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Progress in Medicinal Chemistry

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https://read.qxmd.com/read/30879476/preface
#1
EDITORIAL
David R Witty, Brian Cox
No abstract text is available yet for this article.
2019: Progress in Medicinal Chemistry
https://read.qxmd.com/read/30879475/amyotrophic-lateral-sclerosis
#2
Klara Valko, Lukasz Ciesla
Amyotrophic lateral sclerosis (ALS) is caused by selective and progressive loss of spinal, bulbar and cortical motoneurons and leads to irreversible paralysis, loss of speech, inability to swallow and respiratory malfunctions with the eventual death of the affected individual in a rapid disease course. Several suggested molecular pathways are reviewed including SOD1 gene mutation, protein nitrosylation, phosphorylation and oxidative stress, excitotoxicity, glutamate transporter deprivation, mitochondrial involvement, protein aggregation and motor neuron trophic factors...
2019: Progress in Medicinal Chemistry
https://read.qxmd.com/read/30879474/natural-product-drug-delivery-a-special-challenge
#3
Neil J Press, Emilie Joly, Peter Ertl
Natural products have a long-standing and critical role in drug development and medical use. The structural and physicochemical properties of natural products, while derived evolutionarily to be effective in living systems, may create challenges in translation to a pharmaceutical product. Molecular complexity, low solubility, functional group reactivity and general instability are among the challenges that typically need to be overcome. This review looks at some of the ways that natural products have been formulated and delivered to enable the successful application of these vitally important medicines to patients...
2019: Progress in Medicinal Chemistry
https://read.qxmd.com/read/30879473/rewriting-the-tran-script-application-to-spinal-muscular-atrophy
#4
Hasane Ratni, Lutz Mueller, Martin Ebeling
Targeting RNA drastically expands our target space to therapeutically modulate numerous cellular processes implicated in human diseases. Of particular interest, drugging pre-mRNA splicing appears a very viable strategy; to control levels of splicing product by promoting the inclusion or exclusion of exons. After describing the concept of "splicing modulation", this chapter will cover the outstanding progress achieved in this field, by highlighting the breakthrough accomplished recently for the treatment of spinal muscular atrophy using two therapeutic modalities: splice switching oligonucleotides and small molecules...
2019: Progress in Medicinal Chemistry
https://read.qxmd.com/read/30879472/covalent-binders-in-drug-discovery
#5
Anil Vasudevan, Maria A Argiriadi, Aleksandra Baranczak, Michael M Friedman, Julia Gavrilyuk, Adrian D Hobson, Jonathan J Hulce, Sami Osman, Noel S Wilson
Covalent modulation of protein function can have multiple utilities including therapeutics, and probes to interrogate biology. While this field is still viewed with scepticism due to the potential for (idiosyncratic) toxicities, significant strides have been made in terms of understanding how to tune electrophilicity to selectively target specific residues. Progress has also been made in harnessing the potential of covalent binders to uncover novel biology and to provide an enhanced utility as payloads for Antibody Drug Conjugates...
2019: Progress in Medicinal Chemistry
https://read.qxmd.com/read/29680152/preface
#6
EDITORIAL
David R Witty, Brian Cox
No abstract text is available yet for this article.
2018: Progress in Medicinal Chemistry
https://read.qxmd.com/read/29680151/vmat2-inhibitors-and-the-path-to-ingrezza-valbenazine
#7
REVIEW
Nicole D Harriott, John P Williams, Evan B Smith, Haig P Bozigian, Dimitri E Grigoriadis
The dopaminergic system plays a key role in the central nervous system, regulating executive function, arousal, reward, and motor control. Dysregulation of this critical monoaminergic system has been associated with diseases of the central nervous system including schizophrenia, Parkinson's disease, and disorders such as attention deficit hyperactivity disorders and addiction. Drugs that modify the dopaminergic system by modulating the activity of dopamine have been successful in demonstrating clinical efficacy by providing treatments for these diseases...
2018: Progress in Medicinal Chemistry
https://read.qxmd.com/read/29680150/big-data-in-drug-discovery
#8
REVIEW
Nathan Brown, Jean Cambruzzi, Peter J Cox, Mark Davies, James Dunbar, Dean Plumbley, Matthew A Sellwood, Aaron Sim, Bryn I Williams-Jones, Magdalena Zwierzyna, David W Sheppard
Interpretation of Big Data in the drug discovery community should enhance project timelines and reduce clinical attrition through improved early decision making. The issues we encounter start with the sheer volume of data and how we first ingest it before building an infrastructure to house it to make use of the data in an efficient and productive way. There are many problems associated with the data itself including general reproducibility, but often, it is the context surrounding an experiment that is critical to success...
2018: Progress in Medicinal Chemistry
https://read.qxmd.com/read/29680149/recent-progress-in-the-discovery-and-development-of-small-molecule-modulators-of-cftr
#9
Phil R Kym, Xueqing Wang, Mathieu Pizzonero, Steven E Van der Plas
Cystic fibrosis (CF) is a genetic disorder driven by mutations in the cystic fibrosis transmembrane conductance regulator (CFTR) gene. While different mutations lead to varying levels of disease severity, the most common CFTR F508del mutation leads to defects in protein stability, trafficking to the cell membrane and gating of chloride ions. Recently, advances in medicinal chemistry have led to the identification small-molecule drugs that result in significant clinical efficacy in improving lung function in CF patients...
2018: Progress in Medicinal Chemistry
https://read.qxmd.com/read/29680148/current-trends-in-macrocyclic-drug-discovery-and-beyond-ro5
#10
Sulejman Alihodžić, Mirjana Bukvić, Ivaylo J Elenkov, Antun Hutinec, Sanja Koštrun, Dijana Pešić, Gordon Saxty, Linda Tomašković, Dinko Žiher
This chapter will discuss the recent literature of macrocycles and drug-like property space moving beyond the rule of five (bRo5). Trends in chemical classes that fall within this definition are discussed and the impact of the latest technologies in the field assessed. The physicochemical properties, which have provided both successes and challenges, especially in scale-up, are discussed. A recent patent literature is reviewed and the chapter concludes with a perspective on the future of macrocyclic drug discovery...
2018: Progress in Medicinal Chemistry
https://read.qxmd.com/read/29680147/discovery-and-development-of-calcimimetic-and-calcilytic-compounds
#11
Edward F Nemeth, Bradford C Van Wagenen, Manuel F Balandrin
The extracellular calcium receptor (CaR) is a G protein-coupled receptor (GPCR) and the pivotal molecule regulating systemic Ca2+ homeostasis. The CaR was a challenging target for drug discovery because its physiological ligand is an inorganic ion (Ca2+ ) rather than a molecule so there was no structural template to guide medicinal chemistry. Nonetheless, small molecules targeting this receptor were discovered. Calcimimetics are agonists or positive allosteric modulators of the CaR, while calcilytics are antagonists and all to date are negative allosteric modulators...
2018: Progress in Medicinal Chemistry
https://read.qxmd.com/read/28314414/preface
#12
EDITORIAL
D R Witty, B Cox
No abstract text is available yet for this article.
2017: Progress in Medicinal Chemistry
https://read.qxmd.com/read/28314413/recent-progress-in-the-discovery-and-development-of-trpa1-modulators
#13
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://read.qxmd.com/read/28314412/development-of-lrrk2-inhibitors-for-the-treatment-of-parkinson-s-disease
#14
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://read.qxmd.com/read/28314411/small-molecule-inhibition-of-interleukin-1-receptor-associated-kinase-4-irak4
#15
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://read.qxmd.com/read/28314410/enabling-chemistry-technologies-and-parallel-synthesis-accelerators-of-drug-discovery-programmes
#16
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://read.qxmd.com/read/26852937/preface
#17
EDITORIAL
Geoff Lawton, David Witty
No abstract text is available yet for this article.
2016: Progress in Medicinal Chemistry
https://read.qxmd.com/read/26852936/the-evolving-role-of-the-medicinal-chemist
#18
REVIEW
Geoff Lawton, Peter Nussbaumer
No abstract text is available yet for this article.
2016: Progress in Medicinal Chemistry
https://read.qxmd.com/read/26852935/recent-advances-in-the-discovery-of-deubiquitinating-enzyme-inhibitors
#19
REVIEW
Mark Kemp
No abstract text is available yet for this article.
2016: Progress in Medicinal Chemistry
https://read.qxmd.com/read/26852934/measurement-interpretation-and-use-of-free-ligand-solution-conformations-in-drug-discovery
#20
REVIEW
Charles D Blundell, Thorsten Nowak, Martin J Watson
No abstract text is available yet for this article.
2016: Progress in Medicinal Chemistry
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