Cancer remains a major cause of mortality. However, significant progress has been made in understanding the molecular basis of the disease. Cancer is a multigenic and multicellular disease characterized by a multifactorial etiology, which initiates uncontrolled cell growth. The major problem associated with current cancer treatment regimens is the development of resistance to therapy, which may arise due to several reasons, such as the overexpression of anti-apoptotic proteins, mutations in key signaling molecules, overexpression of drug ef?ux pumps or the presence of dormant and/or resistant tumor cells. Most of the anticancer drugs in clinical use are based on the principle of 'one molecule - one target - one malady'. However, multifactorial diseases such as cancer, may greatly benefit from therapies simultaneously hitting multiple key pathways and/or their pathogenic cross-talk.
The design strategy for Multi-target-directed ligands (MTDLs) involves the incorporation of two or more distinct pharmacophores of different drugs in a single structure to develop hybrid molecules. MTDLs are simultaneously able to bind/inhibit two or more targets at a time, thus boosting the compound's therapeutic potential via a polypharmacological approach. Modern drug discovery has the power to identify potential multifunctional modulators for biologically and clinically validated targets among millions of compounds. The design of MTDLs is an essential and promising research area since recent research confirmed the potential therapeutic benefit for the management/treatment of complex multifactorial diseases. Despite the significant amount of drug discoveries in the vast field of cancer therapy, there is still an urgent need for novel and innovative treatments. The MTDLs approach holds great potential in cancer therapy since it may significantly simplify treatment regimens with respect to standard combination therapy, reducing the risk of possible drug-drug interactions, and, most importantly, limiting the insurgence of resistance.
With this Research Topic, we wish to further stimulate the design and development of novel MTDLs as effective anticancer agents with the potential to turn into promising clinical candidates. We welcome especially submissions with a strong focus on drug discovery such as multitarget modulators or protacs applying modern drug design methods to get first insights into the mechanism of action from an interdisciplinary point of view.
Subtopics
· Strategies for anticancer drug development
· Multi-target Directed Ligands as effective anticancer agents
· Design and Structure-activity relationship studies of MTDLs
· Cancer as a multigenic disease state
· Hot targets for anticancer drug development
Please note: manuscripts consisting solely of bioinformatics or computational analysis of public genomic or transcriptomic databases which are not accompanied by validation (independent cohort or biological validation in vitro or in vivo) are out of scope for this section and will not be accepted as part of this Research Topic.
Cancer remains a major cause of mortality. However, significant progress has been made in understanding the molecular basis of the disease. Cancer is a multigenic and multicellular disease characterized by a multifactorial etiology, which initiates uncontrolled cell growth. The major problem associated with current cancer treatment regimens is the development of resistance to therapy, which may arise due to several reasons, such as the overexpression of anti-apoptotic proteins, mutations in key signaling molecules, overexpression of drug ef?ux pumps or the presence of dormant and/or resistant tumor cells. Most of the anticancer drugs in clinical use are based on the principle of 'one molecule - one target - one malady'. However, multifactorial diseases such as cancer, may greatly benefit from therapies simultaneously hitting multiple key pathways and/or their pathogenic cross-talk.
The design strategy for Multi-target-directed ligands (MTDLs) involves the incorporation of two or more distinct pharmacophores of different drugs in a single structure to develop hybrid molecules. MTDLs are simultaneously able to bind/inhibit two or more targets at a time, thus boosting the compound's therapeutic potential via a polypharmacological approach. Modern drug discovery has the power to identify potential multifunctional modulators for biologically and clinically validated targets among millions of compounds. The design of MTDLs is an essential and promising research area since recent research confirmed the potential therapeutic benefit for the management/treatment of complex multifactorial diseases. Despite the significant amount of drug discoveries in the vast field of cancer therapy, there is still an urgent need for novel and innovative treatments. The MTDLs approach holds great potential in cancer therapy since it may significantly simplify treatment regimens with respect to standard combination therapy, reducing the risk of possible drug-drug interactions, and, most importantly, limiting the insurgence of resistance.
With this Research Topic, we wish to further stimulate the design and development of novel MTDLs as effective anticancer agents with the potential to turn into promising clinical candidates. We welcome especially submissions with a strong focus on drug discovery such as multitarget modulators or protacs applying modern drug design methods to get first insights into the mechanism of action from an interdisciplinary point of view.
Subtopics
· Strategies for anticancer drug development
· Multi-target Directed Ligands as effective anticancer agents
· Design and Structure-activity relationship studies of MTDLs
· Cancer as a multigenic disease state
· Hot targets for anticancer drug development
Please note: manuscripts consisting solely of bioinformatics or computational analysis of public genomic or transcriptomic databases which are not accompanied by validation (independent cohort or biological validation in vitro or in vivo) are out of scope for this section and will not be accepted as part of this Research Topic.