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
Success examples
BI-3231, an enzymatic-inhibitor of HSD17B13, reduces lipotoxic effects induced by palmitic acid in murine and human hepatocytes

Alcober-Boquet L., Kraus N., Huber L. S., Vutukuri R., Fuhrmann D. C., Stross C., Schaefer L., Scholich K., Zeuzem S., Piiper A., Schulz M. H., Trebicka J., Welsch C., Ortiz C.

Am J Physiol Cell Physiol. 2024, 326(3):C880-C892.

HSD17B13 inhibitor
DOI
PubMed
Success examples
Advancing PROTAC Characterization: Structural Insights through Adducts and Multimodal Tandem-MS Strategies

Rahman M., Marzullo B., Holman S. W., Barrow M., Ray A. D., O’Connor P. B.

J. Am. Soc. Mass Spectrom. 2024, 35, 2, 285–299. open access

BRD7/BRD9 PROTAC
DOI