Abstract:
:The number of new chemical entities has remained rather constant (averaging 37 per year) in the past decade, despite the multiple-fold increase in the number of compounds that are being made and tested. Chemical space requires novel methods that can handle the increasing number of potentially accessible molecules. Neighborhood behavior, as an approach to similarity, and chemical property space navigation are some of the recent advances that are discussed, in the context of lead discovery and appropriate pharmacokinetic properties.
journal_name
Curr Opin Chem Bioljournal_title
Current opinion in chemical biologyauthors
Oprea TIdoi
10.1016/s1367-5931(02)00329-0subject
Has Abstractpub_date
2002-06-01 00:00:00pages
384-9issue
3eissn
1367-5931issn
1879-0402pii
S1367593102003290journal_volume
6pub_type
杂志文章,评审abstract::New catalysts and reaction conditions have been developed for the dynamic kinetic resolution or deracemisation of racemic mixtures of chiral compounds. Specific functional groups that lend themselves particularly well to this approach include chiral secondary alcohols, alpha-amino acids, amines and carboxylic acids. A...
journal_title:Current opinion in chemical biology
pub_type: 杂志文章,评审
doi:10.1016/j.cbpa.2004.02.001
更新日期:2004-04-01 00:00:00
abstract::Cellular communication drives diverse aspects of organismal biology ranging from immune function to memory formation. The mechanisms by which cells transact information in vivo, though, are not completely understood. This is due, in part, to a lack of tools for observing collections of cells in their native habitats. ...
journal_title:Current opinion in chemical biology
pub_type: 杂志文章,评审
doi:10.1016/j.cbpa.2014.11.006
更新日期:2015-02-01 00:00:00
abstract::Nanoparticle-based therapeutics have received increasing attention, as these systems can alleviate many drawbacks of conventional therapy. Metal-organic frameworks (MOFs), a new class of hybrid materials composed of metal ions and organic bridging ligands, have emerged as a promising platform for drug delivery, owing ...
journal_title:Current opinion in chemical biology
pub_type: 杂志文章,评审
doi:10.1016/j.cbpa.2009.12.012
更新日期:2010-04-01 00:00:00
abstract::Biosensors use biological elements to detect or quantify an analyte of interest. In bioprocessing, biosensors are employed to monitor key metabolites. There are two main types: fully biological systems or biological recognition coupled with physical/chemical detection. New developments in chemical biosensors include m...
journal_title:Current opinion in chemical biology
pub_type: 杂志文章,评审
doi:10.1016/j.cbpa.2017.05.014
更新日期:2017-10-01 00:00:00
abstract::Natural enzymes that catalyze Diels-Alder reactions have long been sought after, yet few enzymes have been experimentally confirmed to perform this reaction. In the past five years, several stand-alone enzymes that can catalyze the Diels-Alder reaction had been identified and characterized. Among which, the crystal st...
journal_title:Current opinion in chemical biology
pub_type: 杂志文章,评审
doi:10.1016/j.cbpa.2016.09.015
更新日期:2016-12-01 00:00:00
abstract::Recent advances in -omic profiling technologies have ushered in an era where we no longer want to merely measure the presence or absence of a biomolecule of interest, but instead hope to understand its function and interactions within larger signaling networks. Here, we review several emerging proteomic technologies c...
journal_title:Current opinion in chemical biology
pub_type: 杂志文章,评审
doi:10.1016/j.cbpa.2020.02.001
更新日期:2020-02-01 00:00:00
abstract::Great progress has been made in expanding the repertoire of genetically encoded fluorescent sensors for monitoring intracellular transition metals (TMs). This powerful toolkit permits dynamic and non-invasive detection of TMs with high spatial-temporal resolution, which enables us to better understand the roles of TM ...
journal_title:Current opinion in chemical biology
pub_type: 杂志文章,评审
doi:10.1016/j.cbpa.2017.12.002
更新日期:2018-04-01 00:00:00
abstract::Recently, the hypothesis that protein motions are involved in enzymatic turnover has gained significant attention. We review cases where there is evidence that protein motions are rate-limiting in the overall catalytic cycle and examine experimental and theoretical evidence for how such motions enhance the probability...
journal_title:Current opinion in chemical biology
pub_type: 杂志文章,评审
doi:10.1016/j.cbpa.2010.07.020
更新日期:2010-10-01 00:00:00
abstract::Protein cysteine residues are central to redox signaling and to protection against oxidative damage through their interactions with reactive oxygen and nitrogen species, and electrophiles. Although there is considerable evidence for a functional role for cysteine modifications, the identity and physiological significa...
journal_title:Current opinion in chemical biology
pub_type: 杂志文章,评审
doi:10.1016/j.cbpa.2010.11.003
更新日期:2011-02-01 00:00:00
abstract::Systems modeling is emerging as a valuable tool in therapeutics. This is seen by the increasing use of clinically relevant computational models and a rise in systems biology companies working with the pharmaceutical industry. Systems models have helped understand the effects of pharmacological intervention at receptor...
journal_title:Current opinion in chemical biology
pub_type: 杂志文章,评审
doi:10.1016/j.cbpa.2005.06.008
更新日期:2005-08-01 00:00:00
abstract::Protein citrullination is a post-translational modification of arginine that is catalyzed by the Protein Arginine Deiminase (PAD) family of enzymes. Aberrantly increased citrullination is associated with a host of inflammatory diseases and cancer and PAD inhibitors have shown remarkable efficacy in a range of diseases...
journal_title:Current opinion in chemical biology
pub_type: 杂志文章,评审
doi:10.1016/j.cbpa.2015.10.014
更新日期:2016-02-01 00:00:00
abstract::The reactive oxygen and nitrogen species superoxide ion, nitric oxide, nitrogen dioxide and peroxynitrite ion all react with biological target molecules. Some of these interactions are carefully orchestrated segments of signal transduction cascades or part of the armamentarium of the immune system, others are patholog...
journal_title:Current opinion in chemical biology
pub_type: 杂志文章,评审
doi:10.1016/S1367-5931(99)80036-2
更新日期:1999-04-01 00:00:00
abstract::Altered metabolite levels can drive epigenetic changes critical to development and disease. However, in many cases the specific protein-metabolite interactions that underlie this process remain enigmatic. In this review, we make the case that this fundamental missing information may be discovered by applying the tools...
journal_title:Current opinion in chemical biology
pub_type: 杂志文章,评审
doi:10.1016/j.cbpa.2019.02.002
更新日期:2019-08-01 00:00:00
abstract::Complex glycans participate in many essential life processes. Studies of glycan-mediated biological events have traditionally employed structurally defined fragments of the more elaborate natural molecules. However, it is now clear that this approach may sometimes be insufficient and this realization has prompted a de...
journal_title:Current opinion in chemical biology
pub_type: 杂志文章,评审
doi:10.1016/j.cbpa.2013.10.009
更新日期:2013-12-01 00:00:00
abstract::Aside from the demonstration that individual molecular traits of enzymes can be evolutionarily optimised, the discovery that several traits can be simultaneously optimised is a major advance. The first observations of the effects of evolutionary optimisation at the structural level, through X-ray crystallography, rein...
journal_title:Current opinion in chemical biology
pub_type: 杂志文章,评审
doi:10.1016/s1367-5931(00)00087-9
更新日期:2000-06-01 00:00:00
abstract::Single nucleotide polymorphism (SNP) genotyping has become a key technology for genetic studies. In recent years, matrix-assisted laser desorption/ionization (MALDI) time-of-flight mass spectrometry has emerged as a very powerful method for SNP genotyping. Here, we discuss our experience in implementing a high-through...
journal_title:Current opinion in chemical biology
pub_type: 杂志文章,评审
doi:10.1016/s1367-5931(01)00290-3
更新日期:2002-02-01 00:00:00
abstract::Inflammatory and autoimmune diseases, including rheumatoid arthritis, inflammatory bowel diseases, multiple sclerosis, psoriasis and asthma, provide drug discoverers with a tremendous challenge. The precise causes of these diseases are not known, but our understanding of the molecular and cellular mechanisms associate...
journal_title:Current opinion in chemical biology
pub_type: 杂志文章,评审
doi:10.1016/S1367-5931(99)80071-4
更新日期:1999-08-01 00:00:00
abstract::Functional amino acids that play critical roles in catalysis and regulation are known to display elevated nucleophilicity and can be selectively targeted for covalent modification by reactive electrophiles. Chemical-proteomic platforms, such as activity-based protein profiling (ABPP), exploit this reactivity by utiliz...
journal_title:Current opinion in chemical biology
pub_type: 杂志文章,评审
doi:10.1016/j.cbpa.2014.10.021
更新日期:2015-02-01 00:00:00
abstract::Before large, specific peptides could be made, in an RNA world our ancestors may have used an RNA-like molecule for both catalysis and information storage. Taken together, RNA activities suggest RNA could have performed most of the essential informational functions of an ancient organism (i.e. those functions most sim...
journal_title:Current opinion in chemical biology
pub_type: 杂志文章,评审
doi:10.1016/S1367-5931(99)80041-6
更新日期:1999-06-01 00:00:00
abstract::Although biotin and lipoic acid are two universally conserved cofactors essential for intermediary metabolism, their synthetic pathways have become known only in recent years. Both pathways have unusual features. Biotin synthesis in Escherichia coli requires a methylation that is later removed whereas lipoic acid is a...
journal_title:Current opinion in chemical biology
pub_type: 杂志文章,评审
doi:10.1016/j.cbpa.2018.08.004
更新日期:2018-12-01 00:00:00
abstract::The area of lipid molecular design is attracting widespread interest among numerous research groups worldwide. Diverse lipid assemblies in aqueous media, such as vesicles, bilayers and nanorods, offer new applications in chemical biology. Lipids with specifically tailored molecular architecture have been successfully ...
journal_title:Current opinion in chemical biology
pub_type: 杂志文章,评审
doi:10.1016/j.cbpa.2005.10.016
更新日期:2005-12-01 00:00:00
abstract::Fluorescence and reflectance spectroscopy provide the ability to assess tissue structure and metabolism in vivo in real time, providing improved diagnosis of pre-cancerous lesions. Reflectance spectroscopy can probe changes in epithelial nuclei that are important in pre-cancer detection, such as mean nuclear diameter,...
journal_title:Current opinion in chemical biology
pub_type: 杂志文章,评审
doi:10.1016/s1367-5931(02)00381-2
更新日期:2002-10-01 00:00:00
abstract::Peptide natural products (PNPs) represent a unique class of compounds known for their fascinating structural motifs with important biological activities. Lately, PNPs have garnered a lot of interest for their application in drug discovery. Nevertheless, lack of diversity oriented synthetic/biosynthetic platforms to ge...
journal_title:Current opinion in chemical biology
pub_type: 杂志文章,评审
doi:10.1016/j.cbpa.2016.06.006
更新日期:2016-10-01 00:00:00
abstract::Numerous developments in useful linkers are closely related with the advances in solid-phase organic synthesis. These linkers allow facile attachment functionalization and release molecules of interest. Designing a new anchoring group can be essential for synthesis success, especially for small molecules on solid supp...
journal_title:Current opinion in chemical biology
pub_type: 杂志文章,评审
doi:10.1016/j.cbpa.2004.04.004
更新日期:2004-06-01 00:00:00
abstract::A number of nitrile-related enzymes have been screened over the past year for use in synthetic applications. There have also been significant advances in our understanding of the structures and modes of regulation of metal-containing nitrile hydratases. Enzyme structural characterization has provided new insights into...
journal_title:Current opinion in chemical biology
pub_type: 杂志文章,评审
doi:10.1016/s1367-5931(99)00058-7
更新日期:2000-02-01 00:00:00
abstract::The notorious difficulty of elucidating structures of membrane transporters by crystallography has long prevented our understanding of active transport mechanism coupled with ion/proton transport. The determination of the first crystal structure of the drug/H+ antiporter AcrB was a breakthrough for structure-based und...
journal_title:Current opinion in chemical biology
pub_type: 杂志文章,评审
doi:10.1016/j.cbpa.2003.08.014
更新日期:2003-10-01 00:00:00
abstract::The range and diversity of solid-phase synthetic methodology continues to develop very rapidly, allowing the generation of previously inaccessible compound libraries. The design of such libraries requires consideration of linkage strategies, newly developed solid-phase reactions and emerging solution-phase processes. ...
journal_title:Current opinion in chemical biology
pub_type: 杂志文章,评审
doi:10.1016/S1367-5931(99)80046-5
更新日期:1999-06-01 00:00:00
abstract::In recent years, ogliopeptides have enjoyed ever increasing interest in two areas: first, approaches to biomimetic enzyme-like activity; and second, as metal-free catalysts for enantioselective transformations of synthetic interest. The discovery and optimization of peptides for these purposes has often used the metho...
journal_title:Current opinion in chemical biology
pub_type: 杂志文章,评审
doi:10.1016/s1367-5931(03)00065-6
更新日期:2003-06-01 00:00:00
abstract::Technological advances in the automation of parallel synthesis are following the model set by the semiconductor industry: miniaturization, increasing speed, lower costs. Recent work includes preparation of high-density reaction blocks, development of ink-jet dispensing to polypropylene sheets and synthesis inside cust...
journal_title:Current opinion in chemical biology
pub_type: 杂志文章,评审
doi:10.1016/s1367-5931(97)80110-x
更新日期:1997-06-01 00:00:00
abstract::Natural products containing a gamma-butyrolactone ring are abundant in nature; however, few general synthetic approaches to their stereoselective synthesis with broad structural variety are known. In this article, recent developments towards mono- and polycyclic gamma-butyrolactone natural products and analogs are dis...
journal_title:Current opinion in chemical biology
pub_type: 杂志文章,评审
doi:10.1016/j.cbpa.2005.03.005
更新日期:2005-06-01 00:00:00