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Cancers
Special Issues
Cancer Drug Discovery and Development: 2nd Edition
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Cancer Drug Discovery and Development: 2nd Edition

A special issue of Cancers (ISSN 2072-6694). This special issue belongs to the section "Cancer Drug Development".

Deadline for manuscript submissions: 31 March 2026 | Viewed by 1027

Special Issue Editor

Dr. Gary Piazza

E-Mail Website
Guest Editor
Department of Drug Discovery and Development, Harrison College of Pharmacy, Auburn University, Auburn, AL 36849, USA
Interests: RAS; β-catenin; phosphodiesterase; cGMP; cancer
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

We are excited to invite you to contribute to this Special Issue, which is the second edition of "Cancer Drug Discovery and Development" (https://www.mdpi.com/journal/cancers/special_issues/J9600YLLI6).

Cancer drug discovery is vital as it may lead to the development of effective treatments that specifically target cancer cells while minimizing harm to healthy cells. The discovery of new drugs offers hope for greater efficacy and potential in combating drug resistance.  

This Special Issue aims to collect original research articles or reviews relating to the discovery and development of novel anticancer drugs, including the identification or validation of novel molecular targets, drug design and development, strategies for enhancing or broadening the activity of immunotherapy, preclinical and clinical trials, and personalized medicine approaches. This Special Issue will highlight the latest research findings on molecular mechanisms underlying cancer progression and present innovative strategies to target specific cancer types or pathways or to combat resistance. Studies on the role of emerging technologies in accelerating the drug discovery process, such as artificial intelligence and high-throughput screening, are also welcome.

We hope that cancer research experts from around the world will share their knowledge and insights into cancer drug discovery and development. This Special Issue will also provide a platform for discussing the challenges faced in drug resistance and toxicity and the need for more efficient drug delivery systems for cancer treatment, as well as for exploring potential solutions and future directions for cancer research.

Dr. Gary Piazza
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 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. Cancers is an international peer-reviewed open access semimonthly 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 2900 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.

Keywords

  • signal transduction inhibitors
  • small-molecule inhibitors
  • antibodies
  • PROTOC
  • immunotherapy
  • medicinal chemistry
  • chemical optimization
  • high-throughput screening

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Further information on MDPI's Special Issue policies can be found here.

Published Papers (2 papers)

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16 pages, 34747 KB  
Article
Evaluation of a Novel Pan-RAS Inhibitor in 3D Bioprinted Tumor Models
by Daniela D. De Nobrega, Logan C. Eiler, Parmanand Ahirwar, Sonika Nallapu, Urvi P. Rawal, Chelsea L. Crawford, Donald J. Buchsbaum, Adam B. Keeton, Yulia Y. Maxuitenko, Xi Chen, Gary A. Piazza, Allan Tsung and Karim I. Budhwani
Cancers 2025, 17(18), 2958; https://doi.org/10.3390/cancers17182958 - 10 Sep 2025
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Abstract
Background: Colorectal cancer (CRC) remains a significant global health burden, with KRAS mutations driving ~40% of cases. The efficacy of recently approved, mutant-specific KRAS inhibitors is limited by mutational status as well as intrinsic and adaptive resistance mechanisms. Pan-RAS inhibitors, such as [...] Read more.
Background: Colorectal cancer (CRC) remains a significant global health burden, with KRAS mutations driving ~40% of cases. The efficacy of recently approved, mutant-specific KRAS inhibitors is limited by mutational status as well as intrinsic and adaptive resistance mechanisms. Pan-RAS inhibitors, such as ADT-007, offer broader therapeutic potential by targeting multiple RAS isoforms. Here, we evaluate ADT-007 in 3D bioprinted ex vivo slice tissue (BEST) generated from KRAS-mutant and RAS wild-type (WT) CRC cell lines. Methods: Potency and selectivity of ADT-007 were benchmarked against bortezomib (proteasome inhibitor) and YM155 (survivin inhibitor) using high-content imaging and ATP-based luminescence assays. Apoptosis induction was assessed with Annexin V/propidium iodide and flow cytometry. Results: ADT-007 exhibited high potency and selectivity in KRAS-mutant BEST, reducing tumor burdens >30% at nanomolar concentrations, and demonstrated superior selectivity with minimal cytotoxicity in WT RAS BEST. Annexin V staining confirmed selective induction of apoptosis in KRAS-mutant cells. Conclusions: The selective potency and specificity of ADT-007 warrant further investigation of pan-RAS inhibitors for treating RAS-driven cancers. This study also underscores the translational utility of 3D BEST models for preclinical drug response assessment. Further validation in patient-derived BEST is necessary to evaluate the potential of ADT-007 in clinical settings. Full article
(This article belongs to the Special Issue Cancer Drug Discovery and Development: 2nd Edition)
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Review

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18 pages, 1533 KB  
Review
Regulators of Cancer Progression: Succinylation
by Jie Gao and Wei Yu
Cancers 2025, 17(16), 2652; https://doi.org/10.3390/cancers17162652 - 14 Aug 2025
Viewed by 624
Abstract
Lysine succinylation is a recently discovered post-translational protein modification, the process of which requires the participation of various enzymes. The close association between cancer and protein post-translational modifications (PTMs), such as acetylation and phosphorylation, has been extensively investigated and well-established. In recent years, [...] Read more.
Lysine succinylation is a recently discovered post-translational protein modification, the process of which requires the participation of various enzymes. The close association between cancer and protein post-translational modifications (PTMs), such as acetylation and phosphorylation, has been extensively investigated and well-established. In recent years, growing attention has been directed toward the role of succinylation in cancer progression. Accumulating evidence demonstrates that protein succinylation and desuccinylation play critical roles in promoting the development of various cancers, including lung, prostate, and renal cancers. Notably, the primary substrates undergoing succinylation are non-histone proteins. Therefore, elucidating the functions of cancer-related succinylated proteins is essential for identifying novel therapeutic targets. This review comprehensively summarizes current research advances regarding protein succinylation in common cancers and discusses the progress in developing succinylation-targeting drugs. Specifically, we focus on the molecular mechanisms by which succinylation regulates cancer progression, along with the identification of key succinylation sites. Our discussion aims to provide valuable insights for future research and the development of innovative cancer treatments. Full article
(This article belongs to the Special Issue Cancer Drug Discovery and Development: 2nd Edition)
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