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Molecular Biology of Protein Kinases: Regulatory Mechanisms, Therapeutic Targets and Cancer Treatments

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Molecular Biology".

Deadline for manuscript submissions: 20 February 2025 | Viewed by 1684

Special Issue Editor

Dr. Jaw Ji Yang

E-Mail Website
Guest Editor
Department of Stomatology, Chung Shan Medical University Hospital, Taichung 40201, Taiwan
Interests: protein kinases; cancer therapeutics; molecular mechanisms of disease; ribosomal translation regulation; kinase inhibitors; signal transduction pathways; targeted cancer therapy; phage display technology; peptide regulators; translational oncology

Special Issue Information

Dear Colleagues,

This Special Issue, titled “Molecular Biology of Protein Kinases: Regulatory Mechanisms, Therapeutic Targets and Cancer Treatments”, aims to present research on the pivotal roles played by protein kinases in both physiological and pathological contexts. As key regulators within cellular signaling cascades, protein kinases facilitate crucial biological functions, such as cell growth, differentiation, and programmed cell death, in addition to modulating responses to environmental cues. The aberrant regulation of these enzymes is frequently associated with the development of a wide array of diseases, with cancer being a primary focus due to the critical role played by kinases in tumor genesis and progression. We call for submissions that explore the complex molecular biology of protein kinases, shedding light on how they are regulated, introducing new targets for therapy, and promoting the creation of innovative kinase inhibitors. Contributions may extend from the fundamental aspects of kinase research, including biochemistry and structural analysis, to application-driven studies aiming to connect kinase pathways for therapy.

Dr. Jaw Ji Yang
Guest Editor

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 submissions that pass pre-check are 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. International Journal of Molecular Sciences is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. There is an Article Processing Charge (APC) for publication in this open access journal. For details about the APC please see here. 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.

Keywords

  • protein kinases
  • signal transduction
  • cancer therapy
  • regulatory mechanisms
  • kinase inhibitors
  • therapeutic targets
  • molecular biology
  • structural biology
  • translational research
  • clinical applications

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Published Papers (2 papers)

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Review

22 pages, 2639 KiB  
Review
Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors in Cancer: Current Use and Future Prospects
by Henry Dickerson, Ahmad Diab and Othman Al Musaimi
Int. J. Mol. Sci. 2024, 25(18), 10008; https://doi.org/10.3390/ijms251810008 - 17 Sep 2024
Viewed by 290
Abstract
Tyrosine kinase inhibitors (TKIs) have emerged as a leading targeted cancer therapy, reducing the side effects often seen with non-targeted treatments, especially the damage to healthy cells. To tackle resistance, typically caused by epidermal growth factor receptor (EGFR) mutations, four generations of TKIs [...] Read more.
Tyrosine kinase inhibitors (TKIs) have emerged as a leading targeted cancer therapy, reducing the side effects often seen with non-targeted treatments, especially the damage to healthy cells. To tackle resistance, typically caused by epidermal growth factor receptor (EGFR) mutations, four generations of TKIs have been developed. Each generation has shown improved effectiveness and fewer side effects, resulting in better patient outcomes. For example, patients on gefitinib, a first-generation TKI, experienced a progression-free survival (PFS) of 10 months compared to 5 months with conventional chemotherapy. Second-generation TKI afatinib outperformed erlotinib and extended PFS to 11.1 months compared to 6.9 months with cisplatin. Third-generation TKIs further increased survival to 38.6 months, compared to 31.8 months with first-generation TKIs. This progress demonstrates the ability of newer TKIs to overcome resistance, particularly the T790M mutation, while reducing adverse effects. Ongoing research focuses on overcoming resistance from newer mutations like C797S to further improve patient survival. These developments highlight the significant progress in TKI therapy and the continued effort to refine cancer treatment. Recent research in South Korea shows that third-generation TKIs are ineffective against non-small cell lung cancer (NSCLC) with the C797S mutation. Several trials have started showing promising in vitro and in vivo results, but more trials are needed before clinical approval. This review underscores notable advancements in the field of EGFR TKIs, offering a comprehensive analysis of their mechanisms of action and the progression of various TKI generations in response to resistance. Full article
(This article belongs to the Special Issue Molecular Biology of Protein Kinases: Regulatory Mechanisms, Therapeutic Targets and Cancer Treatments)
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11 pages, 964 KiB  
Review
PKIB, a Novel Target for Cancer Therapy
by Anna Musket, Jonathan P. Moorman, Jinyu Zhang and Yong Jiang
Int. J. Mol. Sci. 2024, 25(9), 4664; https://doi.org/10.3390/ijms25094664 - 25 Apr 2024
Viewed by 1060
Abstract
The serine-threonine kinase protein kinase A (PKA) is a cyclic AMP (cAMP)-dependent intracellular protein with multiple roles in cellular biology including metabolic and transcription regulation functions. The cAMP-dependent protein kinase inhibitor β (PKIB) is one of three known endogenous protein kinase inhibitors of [...] Read more.
The serine-threonine kinase protein kinase A (PKA) is a cyclic AMP (cAMP)-dependent intracellular protein with multiple roles in cellular biology including metabolic and transcription regulation functions. The cAMP-dependent protein kinase inhibitor β (PKIB) is one of three known endogenous protein kinase inhibitors of PKA. The role of PKIB is not yet fully understood. Hormonal signaling is correlated with increased PKIB expression through genetic regulation, and increasing PKIB expression is associated with decreased cancer patient prognosis. Additionally, PKIB impacts cancer cell behavior through two mechanisms; the first is the nuclear modulation of transcriptional activation and the second is the regulation of oncogenic AKT signaling. The limited research into PKIB indicates the oncogenic potential of PKIB in various cancers. However, some studies suggest a role of PKIB in non-cancerous disease states. This review aims to summarize the current literature and background of PKIB regarding cancer and related issues. In particular, we will focus on cancer development and therapeutic possibilities, which are of paramount interest in PKIB oncology research. Full article
(This article belongs to the Special Issue Molecular Biology of Protein Kinases: Regulatory Mechanisms, Therapeutic Targets and Cancer Treatments)
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