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Temozolomide (TMZ), which is a triazene derivative that needs no metabolic activation, also has activity in melanoma cells.
Taken together with the fact that the ghrelin receptor GHS-R1A is constitutively active (i.e. has activity in the absence of ghrelin ligand) (Holst et al. 2003), the question arises as to whether circulating ghrelin provides a physiologically relevant gut brain signal for incentive motivation for food reward.
Loss of pRB specifically activates E2F1 to transcriptionally activate ARF through a novel response element that has activity in various tumor cells with defective pRB, but not in normally growing cells [ 3].
OSI-7904L has activity in A-G/GEJA similar to other active agents and an acceptable safety profile.
The data presented support the hypothesis that IBA is minimally active per se, but it remains to be seen whether this compound has activity in vivo as an antagonist.
"Any drug or a cell that has activity in the patients with severe disease is exciting and important," said Dr. Joanne Kurtzberg, director of the pediatric blood and marrow transplant program at Duke University Medical Center.
Sunitinib has activity in patients with metastatic urothelial cancer (UC), but most patients do not respond.
Antimicrotubule therapy (AMT; e.g. vincas and taxanes) has activity in UC.
Antiproliferative assays suggest that the DOX-peptidomimetic conjugate has activity in the lower micromolar range.
In preclinical studies, it has activity in a variety of in vivo tumor model types, including breast cancer.
Retrospective and expanded access data suggest sunitinib has activity in advanced non clear cell renal cell carcinoma (nccRCC).
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