Success examples
Residency time of agonists does not affect the stability of GPCR-arrestin complexes

Mösslein N., Pohle L. G., Fuss A., Bünemann M., Krasel C.

Br J Pharmacol 2022, 179(16):4107-4116. open access

β2AR agonist
DOI
PubMed
Success examples
Targeting Cathepsin C in PR3-ANCA Vasculitis

Jerke U., Eulenberg-Gustavus C., Rousselle A., Nicklin P., Kreideweiss S., Grundl M. A., Eickholz P., Nickles K., Schreiber A., Korkmaz B., Kettritz R.

J Am Soc Nephrol 2022, 33, 5, 936-947.

Cathepsin C inhibitor
DOI
PubMed
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