Expert Opinion on Drug Discovery
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Introduction: Precision medicine is the concept of treating diseases based on environmental factors, lifestyles, and molecular profiles of patients. This approach has been found to increase success rates of clinical trials and accelerate drug approvals. However, current precision medicine applications in early drug discovery use only a handful of molecular biomarkers to make decisions, whilst clinics gear up to capture the full molecular landscape of patients in the near future. This deep multi-...
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Introduction There continues to be an exponential rise in the number of small molecule drugs that contain either a fluorine atom or a fluorinated fragment. While the unique properties of fluorine enable the precise modulation of a molecule's physicochemical properties, strategic bioisosteric replacement of fragments with fluorinated moieties represents an area of significant growth.Areas Covered This review discusses the strategic employment of fluorine-substitution in the design and development...
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#1Giulia Russo (University of Catania)H-Index: 28
#2Valentina Di Salvatore (University of Catania)H-Index: 3
Last. Francesco Pappalardo (University of Catania)H-Index: 22
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#1Kenneth K.W. To (CUHK: The Chinese University of Hong Kong)H-Index: 32
#2William C. ChoH-Index: 37
INTRODUCTION Messenger RNA (mRNA)-based therapeutics and vaccines have emerged as a disruptive new drug class for various applications, including regenerative medicine, cancer treatment, and prophylactic and therapeutic vaccinations. AREAS COVERED This review provides an update about the rational structure-based design of various formats of mRNA-based therapeutics. The authors discuss the recent advances in the mRNA modifications that have been used to enhance stability, promote translation effi...
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#1Ola Spjuth (Science for Life Laboratory)H-Index: 23
Last. Andreas HellanderH-Index: 18
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Introduction: Artificial intelligence (AI) and machine learning (ML) are increasingly used in many aspects of drug discovery. Larger data sizes and methods such as Deep Neural Networks contribute to challenges in data management, the required software stack, and computational infrastructure. There is an increasing need in drug discovery to continuously re-train models and make them available in production environments.Areas covered: This article describes how cloud computing can aid the ML life ...
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#1Florian Wittlinger (University of Tübingen)H-Index: 1
#2Stefan Laufer (University of Tübingen)H-Index: 67
IntroductionOsimertinib is currently the only by FDA and EMA approved 3rd generation small-molecule epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI). It was initially indicated for second-line treatment of patients with metastatic EGFR T790M mutation-positive non-small cell lung cancer (NSCLC) and got approved for first-line treatment of EGFR activation mutation-positive metastatic NSCLC in 2018. Most recently, the FDA granted approval for the adjuvant treatment of patient...
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#1Caroline M Hull (Guy's Hospital)
#2John Maher (University of Cambridge)H-Index: 35
Introduction: Chimeric antigen receptor-engineered T-cells typically use the binding domains of antibodies to target cytotoxicity toward tumors. This approach has produced great efficacy against selected hematological cancers, but benefit in solid tumors has been limited. Characteristically, the microenvironment in solid tumors restricts CAR T cell function, thereby limiting success. Enhancing efficacy will depend on novel target discovery to refine specificity and reduce toxicity. Additionally,...
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#1Marialucia Gallorini (University of Chieti-Pescara)H-Index: 11
#2Simone Carradori (University of Chieti-Pescara)H-Index: 41
Introduction: Among protein and fibers in the extracellular matrix (ECM), collagen is the most copious and widely employed in cosmetic, food, pharmaceutical, and biomedical industries due to its extensive biocompatible and versatile properties. In the last years, the knowledge about functions of collagens increased and expanded dramatically. Once considered only crucial for the ECM scaffolding and mechanotransduction, additional functional roles have now been ascribed to the collagen superfamily...
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#1Michaela Serpi (Cardiff University)H-Index: 13
#2Fabrizio Pertusati (Cardiff University)H-Index: 11
INTRODUCTION The ProTide technology is a phosphate (or phosphonate) prodrug method devised to deliver nucleoside monophosphate (or monophosphonate) intracellularly bypassing the key challenges of antiviral and anticancer nucleoside analogues. Three new antiviral drugs, exploiting this technology, have been approved by the FDA while others are in clinical studies as anticancer agents. AREAS COVERED The authors describe the origin and development of this technology and its incredible success in tr...
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