., Wu X. S., Chou H-C., Song Y. K., Wang C., Wei J. S., Wang M., Wen X., Ngo Q. A., Marques J. G., Vakoc C. R., Schäfer B. W., Stanton B. Z., Khan J.

Nat Commun 2021, 12(1):6924. open access

SMARCA2/4 PROTAC
DOI
PubMed
Success examples
Plk1 regulates mutant IDH1 enzyme activity and mutant IDH2 ubiquitination in mitosis

Reddy M. S., Bhattacharjee D., Jain N.

Cell Signal 2022, 92:110279.

PLK1 inhibitor
DOI
PubMed
Success examples
KRAS(G12D) can be targeted by potent inhibitors via formation of salt bridge

Mao Z., Xiao H., Shen P., Yang Y., Xue J., Yang Y., Shang Y., Zhang L., Li X., Zhang Y., Du Y., Chen C-C., Guo R-T., Zhang Y.

Cell Discov 2022, 8, 5.

KRAS switch I/II pocket inhibitor
DOI
PubMed
Success examples
SMARCA4 biology in alveolar rhabdomyosarcoma

Bharathy N., Cleary M. M., Kim J-A., Nagamori K., Crawford K. A., Wang E., Saha D., Settelmeyer T. P., Purohit R., Skopelitis D., Chang K., Doran J. A., Kirschbaum C. W., Bharathy S., Crews D. W., Randolph M. E., Karnezis A. N., Hudson-Price L., Dhawan J., Michalek J. E., Ciulli A., Vakoc C. R., Keller C.

Oncogene 2022, 41(11):1647-1656.

SMARCA2/4 PROTAC
DOI
PubMed
Success examples
Pharmacological Dissection of the Crosstalk between NaV and CaV Channels in GH3b6 Cells

Réthoré L., Park J., Montnach J., Nicolas S., Khoury J., Le Seac'h E., Mabrouk K., De Pomyers H., Tricoire-Leignel H., Mattei C., Henrion D., Fajloun Z., De Waard M., Legendre C., Legros C.

Int J Mol Sci. 2022, 23 (2):827.

Nav1.2 channel blocker
DOI
PubMed