Success examples
BTB BCL6 dimers as building blocks for reversible drug-induced protein oligomerization

Nitsch L., Jensen P., Yoon H., Koeppel J., Burman S. S. R., Fischer E. S., Scholl C., Fröhling S., Słabicki M.

Cell Rep Methods 2022, 2(4):100193.

BCL6 degrader BCL6 inhibitor BCL6 degrader
DOI
PubMed
Success examples
Identification of Sodium Transients Through Na V 1.5 Channels as Regulators of Differentiation in Immortalized Dorsal Root Ganglia Neurons

Martínez A. L., Brea J., Domínguez E., Varela M. J., Allegue C., Cruz R., Monroy X., Merlos M., Burgueño J., Carracedo A., Loza M. I.

Front Cell Neurosci 2022, 16:816325. open access

Nav1.2 channel blocker
DOI
PubMed
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