Calixarene-mediated liquid membrane transport of choline conjugates 2: Transport of drug-choline conjugates and neurotransmitters
Lower rim carboxylic acid calix[n]arenes and upper rim phosphonic acid functionalized calix[4]arenes effect selective transport of distinct molecular payloads through a liquid membrane. The secret to this success lies in the attachment of a receptor-complementary handle. We find that the trimethylammonium ethylene group present in choline is a general handle for the transport of drug and drug-like species. Furthermore, neurotransmitters possessing ionizable amine termini are also transported. Some limitations to this strategy have been uncovered as payloads become increasingly lipophilic. These developments reveal new approaches to synthetic receptor-mediated selective small molecule transport in vesicular and cellular systems. Ammonium species emerge as general and potent handles for effecting drug transport as mediated by ionizable calixarenes. Trimethylammonium, ammonium and ammonium carboxylates work in conjunction with phosphonic acid and carboxylic acid functionalized calix[n]arenes.
Adhikari, Birendra Babu,Roshandel, Sahar,Fujii, Ayu,Schramm, Michael P.
supporting information
p. 2683 - 2690
(2015/04/27)
Genomic action of permanently charged tamoxifen derivatives via estrogen receptor-α
Tamoxifen is a selective estrogen receptor modulator widely used in oncology and reproductive endocrinology. In order to decrease its non-desirable effects and elucidate mechanisms of action, permanently charged tamoxifen derivatives (PCTDs) have been rep
Rivera-Guevara, Claudia,Perez-Alvarez, Victor,Garcia-Becerra, Rocio,Ordaz-Rosado, David,Morales-Rios, Martha Sonia,Hernandez-Gallegos, Elizabeth,Cooney, Austin J.,Bravo-Gomez, Maria Elena,Larrea, Fernando,Camacho, Javier
experimental part
p. 5593 - 5601
(2010/10/01)
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