231634-78-9Relevant articles and documents
Multistimuli responsive nanocomposite tectons for pathway dependent self-assembly and acceleration of covalent bond formation
Wang, Yuping,Santos, Peter J.,Kubiak, Joshua M.,Guo, Xinheng,Lee, Margaret S.,Macfarlane, Robert J.
, p. 13234 - 13243 (2019)
Nanocomposite tectons (NCTs) are a recently developed building block for polymer-nanoparticle composite synthesis, consisting of nanoparticle cores functionalized with dense monolayers of polymer chains that terminate in supramolecular recognition groups
Discovery of Novel Flavonoid Dimers to Reverse Multidrug Resistance Protein 1 (MRP1, ABCC1) Mediated Drug Resistance in Cancers Using a High Throughput Platform with "click Chemistry"
Wong, Iris L. K.,Zhu, Xuezhen,Chan, Kin-Fai,Law, Man Chun,Lo, Aya M. Y.,Hu, Xuesen,Chow, Larry M. C.,Chan, Tak Hang
, p. 9931 - 9951 (2018/12/11)
A 300-member flavonoid dimer library of multidrug resistance-associated protein 1 (MRP1, ABCC1) modulators was rapidly assembled using "click chemistry". Subsequent high-throughput screening has led to the discovery of highly potent (EC50 ranging from 53 to 298 nM) and safe (selective indexes ranging from >190 to >1887) MRP1 modulators. Some dimers have potency about 6.5- to 36-fold and 64- to 358-fold higher than the well-known MRP1 inhibitors, verapamil, and MK571, respectively. They inhibited DOX efflux and restored intracellular DOX concentration. The most potent modulator, Ac3Az11, was predicted to bind to the bipartite substrate-binding site of MRP1 in a competitive manner. Moreover, it provided sufficient concentration to maintain its plasma level above its in vitro EC50 (53 nM for DOX) for about 90 min. Overall, we demonstrate that "click chemistry" coupled with high throughput screening is a rapid, reliable, and efficient tool in the discovery of compounds having potent MRP1-modualting activity.
Competition-based, quantitative chemical proteomics in breast cancer cells identifies new target profiles for sulforaphane
Clulow, James A.,Storck, Elisabeth M.,Lanyon-Hogg, Thomas,Kalesh, Karunakaran A.,Jones, Lyn H.,Tate, Edward W.
supporting information, p. 5182 - 5185 (2017/07/12)
Sulforaphane is a small molecule isothiocyanate which exhibits anticancer potential, yet its biological targets remain poorly understood. Here we employ a competition-based chemical proteomics strategy to profile sulforaphane's targets and identify over 500 targets along with their relative affinities. These targets provide a new set of mediators for sulforaphane's bioactivity, and aid understanding of its complex mode of action.
A switchable [2]rotaxane asymmetric organocatalyst that utilizes an acyclic chiral secondary amine
Blanco, Victor,Leigh, David A.,Marcos, Vanesa,Morales-Serna, José A.,Nussbaumer, Alina L.
supporting information, p. 4905 - 4908 (2014/04/17)
A rotaxane-based switchable asymmetric organocatalyst has been synthesized in which the change of the position of the macrocycle reveals or conceals an acyclic, yet still highly effective, chiral organocatalytic group. This allows control over both the rate and stereochemical outcome of a catalyzed asymmetric Michael addition.
Design and synthesis of novel histone deacetylase inhibitor derived from nuclear localization signal peptide
Canzoneri, Joshua C.,Chen, Po C.,Oyelere, Adegboyega K.
supporting information; scheme or table, p. 6588 - 6590 (2010/06/12)
We describe herein the synthesis and characterization of a new class of histone deacetylase (HDAC) inhibitors derived from conjugation of a suberoylanilide hydroxamic acid-like aliphatic-hydroxamate pharmacophore to a nuclear localization signal peptide. We found that these conjugates inhibited the histone deacetylase activities of HDACs 1, 2, 6, and 8 in a manner similar to suberoylanilide hydroxamic acid (SAHA). Notably, compound 7b showed a threefold improvement in HDAC 1/2 inhibition, a threefold increase in HDAC 6 selectivity and a twofold increase in HDAC 8 selectivity when compared to SAHA.
