Recognizing and Exploiting Differences Between RNAi and Small-molecule Inhibitors

Overview

Journal Nat Chem Biol

Specialties Biochemistry
Biology
Chemistry

Date 2007 Nov 17

PMID 18007642

Citations 148

Authors

William A Weiss

Stephen S Taylor

Kevan M Shokat

Affiliations

Soon will be listed here.

Citing Articles

Identification of a Privileged Scaffold for Inhibition of Sterol Transport Proteins through the Synthesis and Ring Distortion of Diverse, Pseudo-Natural Products.

Bro F, Depta L, Dekker N, Bryce-Rogers H, Madsen M, Praestegaard K ACS Cent Sci. 2025; 11(1):136-146.

PMID: 39866705 PMC: 11758220. DOI: 10.1021/acscentsci.4c01657.

Targeting the ERK1/2 and p38 MAPK pathways attenuates Golgi tethering factor golgin-97 depletion-induced cancer progression in breast cancer.

Liu Y, Lin T, Chong K, Chen G, Kuo C, Lin Y Cell Commun Signal. 2025; 23(1):22.

PMID: 39800687 PMC: 11727508. DOI: 10.1186/s12964-024-02010-0.

Redirecting the pioneering function of FOXA1 with covalent small molecules.

Won S, Zhang Y, Reinhardt C, Hargis L, MacRae N, DeMeester K Mol Cell. 2024; 84(21):4125-4141.e10.

PMID: 39413792 PMC: 11560529. DOI: 10.1016/j.molcel.2024.09.024.

A Paradoxical AKT: Exploring the Promise and Challenges of PI3K/AKT/mTOR Targeted Therapies.

Parkman G, Holmen S J Cancer Immunol (Wilmington). 2024; 6(3):92-99.

PMID: 39381117 PMC: 11460539. DOI: 10.33696/cancerimmunol.6.089.

Discovery and Characterization of a Chemical Probe for Cyclin-Dependent Kinase-Like 2.

Bashore F, Min S, Chen X, Howell S, Rinderle C, Morel G ACS Med Chem Lett. 2024; 15(8):1325-1333.

PMID: 39140040 PMC: 11318004. DOI: 10.1021/acsmedchemlett.4c00219.

References

Andrews P . Aurora kinases: shining lights on the therapeutic horizon?. Oncogene. 2005; 24(32):5005-15. DOI: 10.1038/sj.onc.1208752. View

Luo J, Cantley L . The negative regulation of phosphoinositide 3-kinase signaling by p85 and it's implication in cancer. Cell Cycle. 2005; 4(10):1309-12. DOI: 10.4161/cc.4.10.2062. View

Seidler J, McGovern S, Doman T, Shoichet B . Identification and prediction of promiscuous aggregating inhibitors among known drugs. J Med Chem. 2003; 46(21):4477-86. DOI: 10.1021/jm030191r. View

Carmena M, Earnshaw W . The cellular geography of aurora kinases. Nat Rev Mol Cell Biol. 2003; 4(11):842-54. DOI: 10.1038/nrm1245. View

Knight Z, Shokat K . Features of selective kinase inhibitors. Chem Biol. 2005; 12(6):621-37. DOI: 10.1016/j.chembiol.2005.04.011. View

Ditchfield C, Johnson V, Tighe A, Ellston R, Haworth C, Johnson T . Aurora B couples chromosome alignment with anaphase by targeting BubR1, Mad2, and Cenp-E to kinetochores. J Cell Biol. 2003; 161(2):267-80. PMC: 2172902. DOI: 10.1083/jcb.200208091. View

Knight Z, Gonzalez B, Feldman M, Zunder E, Goldenberg D, Williams O . A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling. Cell. 2006; 125(4):733-47. PMC: 2946820. DOI: 10.1016/j.cell.2006.03.035. View

Ruchaud S, Carmena M, Earnshaw W . Chromosomal passengers: conducting cell division. Nat Rev Mol Cell Biol. 2007; 8(10):798-812. DOI: 10.1038/nrm2257. View

Keen N, Taylor S . Aurora-kinase inhibitors as anticancer agents. Nat Rev Cancer. 2004; 4(12):927-36. DOI: 10.1038/nrc1502. View

10.

Kim D, Rossi J . Strategies for silencing human disease using RNA interference. Nat Rev Genet. 2007; 8(3):173-84. DOI: 10.1038/nrg2006. View

11.

Walensky L, Kung A, Escher I, Malia T, Barbuto S, Wright R . Activation of apoptosis in vivo by a hydrocarbon-stapled BH3 helix. Science. 2004; 305(5689):1466-70. PMC: 1360987. DOI: 10.1126/science.1099191. View

12.

Marumoto T, Honda S, Hara T, Nitta M, Hirota T, Kohmura E . Aurora-A kinase maintains the fidelity of early and late mitotic events in HeLa cells. J Biol Chem. 2003; 278(51):51786-95. DOI: 10.1074/jbc.M306275200. View

13.

Girdler F, Gascoigne K, Eyers P, Hartmuth S, Crafter C, Foote K . Validating Aurora B as an anti-cancer drug target. J Cell Sci. 2006; 119(Pt 17):3664-75. DOI: 10.1242/jcs.03145. View

14.

Biggins S, Murray A . The budding yeast protein kinase Ipl1/Aurora allows the absence of tension to activate the spindle checkpoint. Genes Dev. 2001; 15(23):3118-29. PMC: 312839. DOI: 10.1101/gad.934801. View

15.

Ueki K, Fruman D, Yballe C, Fasshauer M, Klein J, Asano T . Positive and negative roles of p85 alpha and p85 beta regulatory subunits of phosphoinositide 3-kinase in insulin signaling. J Biol Chem. 2003; 278(48):48453-66. DOI: 10.1074/jbc.M305602200. View

16.

Jackson A, Bartz S, Schelter J, Kobayashi S, Burchard J, Mao M . Expression profiling reveals off-target gene regulation by RNAi. Nat Biotechnol. 2003; 21(6):635-7. DOI: 10.1038/nbt831. View

17.

An H, Cho N, Yang H, Kwak K, Kim N, Oh D . Targeted RNA interference of phosphatidylinositol 3-kinase p110-beta induces apoptosis and proliferation arrest in endometrial carcinoma cells. J Pathol. 2007; 212(2):161-9. DOI: 10.1002/path.2158. View

18.

Barr A, Gergely F . Aurora-A: the maker and breaker of spindle poles. J Cell Sci. 2007; 120(Pt 17):2987-96. DOI: 10.1242/jcs.013136. View

19.

Meraldi P, Honda R, Nigg E . Aurora-A overexpression reveals tetraploidization as a major route to centrosome amplification in p53-/- cells. EMBO J. 2002; 21(4):483-92. PMC: 125866. DOI: 10.1093/emboj/21.4.483. View

20.

Fan Q, Knight Z, Goldenberg D, Yu W, Mostov K, Stokoe D . A dual PI3 kinase/mTOR inhibitor reveals emergent efficacy in glioma. Cancer Cell. 2006; 9(5):341-9. PMC: 2925230. DOI: 10.1016/j.ccr.2006.03.029. View