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Progress in Medicinal Chemistry

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https://www.readbyqxmd.com/read/28314414/preface
#1
EDITORIAL
D R Witty, B Cox
No abstract text is available yet for this article.
2017: Progress in Medicinal Chemistry
https://www.readbyqxmd.com/read/28314413/recent-progress-in-the-discovery-and-development-of-trpa1-modulators
#2
REVIEW
S Skerratt
TRPA1 is a well-validated therapeutic target in areas of high unmet medical need that include pain and respiratory disorders. The human genetic rationale for TRPA1 as a pain target is provided by a study describing a rare gain-of-function mutation in TRPA1, causing familial episodic pain syndrome. There is a growing interest in the TRPA1 field, with many pharmaceutical companies reporting the discovery of TRPA1 chemical matter; however, GRC 17536 remains to date the only TRPA1 antagonist to have completed Phase IIa studies...
2017: Progress in Medicinal Chemistry
https://www.readbyqxmd.com/read/28314412/development-of-lrrk2-inhibitors-for-the-treatment-of-parkinson-s-disease
#3
REVIEW
K V Christensen, G P Smith, D S Williamson
Linkage and genome-wide association studies have identified a genetic risk locus for late-onset Parkinson's disease in chromosome 12, originally identified as PARK6. The causative gene was identified to code for a large multifunctional protein, LRRK2 (leucine-rich repeat kinase 2). The combined genetic and biochemical evidence supports a hypothesis in which the LRRK2 kinase function is causally involved in the pathogenesis of sporadic and familial forms of PD, and therefore that LRRK2 kinase inhibitors could be useful for treatment...
2017: Progress in Medicinal Chemistry
https://www.readbyqxmd.com/read/28314411/small-molecule-inhibition-of-interleukin-1-receptor-associated-kinase-4-irak4
#4
REVIEW
N E Genung, K M Guckian
In recent years, interleukin-1 receptor-associated kinase 4, IRAK4, has become an attractive target for many medicinal chemistry programmes. Target inhibition is of potential therapeutic value in areas including autoimmune disorders, cancer, inflammatory diseases, and possibly neurodegenerative diseases. Results from high-throughput screening efforts have led, in conjunction with structure-based drug design, to the identification of highly potent and selective small molecule IRAK4 inhibitors from many diverse chemical series...
2017: Progress in Medicinal Chemistry
https://www.readbyqxmd.com/read/28314410/enabling-chemistry-technologies-and-parallel-synthesis-accelerators-of-drug-discovery-programmes
#5
REVIEW
A Vasudevan, A R Bogdan, H F Koolman, Y Wang, S W Djuric
There is a pressing need to improve overall productivity in the pharmaceutical industry. Judicious investments in chemistry technologies can have a significant impact on cycle times, cost of goods and probability of technical success. This perspective describes some of these technologies developed and implemented at AbbVie, and their applications to the synthesis of novel scaffolds and to parallel synthesis.
2017: Progress in Medicinal Chemistry
https://www.readbyqxmd.com/read/26852937/preface
#6
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
#7
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
#8
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
#9
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
#10
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
#11
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
#12
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
#13
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
#14
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
#15
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
#16
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
#17
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
#18
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
#19
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
#20
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
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