Success examples
The small molecule BI-2852 induces a nonfunctional dimer of KRAS

Tran T. H., Alexander P., Dharmaiah S., Agamasu C., Nissley D. V., McCormick F., Esposito D., Simanshu D. K., Stephen A. G., Balius T. E.

Proc Natl Acad Sci U S A. 2020, 117(7):3363-3364.

KRAS switch I/II pocket inhibitor
DOI
PubMed
Success examples
Glutamine deprivation alters the origin and function of cancer cell exosomes

Fan S. J., Kroeger B., Marie P. P., Bridges E. M., Mason J. D., McCormick K., Zois C. E., Sheldon H., Khalid Alham N., Johnson E., Ellis M., Stefana M. I., Mendes C. C., Wainwright S.M., Cunningham C., Hamdy F. C., Morris J. F., Harris A. L., Wilson C., Goberdhan D. C. 

EMBO J. 2020, 39(16):e103009.

KRAS switch I/II pocket inhibitor
DOI
PubMed
Success examples
Co-targeting SOS1 enhances the antitumor effects of KRASG12C inhibitors by addressing intrinsic and acquired resistance

Thatikonda V., Lyu H., Jurado S., Kostyrko K., Bristow C. A., Albrecht C., Alpar D., Arnhof H., Bergner O., Bosch K., Feng N., Gao S., Gerlach D., Gmachl M., Hinkel M., Lieb S., Jeschko A., Machado A. A., Madensky T., Marszalek E. D., Mahendra M., Melo-Zainzinger G., Molkentine J. M., Jaeger P. A., Peng D. H., Schenk R. L., Sorokin A., Strauss S., Trapani F., Kopetz S., Vellano C. P., Petronczki M., Kraut N., Heffernan T. P., Marszalek J. R., Pearson M., Waizenegger I. C., Hofmann M. H.

Nat Cancer. 2024, 5:1352–1370.

SOS1::KRAS inhibitor
DOI
PubMed
Success examples
On-demand release of a selective MMP-13 blocker from an enzyme-responsive injectable hydrogel protects cartilage from degenerative progression in osteoarthritis

Roy H. S., Murugesan P., Kulkarni C., Arora M., Nagar G. K., Guha R., Chattopadhyay N., Ghosh D.

J Mater Chem B. 2024, 12(22):5325-5338.

MMP-13 antagonist
DOI
PubMed
Success examples
LOX-1 acts as an N6-methyladenosine-regulated receptor for Helicobacter pylori by binding to the bacterial catalase

Zeng J., Xie C., Huang Z., Cho C. H., Chan H., Li Q., Ashktorab H., Smoot D. T., Wong S. H., Yu J., Gong W., Liang C., Xu H., Chen H., Liu X., Wu J. C. Y., Ip M., Gin T., Zhang L., Chan M. T. V., Hu W., Wu W. K. K.

Nat Commun. 2024, 15(1):669.

LOX-1 inhibitor
DOI
PubMed