Literature DB >> 31082225

Rational Design of Multitarget-Directed Ligands: Strategies and Emerging Paradigms.

Junting Zhou1,2, Xueyang Jiang1,2, Siyu He1, Hongli Jiang1,2, Feng Feng2,3, Wenyuan Liu4, Wei Qu2, Haopeng Sun1.   

Abstract

Due to the complexity of multifactorial diseases, single-target drugs do not always exhibit satisfactory efficacy. Recently, increasing evidence indicates that simultaneous modulation of multiple targets may improve both therapeutic safety and efficacy, compared with single-target drugs. However, few multitarget drugs are on market or in clinical trials, despite the best efforts of medicinal chemists. This article discusses the systematic establishment of target combination, lead generation, and optimization of multitarget-directed ligands (MTDLs). Moreover, we analyze some MTDLs research cases for several complex diseases in recent years and the physicochemical properties of 117 clinical multitarget drugs, with the aim to reveal the trends and insights of the potential use of MTDLs.

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Year:  2019        PMID： 31082225     DOI： 10.1021/acs.jmedchem.9b00017

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  26 in total

1.  Multiple Target Drug Design Using LigBuilder 3.

Authors:  Xiaoyu Qing; Shiwei Wang; Yaxia Yuan; Jianfeng Pei; Luhua Lai
Journal:  Methods Mol Biol       Date:  2021

2.  New Dual CK2/HDAC1 Inhibitors with Nanomolar Inhibitory Activity against Both Enzymes.

Authors:  Loganathan Rangasamy; Irene Ortín; José María Zapico; Claire Coderch; Ana Ramos; Beatriz de Pascual-Teresa
Journal:  ACS Med Chem Lett       Date:  2020-04-07       Impact factor: 4.345

3.  Multifunctional Arylsulfone and Arylsulfonamide-Based Ligands with Prominent Mood-Modulating Activity and Benign Safety Profile, Targeting Neuropsychiatric Symptoms of Dementia.

Authors:  Monika Marcinkowska; Adam Bucki; Joanna Sniecikowska; Agnieszka Zagórska; Nikola Fajkis-Zajączkowska; Agata Siwek; Monika Gluch-Lutwin; Paweł Żmudzki; Magdalena Jastrzebska-Wiesek; Anna Partyka; Anna Wesołowska; Michał Abram; Katarzyna Przejczowska-Pomierny; Agnieszka Cios; Elżbieta Wyska; Kamil Mika; Magdalena Kotańska; Paweł Mierzejewski; Marcin Kolaczkowski
Journal:  J Med Chem       Date:  2021-08-26       Impact factor: 7.446

4.  1-(7-Chloroquinolin-4-yl)-N-(4-Methoxybenzyl)-5-Methyl-1H-1,2, 3-Triazole-4- carboxamide Reduces Aβ Formation and Tau Phosphorylation in Cellular Models of Alzheimer's Disease.

Authors:  Mariana G Fronza; Manoela Sacramento; Diego Alves; Domenico Praticò; Lucielli Savegnago
Journal:  Neurochem Res       Date:  2022-02-15       Impact factor: 3.996

5.  Candidate Therapeutics by Screening for Multitargeting Ligands: Combining the CB2 Receptor With CB1, PPARγ and 5-HT4 Receptors.

Authors:  Shayma El-Atawneh; Amiram Goldblum
Journal:  Front Pharmacol       Date:  2022-02-28       Impact factor: 5.810

Review 6.  Recent advances in multitarget-directed ligands targeting G-protein-coupled receptors.

Authors:  Hongguang Ma; Boshi Huang; Yan Zhang
Journal:  Drug Discov Today       Date:  2020-07-09       Impact factor: 7.851

7.  Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer.

Authors:  Shruti Choudhary; Arpit Doshi; Lerin Luckett-Chastain; Michael Ihnat; Ernest Hamel; Susan L Mooberry; Aleem Gangjee
Journal:  Bioorg Med Chem       Date:  2021-02-12       Impact factor: 3.641

8.  Introducing the metacore concept for multi-target ligand design.

Authors:  Dagmar Stumpfe; Alexander Hoch; Jürgen Bajorath
Journal:  RSC Med Chem       Date:  2021-04-15

9.  Recent Advances in the Development of Sigma Receptor Ligands as Cytotoxic Agents: A Medicinal Chemistry Perspective.

Authors:  Antonino N Fallica; Valeria Pittalà; Maria N Modica; Loredana Salerno; Giuseppe Romeo; Agostino Marrazzo; Mohamed A Helal; Sebastiano Intagliata
Journal:  J Med Chem       Date:  2021-06-02       Impact factor: 7.446

10.  Combination of Heme Oxygenase-1 Inhibition and Sigma Receptor Modulation for Anticancer Activity.

Authors:  Giuseppe Romeo; Valeria Ciaffaglione; Emanuele Amata; Maria Dichiara; Loredana Calabrese; Luca Vanella; Valeria Sorrenti; Salvo Grosso; Agata Grazia D'Amico; Velia D'Agata; Sebastiano Intagliata; Loredana Salerno
Journal:  Molecules       Date:  2021-06-24       Impact factor: 4.411
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