RAS proteins are small GTPases that act as molecular switches to transduce signals from activated receptors. When in its GTP-bound state, RAS can bind to and activate a range of downstream effector proteins, which may then result in diverse cellular outcomes like cell proliferation, survival, differentiation, and neoplastic transformation. Three RASgenes code for four highly homologous RAS proteins, NRAS, HRAS, and KRAS4B/KRAS4A. These proteins have identical effector binding domains and hence can interact with the same set of downstream effectors. However, RASisoforms have been shown to differ in their abilities to activate various downstream proteins. Mutations affecting the three prototype Ras oncoproteins, HRAS, NRAS and KRAS, show a high degree of tumor-type specificity[1]. Oncogenic versions of HRAS are better than NRAS or KRAS at transforming fibroblast cells, whereas NRAS is better at transforming hematopoietic cells. Nearly 30% of human cancers, including solid tumors and hematologic malignancies, are associated with mutations in RAS genes[2]. Therapies that target the RAS proteins and the signaling pathways that they control would therefore be very valuable in treating tumours that have activating RAS mutations. However, their potential might be even greater, as many tumours that lack RAS mutations have found other ways to activate the same pathways[3].

RAS GTPases listed: HRAS, Rab7, Rac

[1] A. Berns et al. Kras and Hras--what is the difference? Nat. Genet. 2008, 40, 1149-1150.
[2] C. Parikh et al. Oncogenic NRAS, KRAS, and HRAS exhibit different leukemogenic potentials in mice. Cancer Res. 2007, 67, 7139-7146.
[3] J. Downward et al. TargetingRAS signalling pathways in cancer therapy. Nat. Rev. Cancer. 2003, 3, 11-22.

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Axon ID Name Description From price
3575 AMG510 Highly potent, selective, and orally bioavailable KRAS-G12C inhibitor €90.00
3084 ARS-1620 Potent, selective, and orally bioavailable covalent KRAS-G12C inhibitor €145.00
3053 BAY-293 Potent, selective and cell-active inhibitor of KRAS-SOS1 interaction €140.00
3471 BI-3406 Inhibitor of KRAS/Son of Sevenless 1 (SOS1) interaction Inquire
2829 Fendiline hydrochloride KRAS inhibitor; Ca2+ channel blocker (L-type voltage gated) €50.00
3768 GDC-6036 Inhibitor of KRAS G12C Inquire
3761 MRTX1133 First-in-class, noncovalent, selective & reversible inhibitor of KRASG12D mutant €220.00
3733 MRTX1257 Irreversible covalent inhibitor of KRAS G12C Inquire
4036 MRTX849 Potent, mutation-selective, and irreversible covalent inhibitor of KRAS-G12C Inquire

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