Abstract
The macrocycles representing a unique chemical structure bridging conventional small molecules and large biomolecules, have attracted more and more attention in drug discovery over the past decade, and tremendous progress has been made toward the macrocyclization synthesis and structure diversification recently. Because of their favored size, flexibility and complexity, macrocycles can engage previously undruggable targets through numerous and spatially distributed binding interactions, and offer many privileged features including high potency, prominent selectivity, as well as favorable pharmacokinetics properties, and unique intellectual property(IP) space, and even safety profiles, etc. Currently around 70 macrocyclic molecules have been approved for clinical therapy, over 76 macrocycles are being evaluated in clinical trials from phase I to phase III. It is believed that the macrocycles will play more and more important role in the future, and provide very distinctive and promising opportunities for drug discovery along with the development of synthetic methodology, phenotypical screening, and computational studies.
Keywords: Macrocycle, Macrocyclic peptide, Macrolide, Macrocyclization, Infection disease, Oncology, Drug discovery.
Current Pharmaceutical Design
Title:Macrocyclic Compounds: Emerging Opportunities for Current Drug Discovery
Volume: 22 Issue: 26
Author(s): Lisha You, Rui An, Kun Liang, Bo Cui and Xinhong Wang
Affiliation:
Keywords: Macrocycle, Macrocyclic peptide, Macrolide, Macrocyclization, Infection disease, Oncology, Drug discovery.
Abstract: The macrocycles representing a unique chemical structure bridging conventional small molecules and large biomolecules, have attracted more and more attention in drug discovery over the past decade, and tremendous progress has been made toward the macrocyclization synthesis and structure diversification recently. Because of their favored size, flexibility and complexity, macrocycles can engage previously undruggable targets through numerous and spatially distributed binding interactions, and offer many privileged features including high potency, prominent selectivity, as well as favorable pharmacokinetics properties, and unique intellectual property(IP) space, and even safety profiles, etc. Currently around 70 macrocyclic molecules have been approved for clinical therapy, over 76 macrocycles are being evaluated in clinical trials from phase I to phase III. It is believed that the macrocycles will play more and more important role in the future, and provide very distinctive and promising opportunities for drug discovery along with the development of synthetic methodology, phenotypical screening, and computational studies.
Export Options
About this article
Cite this article as:
You Lisha, An Rui, Liang Kun, Cui Bo and Wang Xinhong, Macrocyclic Compounds: Emerging Opportunities for Current Drug Discovery, Current Pharmaceutical Design 2016; 22 (26) . https://dx.doi.org/10.2174/1381612822666160204114838
DOI https://dx.doi.org/10.2174/1381612822666160204114838 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
Call for Papers in Thematic Issues
"Tuberculosis Prevention, Diagnosis and Drug Discovery"
The Nobel Prize-winning discoveries of Mycobacterium tuberculosis and streptomycin have enabled an appropriate diagnosis and an effective treatment of tuberculosis (TB). Since then, many newer diagnosis methods and drugs have been saving millions of lives. Despite advances in the past, TB is still a leading cause of infectious disease mortality ...read more
Current Pharmaceutical challenges in the treatment and diagnosis of neurological dysfunctions
Neurological dysfunctions (MND, ALS, MS, PD, AD, HD, ALS, Autism, OCD etc..) present significant challenges in both diagnosis and treatment, often necessitating innovative approaches and therapeutic interventions. This thematic issue aims to explore the current pharmaceutical landscape surrounding neurological disorders, shedding light on the challenges faced by researchers, clinicians, and ...read more
Emerging and re-emerging diseases
Faced with a possible endemic situation of COVID-19, the world has experienced two important phenomena, the emergence of new infectious diseases and/or the resurgence of previously eradicated infectious diseases. Furthermore, the geographic distribution of such diseases has also undergone changes. This context, in turn, may have a strong relationship with ...read more
Melanoma and Non-Melanoma Skin Cancer Treatment: Standard of Care and Recent Advances
In this thematic issue, we aim to provide a standard of care of the diagnosis and treatment of melanoma and non-melanoma skin cancer. The editor will invite authors from different countries who will write review articles of melanoma and non-melanoma skin cancers. The Diagnosis, Staging, Surgical Treatment, Non-Surgical Treatment all ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Marine Collagen as a Source of Bioactive Molecules: A Review
The Natural Products Journal Neutrophil Derived Microvesicles: Emerging Role of a Key Mediator to the Immune Response
Endocrine, Metabolic & Immune Disorders - Drug Targets Treatment of Fabry Disease: Current and Emerging Strategies
Current Pharmaceutical Biotechnology All for Statins and Statins for All; An Update
Current Pharmaceutical Design Identification of Molecular Targets Associated with Ethanol Toxicity and Implications in Drug Development
Current Pharmaceutical Design The Role of PPARs in Obesity and other Insulin Resistance Associated Disorders
Current Medicinal Chemistry - Immunology, Endocrine & Metabolic Agents Protein Z and Ischemic Stroke
Vascular Disease Prevention (Discontinued) Role of Phase II Drug Metabolizing Enzymes in Cancer Chemoprevention
Current Drug Metabolism A Diabetes Treatment Strategy to Reduce the Risk of Cardiovascular Events: Clinical Benefits and Potential of Linagliptin
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Melatonin, a Potential Therapeutic Agent for Smooth Muscle-Related Pathological Conditions and Aging
Current Medicinal Chemistry Infectious Burden: A New Risk Factor and Treatment Target for Atherosclerosis
Infectious Disorders - Drug Targets Nucleic Acids Delivery Systems: A Challenge for Pharmaceutical Technologists
Current Drug Metabolism Surrogate Outcomes for Progression in the Initial Stages of Diabetic Retinopathy
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Is there a Teratogenicity Risk Associated with Cannabis and Synthetic Cannabimimetics’ (‘Spice’) Intake?
CNS & Neurological Disorders - Drug Targets Carotid Intima Media-thickness and Genes Involved in Lipid Metabolism in Diabetic Patients using Statins – a Pathway Toward Personalized Medicine
Cardiovascular & Hematological Agents in Medicinal Chemistry Therapeutic Potential of microRNA Modulation in Pulmonary Arterial Hypertension
Current Vascular Pharmacology Goto-kakizaki Rats: Its Suitability as Non-obese Diabetic Animal Model for Spontaneous Type 2 Diabetes Mellitus
Current Diabetes Reviews Editorial: Exploring Lipid-related Treatment Options for the Treatment of NASH
Current Vascular Pharmacology Second-Generation Antipsychotic Agents: A Review of Safety Profiles
Current Psychiatry Reviews Obesity: The Metabolic Disease, Advances on Drug Discovery and Natural Product Research
Current Topics in Medicinal Chemistry