Small Molecule Inhibitors as Anticancer Drugs: Advances and Challenges
A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".
Deadline for manuscript submissions: closed (30 June 2023) | Viewed by 17987
Special Issue Editors
Interests: medicinal chemistry; drug design; peptide chemistry; peptidomimetics; small molecules; structure–activity relationships studies; cysteine protease inhibitors; neurotensin analogues
Special Issues, Collections and Topics in MDPI journals
Interests: medicinal chemistry; drug design; peptidomimetics, small molecules; structure–activity relationships studies; cysteine protease inhibitors; proteasome inhibitors
Special Issue Information
Dear Colleagues，
Chemotherapy was for a long time the first choice for cancer treatment, along with surgery and radiotherapy. Chemotherapeutic drugs kill tumor cells, but their inability to distinguish cancer and non-cancerous cells results in relevant adverse effects. At the beginning of the new millennium, great efforts made by scientists led to the approval of Imatinib, which could be considered the first small molecule with targeted anticancer activity. Compared to the outdated anticancer therapies, small molecule targeted drugs can selectively target tumor cells with limited toxicity. Over the last 20 years, about 90 anti-cancer small molecules have been approved around the world, and an increasing number of candidates are in clinical trials. Among the possible strategies, the inhibition of protein kinases, both receptor and non-receptor kinases, proteasome, poly (ADP-ribose) polymerases (PARPs), and B-cell lymphoma 2 (BCL-2) proteins, as well as the modulation of epigenetic and hedgehog pathways, represent valid and precious approaches for the development of targeted drugs. Despite the promising advances in cancer therapy, the small-molecule targeted cancer-fighting drugs still face challenges that limit the successful treatment. Drug resistance and low efficacy are the main limiting factors affecting most cancer patients. Several cellular and molecular paradigms influence the drug resistance onset, meanwhile, the efficacy of targeted anti-cancer drugs is restricted in a limited number of patients, mainly due to mutations and gene rearrangements. However, different strategies to overcome these issues were carried-out: the discovery of new anti-cancer targets, the use of small molecules in combination therapies, the antibody-drug conjugates, and the PROTAC technology could significantly improve the cancer treatment.
This Special Issue aims to collect reviews and research articles concerning small molecule-drugs in targeted cancer therapy. The rational analysis of the obtained findings so far and new investigation studies could provide precious information for the research and development of small molecules with targeted anticancer activity.
Dr. Santo Previti
Prof. Dr. Maria Zappalà
Guest Editors
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Keywords
- anticancer
- small molecules
- targeted anticancer therapy
- drug resistance
- protein kinases
- epigenetic
- proteasome
- PROTAC
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