Students' active engagement is one of the most critical challenges to any successful learning environment. The blending of active engagement along with rich, meaningful content is necessary for chemical educators to re-examine the purpose of the chemistry classroom. The Spring 2014 ConfChem conference, Flipped Classroom, was held from May 9 to June 12, 2014, and contained eight papers and a poster session discussing a variety of ways to engage students within a flipped learning approach to the classroom. This communication introduces the conference, suggests that the flipped classroom is a growing trend, and invites readers to engage in further discussions on how technology can be leveraged to transform the face-to-face practice with our students. The Spring 2014 ConfChem conference was hosted by the ACS DivCHED Committee on Computers in Chemical Education (CCCE).
Treatment of an electron-rich benzyl ether with DDQ at ambient temperature followed by addition of a silyl enol ether undergoes a C-C bond-forming reaction to afford 3-alkoxy-3-phenyl-propionyl compound. This is a general reaction and works well with a variety of silyl enol ethers to give carbonyl products in yields ranging from 10 to 85%.
Abby is a doctoral student in the Learning Sciences program at Clemson University. Broadly, her research interests include intergenerational learning in informal settings, self-directed learning, and cultural influences on the learning process. Abby currently works as a graduate assistant for the General Engineering Learning Community (GELC), a program that supports first-year engineering students in their development of self-regulation and time management skills, effective learning strategies, and positive habits of mind.
To create ligands for the estrogen receptor that contain pendant groups for tethering to a poly(amido) amine (PAMAM) dendrimer, we have explored a class of N-substituted 2-phenyl indoles. Attachment of tethers of different length and chemical nature to this non-steroidal indole scaffold gave high affinity ligand-tether conjugates that can be easily functionalized. To further explore the utility of this system, an indole-conjugated dendrimer was prepared and evaluated as an estrogen receptor ligand.The estrogen receptor (ER) is a member of the nuclear hormone receptor superfamily of ligandregulated transcription factors. The ER is regulated primarily by the endogenous estrogen, estradiol (E2, Figure 1), but it is also the target of pharmaceutical agents, including estrogen agonists, antagonists, and selective estrogen receptor modulators (SERMs) that activate the subtypes ERα and ERβ. 1 The binding of E2 or other agonists to ER results in conformational changes that affect its ability to recruit coactivators or corepressors and controls ER interaction with DNA-regulatory sequences, termed estrogen response elements. 2In addition to its nuclear role to regulate gene transcription, ER can also have non-genomic actions by directly activating kinase cascades. These non-genomic effects are more rapid than the transcriptional ones and are mediated through ER from membrane or other extranuclear sites, where it acts as a classical activator of signal transduction. 3 Extranuclear ER is most likely the same protein as nuclear ER, yet it represents only a few percent of total cellular ER, so rigorous characterization of membrane ER has been difficult.Estrogens conjugated to poly(amido)amine (PAMAM) dendrimers have been used to study the non-genomic, extranuclear effects of the estrogen receptor. 4,5 We have found that when an estrogen is conjugated to the highly charged, abiotic PAMAM macromolecule, this estrogen-dendrimer conjugate remains outside of the nucleus, allowing the ligand to activate signaling of only non-nuclear, non-genomic pathways.PAMAMs are available in a number of generations that correspond to progressively increasing molecular weights and surface functionalities. PAMAMs contain multiple surface amine substituents onto which ligands can be covalently attached. Generation-6 PAMAM has a nominal molecular weight of 58 kDa, similar to bovine serum albumin, which has been used as an estradiol carrier 6 ; the dendrimer also has nominally 256 surface primary amines. A distinct advantage of a PAMAM over a protein as a macromolecule for hormone conjugation is that the PAMAM can withstand organic solvents and extraction protocols needed to remove any remaining free ligand, which can confound biological experiments. 4-6 NIH-PA Author ManuscriptNIH-PA Author Manuscript NIH-PA Author ManuscriptProduction of ER ligand-macromolecule conjugates involves four design steps: (I) identifying a good ligand scaffold with a position for covalent attachment of the tether, (II) determining an optimal tether length and ch...
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