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. Author manuscript; available in PMC: 2017 Feb 1.
Published in final edited form as: Semin Cancer Biol. 2015 Sep 30;36:105–119. doi: 10.1016/j.semcancer.2015.09.014

Table 1.

Summary of small molecule targeting F-box protein in cancer

F-box Protein Disease Link Compound Structure Mechanism Reference
Skp2 Multiple myeloma Compound A (CpdA) graphic file with name nihms726875t1.jpg Interferes Skp2-Skp1 interaction and stabilizes p27 (49)
Prostate cancer SMIP004 graphic file with name nihms726875t2.jpg Downregulates Skp2 (51)
Metastatic melanoma, prostate, breast, ovarian, lung cancer C1, C2, C16, C20 graphic file with name nihms726875t3.jpg Binds to a pocket formed by Skp2 and Cks1 to block substrate binding (52)
Cancer, general Compound #25 graphic file with name nihms726875t4.jpg Binds to Skp2 and prevents Skp2-Skp1 interaction (47)
Breast, prostate cancer Curcumin graphic file with name nihms726875t5.jpg Natural agents, inhibit Skp2 expression (146–148)
Quercetin graphic file with name nihms726875t6.jpg
Lycopene graphic file with name nihms726875t7.jpg
silibinin graphic file with name nihms726875t8.jpg
EGCG graphic file with name nihms726875t9.jpg
Vitamin D graphic file with name nihms726875t10.jpg
κ-TrCP Inflammation GS143 graphic file with name nihms726875t11.jpg Disrupts interaction between phospho-IκBκκ and κ-TrCP and suppress IκBκ ubiquitylation (65)
Cancer, general Erioflorin graphic file with name nihms726875t12.jpg Inhibits the interaction between κ-TrCP and tumor suppressor Pdcd4 (71)
Fbxw7 Pancreatic cancer SINE KPT-185 graphic file with name nihms726875t13.jpg Inhibits nuclear export of Fbxw7, enhances nuclear retention of Fbxw7 and degrades Notch1 (149)
Leukemia, lymphoma Oridonin graphic file with name nihms726875t14.jpg Increases Fbxw7 expression, activates GSK3 and facilitates c-Myc turnover (150)
Genistein graphic file with name nihms726875t15.jpg Inhibits miR-223 expression and elevates its target Fbxw7 expression (87)
Fbxl2 Inflammation BC-1215 graphic file with name nihms726875t16.jpg Inhibits the Fbxo3 and Fbxl2 binding (28)
BC-1258 graphic file with name nihms726875t17.jpg Inhibits binding between Fbxo3 and Fbxl2, stabilizes Fbxl2 and promotes Aurora B degradation (103)
Fbxl3 circadian-related disorders (sleep disorder, cancer, cardiovascular and metabolic diseases KL001 graphic file with name nihms726875t18.jpg Competes for binding in the FAD pocket of CRYs and prevents Fbxl3 binding (151,152)