Special Issue "Reagents and Methods for Protein Target Identification"
A special issue of Molecules (ISSN 1420-3049).
Deadline for manuscript submissions: closed (31 July 2013)
Dr. Nicholas James Westwood
School of Chemistry, University of St Andrews, North Haugh, St Andrews, KY16 9ST, UK
Interests: chemical biology; natural product synthesis
Two main factors are driving the resurgence in the use of protein target identification strategies. First, there is an increased interest in the identification of off-target effects of know drugs and second, improvements in phenotypic screening methods have led to a significant increase in the number of compounds that have been assigned as inducing an important biological phenotype through an unknown mechanism. In both cases, researchers at the chemistry-biology interface have been revisiting and in many cases inventing strategies to identify and subsequently validated protein targets. A number of target identification strategies use genomic and proteomic techniques. Typically these approaches, including the selection of resistant mutants followed by full genome sequencing, do not require the chemical synthesis of specific reagents. In other approaches, however, the preparation of specific reagents (radiolabeled, photoaffinity labelled, tagged etc) is essential. Structure activity relationship studies are also required to inform reagent synthesis programmes. Once the reagent has been prepared a range of methods for using it can then be envisaged. Overall, target identification is testing the creativity and skills of chemical biologists to the limit. In this special issue of Molecules, we aim to bring together papers that cover all aspects of the protein target identification challenge.
Dr. Nicholas James Westwood
Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. Papers will be published continuously (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.
Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are refereed through a peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Molecules is an international peer-reviewed Open Access monthly journal published by MDPI.
- protein target identification
- reagent synthesis
- affinity chromatography
- photoaffinity labelling
- off target effects
- genome-wide approaches
- proteomic approaches
- chemical proteomics
- forward chemical genetics
- protein target validation
Article: Distinct Metabolites for Photoreactive l-Phenylalanine Derivatives in Klebsiella sp. CK6 Isolated from Rhizosphere of a Wild Dipterocarp Sapling
Molecules 2013, 18(7), 8393-8401; doi:10.3390/molecules18078393
Received: 14 June 2013; in revised form: 2 July 2013 / Accepted: 11 July 2013 / Published: 16 July 2013| Cited by 1 | PDF Full-text (244 KB)
Article: Combination of Small Molecule Microarray and Confocal Microscopy Techniques for Live Cell Staining Fluorescent Dye Discovery
Molecules 2013, 18(8), 9999-10013; doi:10.3390/molecules18089999
Received: 26 June 2013; in revised form: 13 August 2013 / Accepted: 14 August 2013 / Published: 20 August 2013| PDF Full-text (4706 KB)
Molecules 2013, 18(9), 10425-10451; doi:10.3390/molecules180910425
Received: 30 July 2013; in revised form: 23 August 2013 / Accepted: 23 August 2013 / Published: 29 August 2013| Cited by 3 | PDF Full-text (1586 KB)
Article: A Modular Approach to Triazole-Containing Chemical Inducers of Dimerisation for Yeast Three-Hybrid Screening
Molecules 2013, 18(9), 11639-11657; doi:10.3390/molecules180911639
Received: 1 August 2013; in revised form: 5 September 2013 / Accepted: 6 September 2013 / Published: 23 September 2013| Cited by 1 | PDF Full-text (1196 KB) | Supplementary Files
Communication: Design and Synthesis of a Biotinylated Chemical Probe for Detecting the Molecular Targets of an Inhibitor of the Production of the Pseudomonas aeruginosa Virulence Factor Pyocyanin
Molecules 2013, 18(10), 11783-11796; doi:10.3390/molecules181011783
Received: 5 August 2013; in revised form: 9 September 2013 / Accepted: 17 September 2013 / Published: 25 September 2013| PDF Full-text (279 KB)
Molecules 2013, 18(11), 13831-13859; doi:10.3390/molecules181113831
Received: 20 August 2013; in revised form: 22 October 2013 / Accepted: 4 November 2013 / Published: 8 November 2013| PDF Full-text (1974 KB)
Molecules 2014, 19(2), 2135-2165; doi:10.3390/molecules19022135
Received: 6 September 2013; in revised form: 16 January 2014 / Accepted: 1 February 2014 / Published: 18 February 2014| PDF Full-text (432 KB) | HTML Full-text | XML Full-text
The below list represents only planned manuscripts. Some of these manuscripts have not been received by the Editorial Office yet. Papers submitted to MDPI journals are subject to peer-review.
Title: Radiolabeling Strategies for Tumor targeting Proteinaqueos Drugs
Authors: Max Sauter, Uwe Haberkorn and Walter Mier
Affiliations: University Hospital Heidelberg, Department of Nuclear Medicine, 69120 Heidelberg, Germany
Abstract: Owing to their large size proteinaceous drugs offer higher in operative information content compared to the small molecules that correspond to the traditional understanding of druglikeness. As a consequence these drugs allow developing patient-specific therapies that provide the means to go beyond the possibilities of current drug therapy. However, the efficacy of these strategies, in particular "personalized medicine" depends on precise information about individual target expression rates. Molecular imaging combines non-invasive imaging methods with tools of molecular and cellular biology and thus bridges current knowledge to the clinical use. Moreover, nuclear medicine techniques exploit this potential by allowing therapeutic applications with tracers that behave like the diagnostic tracer. The advantages of radioiodination, still the most versatile radiolabeling strategy and other labeled compounds comprising covalently attached radioisotopes are compared to the use of chelator-protein conjugates that are complexed with metallic radioisotopes. With the techniques use radioactive isotopes as reporting unit or even the therapeutic principle, care has to be taken to avoid cleavage of the radionuclide from the protein it is linked to and the tracers used in molecular imaging require labeling techniques that provide site specific conjugation and metabolic stability. Appropriate choice of the radionuclide allows tailoring the properties of the labeled protein to the application required. Until the event of positron emission tomography the spectrum of nuclides used to visualize cellular and biochemical processes was largely restricted to iodine isotopes and 99m-technetium. Today, several nuclides such as 18-fluorine, 68-gallium and 86-yttrium have fundamentally extended the possibilities of tracer design and in turn caused the need for the development of chemical methods for their conjugation.
Last update: 26 March 2013