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Progress in Medicinal Chemistry

journal
https://www.readbyqxmd.com/read/26852937/preface
#1
EDITORIAL
Geoff Lawton, David Witty
No abstract text is available yet for this article.
2016: Progress in Medicinal Chemistry
https://www.readbyqxmd.com/read/26852936/the-evolving-role-of-the-medicinal-chemist
#2
REVIEW
Geoff Lawton, Peter Nussbaumer
No abstract text is available yet for this article.
2016: Progress in Medicinal Chemistry
https://www.readbyqxmd.com/read/26852935/recent-advances-in-the-discovery-of-deubiquitinating-enzyme-inhibitors
#3
REVIEW
Mark Kemp
No abstract text is available yet for this article.
2016: Progress in Medicinal Chemistry
https://www.readbyqxmd.com/read/26852934/measurement-interpretation-and-use-of-free-ligand-solution-conformations-in-drug-discovery
#4
REVIEW
Charles D Blundell, Thorsten Nowak, Martin J Watson
No abstract text is available yet for this article.
2016: Progress in Medicinal Chemistry
https://www.readbyqxmd.com/read/26852933/non-systemic-intestine-targeted-drugs
#5
REVIEW
Matthew C T Fyfe
No abstract text is available yet for this article.
2016: Progress in Medicinal Chemistry
https://www.readbyqxmd.com/read/25727707/preface
#6
EDITORIAL
Geoff Lawton, David Witty
No abstract text is available yet for this article.
2015: Progress in Medicinal Chemistry
https://www.readbyqxmd.com/read/25727706/imaging-in-drug-development
#7
REVIEW
James Nairne, Peter B Iveson, Andreas Meijer
Imaging has played an important part in the diagnosis of disease and development of the understanding of the underlying disease mechanisms and is now poised to make an impact in the development of new pharmaceuticals. This chapter discusses the underlying technologies that make the field ready for this challenge. In particular, the potentials of magnetic resonance imaging and functional magnetic resonance imaging are outlined, including the new methods developed to provide additional information from the scans carried out...
2015: Progress in Medicinal Chemistry
https://www.readbyqxmd.com/read/25727705/a-new-era-for-chagas-disease-drug-discovery
#8
REVIEW
Martine Keenan, Jason H Chaplin
Recent clinical trials investigating treatment of chronic indeterminate Chagas disease with two re-purposed azole anti-fungal drugs, posaconazole and ravuconazole, revealed their inferiority to the current standard-of-care benznidazole and highlighted the inadequacy of the existing pre-clinical testing paradigm for this disease. A very limited number of controlled clinical trials for Chagas disease have been conducted to date. The selection of these compounds for clinical evaluation relied heavily on pre-clinical data obtained from in vitro screens and animal studies...
2015: Progress in Medicinal Chemistry
https://www.readbyqxmd.com/read/25727704/a-perspective-on-the-next-generation-of-antibacterial-agents-derived-by-manipulation-of-natural-products
#9
REVIEW
Pamela Brown, Michael J Dawson
Natural products have been a major source of anti-infective drugs for many decades. With urgent need for new antibacterial agents to combat drug-resistant bacteria, the investigation of both new and existing classes of natural products has once again become an important focus. In this review, we highlight how a medicinal chemistry/semi-synthetic approach to natural product manipulation continues to offer a valuable strategy to overcome limitations in current therapy. Approaches to address toxicity and to improve the solubility, bioavailability and the spectrum of activity are demonstrated...
2015: Progress in Medicinal Chemistry
https://www.readbyqxmd.com/read/25727703/fluorine-in-medicinal-chemistry
#10
REVIEW
Steven Swallow
Since its first use in the steroid field in the late 1950s, the use of fluorine in medicinal chemistry has become commonplace, with the small electronegative fluorine atom being a key part of the medicinal chemist's repertoire of substitutions used to modulate all aspects of molecular properties including potency, physical chemistry and pharmacokinetics. This review will highlight the special nature of fluorine, drawing from a survey of marketed fluorinated pharmaceuticals and the medicinal chemistry literature, to illustrate key concepts exploited by medicinal chemists in their attempts to optimize drug molecules...
2015: Progress in Medicinal Chemistry
https://www.readbyqxmd.com/read/25727702/recent-advances-in-cancer-therapeutics
#11
REVIEW
Nicola Chessum, Keith Jones, Elisa Pasqua, Michael Tucker
In the past 20 years, cancer therapeutics has undergone a paradigm shift away from the traditional cytotoxic drugs towards the targeting of proteins intimately involved in driving the cancer phenotype. The poster child for this alternative approach to the treatment of cancer is imatinib, a small-molecule kinase inhibitor designed to target chronic myeloid leukaemia driven by the BCR-ABL translocation in a defined patient population. The improvement in survival achieved by treatment of this patient cohort with imatinib is impressive...
2015: Progress in Medicinal Chemistry
https://www.readbyqxmd.com/read/24418611/preface
#12
EDITORIAL
Geoff Lawton, David Witty
No abstract text is available yet for this article.
2014: Progress in Medicinal Chemistry
https://www.readbyqxmd.com/read/24418610/recent-progress-in-the-discovery-and-development-of-n-type-calcium-channel-modulators-for-the-treatment-of-pain
#13
REVIEW
Margaret S Lee
The importance of voltage-gated calcium channels (VGCCs) in basic physiological processes such as cardiac and neurological function has generated intense interest in these proteins as targets of pharmacological intervention. N-type calcium channels are a subset of VGCCs distinguished by their physiology, pharmacology and significance to the pathology of chronic pain. Despite decades of investigation, only a single drug targeting N-type channel function has entered the marketplace. This review will summarize our current understanding of the biology, physiology and pharmacology of N-type calcium channels and the implication of these features for therapeutic intervention...
2014: Progress in Medicinal Chemistry
https://www.readbyqxmd.com/read/24418609/%C3%AE-secretase-modulators-current-status-and-future-directions
#14
REVIEW
Adrian Hall, Toshal R Patel
This chapter reviews the current status of γ-secretase modulators, highlighting key compounds by each company involved in the area. The review focuses on the three main chemotypes: acids, imidazoles and related derivatives and natural products. A section on chemical biology and ligand-binding site elucidation studies is also included. The primary source of information is drawn from peer reviewed literature as this permits analysis of PK-PD relationships and subsequent comment. Discussion of the patent literature is included for completeness...
2014: Progress in Medicinal Chemistry
https://www.readbyqxmd.com/read/24418608/p2x7-antagonists-as-potential-therapeutic-agents-for-the-treatment-of-cns-disorders
#15
REVIEW
Christa C Chrovian, Jason C Rech, Anindya Bhattacharya, Michael A Letavic
The use of P2X7 antagonists to treat inflammatory disorders has garnered considerable interest in recent years. An increasing number of literature reports support the role of P2X7 in inflammatory pathways of the peripheral and central nervous systems (CNSs). A number of CNS indications such as neuropsychiatric and neurodegenerative disorders and neuropathic pain have been linked to a neuroinflammatory response, and clinical studies have shown that inflammatory biomarkers can be mitigated by modulating P2X7...
2014: Progress in Medicinal Chemistry
https://www.readbyqxmd.com/read/24418607/structure-based-drug-design-for-g-protein-coupled-receptors
#16
REVIEW
Miles Congreve, João M Dias, Fiona H Marshall
Our understanding of the structural biology of G protein-coupled receptors has undergone a transformation over the past 5 years. New protein-ligand complexes are described almost monthly in high profile journals. Appreciation of how small molecules and natural ligands bind to their receptors has the potential to impact enormously how medicinal chemists approach this major class of receptor targets. An outline of the key topics in this field and some recent examples of structure- and fragment-based drug design are described...
2014: Progress in Medicinal Chemistry
https://www.readbyqxmd.com/read/23384669/glucokinase-preface
#17
Geoff Lawton, David R Witty
No abstract text is available yet for this article.
2013: Progress in Medicinal Chemistry
https://www.readbyqxmd.com/read/23384668/advances-in-the-discovery-of-selective-jak-inhibitors
#18
Christel J Menet, Luc Van Rompaey, Raphaël Geney
In this review, we describe the current knowledge of the biology of the JAKs. The JAK family comprises the four nonreceptor tyrosine kinases JAK1, JAK2, JAK3, and Tyk2, all key players in the signal transduction from cytokine receptors to transcription factor activation. We also review the progresses made towards the optimization of JAK inhibitors and the importance of their selectivity profile. Indeed, the full array of many medicinal chemistry enabling tools (HTS, X-ray crystallography, scaffold morphing, etc...
2013: Progress in Medicinal Chemistry
https://www.readbyqxmd.com/read/23384667/antimalarial-drug-discovery-recent-progress-and-future-directions
#19
REVIEW
Félix Calderón, David M Wilson, Francisco-Javier Gamo
No abstract text is available yet for this article.
2013: Progress in Medicinal Chemistry
https://www.readbyqxmd.com/read/23384666/medicinal-chemistry-of-glucagon-like-peptide-receptor-agonists
#20
Lyn H Jones, David A Price
No abstract text is available yet for this article.
2013: Progress in Medicinal Chemistry
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