Progress in Medicinal Chemistry, Volume 58, provides a review of eclectic developments in medicinal chemistry, with each chapter written by an international board of authors. Topics covered in this new release include Amyotrophic lateral sclerosis (ALS), Covalent-binding Drugs, Natural Product Drug Delivery A Special Challenge , and SMN2 gene splicing modifier, and more.
- Provides extended, timely reviews of topics in medicinal chemistry
- Contains targets and technologies relevant to the discovery of tomorrows drugs
- Presents analyses of successful drug discovery programs
| Contributors |
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vii | |
| Preface |
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ix | |
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1 Covalent binders in drug discovery |
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1 | (62) |
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2 | (1) |
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2 Types of covalent binders |
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3 | (23) |
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3 Structure-based considerations |
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26 | (7) |
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4 Approved/clinical covalent inhibitors |
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33 | (7) |
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5 Covalent probes in chemical biology |
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40 | (6) |
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6 Natural products as ADC payloads |
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46 | (6) |
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52 | (1) |
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53 | (9) |
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62 | (1) |
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2 Amyotrophic lateral sclerosis |
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63 | (56) |
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1 Amyotrophic lateral sclerosis (ALS) |
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64 | (6) |
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2 Potential cellular signalling pathways that could be targeted for the treatment of motoneuron diseases |
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70 | (11) |
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3 Current markers and animal models used to evaluate the effect of new therapeutics in ALS |
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81 | (3) |
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4 Current medicinal chemistry approaches |
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84 | (21) |
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5 Summary of current approaches and future directions |
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105 | (3) |
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108 | (1) |
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108 | (11) |
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3 Rewriting the (tran)script: Application to spinal muscular atrophy |
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119 | (38) |
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119 | (1) |
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120 | (3) |
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3 Spinal muscular atrophy (SMA) |
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123 | (2) |
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4 Discovery of nusinersen |
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125 | (2) |
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127 | (3) |
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130 | (14) |
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7 Selectivity of risdiplam compared to other small molecule splicing modifiers |
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144 | (6) |
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150 | (1) |
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151 | (1) |
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152 | (5) |
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4 Natural product drug delivery: A special challenge? |
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157 | (1) |
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158 | (2) |
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160 | (2) |
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162 | (2) |
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164 | (3) |
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5 Rapamycin and analogues |
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167 | (4) |
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171 | (4) |
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175 | (2) |
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177 | (3) |
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180 | (1) |
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181 | (1) |
| References |
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182 | |
Dr David Witty has more than 20 years experience in the pharmaceutical industry as a medicinal chemist and project leader working principally in areas of anti-infectives, metabolic diseases, cognition and pain, delivering clinical candidates for several conditions. He led IT Strategy within the Neurology division of GSK, developing and deploying the first Electronic Notebooks for drug discovery to sites in the UK and Singapore. He has contributed more than 90 scientific papers, reviews, patents and books on medicinal and synthetic chemistry.In 2010 David and several colleagues successfully raised $35M in venture funding to found Convergence Pharmaceuticals, a specialist ion channel company focused on the development of novel treatments for pain, based in Cambridge UK. David presently leads their discovery programme and manages scientific operations within the business.David is chairman of the Fine Chemicals Group of the Society of Chemical Industry, with responsibility for the delivery of conferences, seminars and training courses for chemists throughout the UK and Europe, and advising parliamentary bodies on matters of relevance to the UK chemical industry.Since 2008 David has been a STEM ambassador for SETPOINT, introducing school students at both primary and secondary level to the excitement and possibilities of pursuing scientific careers, through workshops, lectures and competitions. Professor Brian Cox is at University of Sussex, Brighton, UK
Daugiau apie elektronines knygas