In the originally published version of this article, Daniel Geiszler's last name was misspelled. This error has now been corrected in the article online.
The 973 Program is China's keystone national research program established to support basic research in natural and physical sciences. In addition to promoting the development of core technology and scientific infrastructure needed to enable China to meet the social and economic challenges of the 21st century, the training and mentoring of the new generation of China's young scientists are also important objectives of this national program. The green chemical pesticide research program is a part of the 973 Program. The main objectives of stage 1 of the green chemical pesticide research program (2003-2008) are to establish China's capability to conduct basic research in the discovery of "green" crop protection chemicals that are not only novel in mode of action and highly selective to pest species that are unique to China's agricultural situation but also possess favorable environmental and human hazard and risk potentials. The target-based discovery strategy was selected as the main discovery platform. This strategy not only provided this research program the best chance to discover new products but also provided members of this research team opportunities to establish core technologies in chemoinformatics/computation-aided pesticide design using QSAR, QAAR, sensitive and selective bioassay methodology, combinatorial synthesis, hit to lead optimization, and biological targets that were derived from resistance-AChE, IGR, nAChR, etc. On the basis of the learning from stage 1, stage 2 (2010-2014) of this program will focus on the molecular target-oriented innovation of green chemical pesticides. This commentary presents key learnings and accomplishments from the stage 1 of China's green chemical pesticide research program. It is hoped that this information will stimulate further constructive collaborations between pesticide scientists from China and abroad.
Inorganic nanoparticles (NPs) are promising drug delivery carriers owing to their high drug loading efficiency, scalable preparation, facile functionalization, and chemical/thermal stability. However, the clinical translation of inorganic nanocarriers is often hindered by their poor biodegradability and lack of controlled pH response. Herein, a fully degradable and pH-responsive DOX@ACC/PAA NP (pH 7.4-5.6) is developed by encapsulating doxorubicin (DOX) in poly(acrylic acid) (PAA) stabilized amorphous calcium carbonate (ACC) NPs. The DOX-loaded NPs have small sizes (62 ± 10 nm), good serum stability, high drug encapsulation efficiency (>80%), and loading capacity (>9%). By doping proper amounts of Sr 2+ or Mg 2+ , the drug release of NPs can be further modulated to higher pH responsive ranges (pH 7.7-6.0), which enables drug delivery to the specific cell domains of tissues with a less acidic microenvironment. Tumor inhibition and lower drug acute toxicity are further confirmed via intracellular uptake tests and zebrafish models, and the particles also improve pharmacokinetics and drug accumulation in mouse xenograft tumors, leading to enhanced suppression of tumor growth. Owing to the excellent biocompatibility, biodegradability, and tunable drug release behavior, the present hybrid nanocarrier may find broad applications in tumor therapy.
A novel and efficient method for the synthesis of (Z)-fluorinated alkenylboronic acid pinacol esters via Cu-catalyzed stereoselective borylation of gem-difluoroalkenes using bis(pinacolato)diboron (Bpin) as the boron source with the assistance of NaOtBu and Xantphos at room temperature was developed.
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