| Target Validation Information | |||||
|---|---|---|---|---|---|
| TTD ID | T16016 | ||||
| Target Name | C-C chemokine receptor type 1 (CCR1) | ||||
| Type of Target |
Clinical trial |
||||
| Drug Potency against Target | MLN3897 | Drug Info | IC50 = 0.8 nM | [2] | |
| COSALANE | Drug Info | IC50 = 260 nM | [1] | ||
| Action against Disease Model | MLN3897 | Drug Info | MLN3897, a novel CCR1 inhibitor, impairs osteoclastogenesis and inhibits the interaction of multiple myeloma cells and osteoclasts. MLN3897 demonstrates significant impairment of OC formation (by 40%) and function (by 70%), associated with decreased precursor cell multinucleation and down-regulation of c-fos signaling. OCs secrete high levels of CCL3, which triggers MM cell migration; conversely, MLN3897 abrogates its effects by inhibiting Akt signaling. Moreover, MM cell-to-OC adhesion was abrogated by MLN3897, thereby inhibiting MM cell survival and proliferation. | [2] | |
| References | |||||
| REF 1 | Inhibition of RANTES/CCR1-mediated chemotaxis by cosalane and related compounds. Bioorg Med Chem Lett. 2001 Jan 8;11(1):59-62. | ||||
| REF 2 | MLN3897, a novel CCR1 inhibitor, impairs osteoclastogenesis and inhibits the interaction of multiple myeloma cells and osteoclasts. Blood. 2007 Nov 15;110(10):3744-52. | ||||
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