Special Issue "Kinase Inhibitors II"
Deadline for manuscript submissions: 28 February 2019
Since the discovery of protein phosphorylation as a post-translational modification in glycogen metabolism in the1960s, protein kinases (PK) and their opponents, phosphatases, have been crucial to many scientists. Approximately 2% of the human genome encodes for PKs, named the human “kinome”, consisting of 518 PKs and their splice variants. PKs typically use ATP for γ-phosphor-transfer reactions for OH-functions of serine, threonine, or tyrosine residues in proteins. In fact, the relatively simple attachment of a phosphate moiety induces critical conformational and functional changes of the substrate protein. Due to the powerful nature of protein modification involved in key cellular processes, such as signal transduction, cell cycle, metabolism, differentiation, and cell survival, PKs have to be strictly regulated in a physiological context. In contrast, their dysregulation leads to severe diseases, including cancer. In line with this notion, the first proto-oncogene c-SRC was identified as a non-receptor tyrosine kinase in 1978.
Today, PKs are validated and widely accepted targets for drug discovery, triggered significantly by the clinical success of imatinib in 2001. Thus far, more than 40 drugs have been FDA-approved and are on the market. The majority of compounds address tyrosine kinases, with their main therapeutical applications being cancer and inflammation. In addition to massive commercial drug discovery programs for the development of kinase inhibitors, academia has contributed a solid part to today´s knowledge on PK and their inhibitors. A wealth of biological studies towards the validation of PKs as drug targets, hit-compounds, lead structures, pharmacological tools, and ligand–protein complexes for the development of novel PK inhibitors are reported in literature. The topics cover various scientific areas, including molecular biology, biological and medicinal chemistry, and clinical applications.
This Special Issue of Molecules will focus on the exciting area of protein kinases and novel approaches in PK drug discovery.
Prof. Dr. Christian Peifer
Manuscript Submission Information
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. All papers will be peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short 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 thoroughly refereed through a single-blind 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.
Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 1800 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.
- protein phosphorylation
- signal transduction
- small molecule kinase inhibitors (smKI)
- receptor tyrosine kinases
- serin-threonine kinases
- Type I-VI
- ATP competitive/alosteric/covalent inhibition
- kinome-screening selectivity
- 518 human protein kinases
- in-vitro activity/in-vivo efficacy
- mutated kinases,
- rational structure- based design
- medicinal chemistry/drug discovery
- targeted therapy
- personalized medicine