Drug Discovery Stories: From Bench to Bedside presents a collection of cases on the development of highly successful pharmaceuticals. It delves into the realm of drug discovery, exploring the structural biology and biological functions of the sought-after targets. The book covers the identification of promising compounds, their transformation from hits to leads through meticulous optimization, and the elucidation of how key compounds interact with the target (in essence, providing invaluable insights for drug design). Additionally, it covers essential information such as the pivotal biological and PK data of lead compounds, any noteworthy clinical results, and a comprehensive overview of other candidate compounds. The field of drug discovery and development has experienced rapid evolution, with numerous new drugs receiving approval each year. While several books have been published on this subject, there is a pressing need for a new book series that accurately reflects the current advancements in drug discovery. This book aims to not only cater to the drug discovery community but also engage other communities involved in chemical biology, synthetic chemistry, and pharmacology.
1. Drug Discovery Stories - p. Page i 2. Cover - p. Page i 3. Title page - p. Page ii 4. Table of Contents - p. Page iii 5. Copyright - p. Page iii 6. Dedication - p. Page v 7. Contents - p. Page viii 8. List of contributors - p. Page viii 9. About the editors - p. Page xiii 10. Foreword 1 - p. Page xiv 11. Foreword 2 - p. Page xv 12. List of Illustrations - p. Page xviii 13. List of Tables - p. Page xix 14. Chapter 1 : Artificial intelligence in early stages of structure-based drug discovery - p. Page xix 15. Chapter 2 : Target-based vs phenotypic drug discovery: opportunities and challenges with evidence-based application - p. Page 16 16. Chapter 3 : Hit discovery from DNA-encoded chemical library - p. Page 41 17. Chapter 4 : Discovery of lead compounds from pseudo-natural macrocycles enabled by modular biomimetic strategy - p. Page 60 18. Chapter 5 : Macrocyclization strategy in kinase drug discovery - p. Page 80 19. Chapter 6 : Cobalt-catalyzed C–H functionalization for the synthesis of chiral heterocyclic molecules - p. Page 96 20. Chapter 7 : Advancing proteolysis targeting chimeras toward clinical drug developments - p. Page 118 21. Chapter 8 : A future battle, small-molecule drugs for cancer stem cell targeted therapy - p. Page 133 22. Chapter 9 : Stem cell therapies for combating emerging and reemerging viral infections - p. Page 151 23. Chapter 10 : Targeting autophagy with pharmacological small molecules to treat human diseases - p. Page 172 24. Chapter 11 : Interferons in human papillomavirus infection: antiviral effectors or immunopathogenic role? - p. Page 188 25. Chapter 12 : Selenium and small molecules: a symbiotic partnership - p. Page 206 26. Chapter 13 : Novel combinations of CD33-targeted immunotherapies - p. Page 227 27. Chapter 14 : Novel payloads of antibody-drug conjugates - p. Page 244 28. Chapter 15 : Antibody−drug conjugates: a new generation of cancer vaccines - p. Page 265 29. Chapter 16 : mRNA vaccines: the next frontier in disease prevention - p. Page 280 30. Chapter 17 : Unravelling the drying techniques of protein biopharmaceuticals - p. Page 301 31. Chapter 18 : Lenacapavir: a first-in-class HIV-1 capsid inhibitor for the treatment of multidrug-resistant HIV infections - p. Page 333 32. Chapter 19 : Nirmatrelvir, SIM0417, and RAY1216: potent and selective SARS-CoV-2 main protease inhibitors for the potential treatment of COVID-19 - p. Page 346 33. Chapter 20 : Bavdegalutamide (ARV-110): a potent PROTAC androgen receptor degrader for the treatment of metastatic-castration resistant prostate cancer - p. Page 355 34. Chapter 21 : Darolutamide: an androgen receptor antagonist for the treatment of prostate cancer - p. Page 371 35. Chapter 22 : Palbociclib, ribociclib, and abemaciclib: potent and selective CDK4/6 inhibitors for the treatment of breast cancer - p. Page 396 36. Chapter 23 : Zanubrutinib: a breakthrough in cancer therapy targeting Bruton’s tyrosine kinase, originating from China, and benefiting the global community - p. Page 420 37. Chapter 24 : Discovery of FT-2102 (olutasidenib), an inhibitor of mutant isocitrate dehydrogenase 1, for treatment of relapsed or refractory acute myeloid leukemia - p. Page 441 38. Chapter 25 : Ziftomenib (KO-539): a potent and selective Menin inhibitor for the treatment of recurrent or refractory acute myeloid leukemia - p. Page 452 39. Chapter 26 : Pulrodemstat (CC-90011): a highly potent, selective, and reversible lysine-specific demethylase 1 (LSD1) inhibitor - p. Page 464 40. Chapter 27 : Mavacamten, a first-in-class cardiac myosin inhibitor for the treatment of hypertrophic cardiomyopathy - p. Page 480 41. Chapter 28 : Verquvo, a first-in-class soluble guanylate cyclase stimulator for the treatment of heart failure - p. Page 508 42. Chapter 29 : Tafamidis: a transthyretin stabilizer for rare cardiac amyloidosis - p. Page 531 43. Chapter 30 : Oliceridine (TRV130): a biased agonist of the μ opioid receptor as a novel analgesic - p. Page 545 44. Chapter 31 : Sotyktu (Deucravacitinib): the first tyrosine kinase 2 (TYK2) inhibitor approved for the treatment of psoriasis - p. Page 567 45. Chapter 32 : Bexagliflozin: a sodium-glucose co-transporter-2 inhibitor as anti-diabetic drug derived from phlorizin - p. Page 584 46. Chapter 33 : Antidiabetic drugs−targeted PPARγ: from full agonists to selective modulators - p. Page 599 47. Chapter 34 : Pretomanid: an antibiotic used for the treatment of multidrug-resistant tuberculosis - p. Page 621 48. Chapter 35 : Lecanemab (Leqembi): an amyloid beta monoclonal antibody approved for the treatment of Alzheimer’s disease - p. Page 640 49. Chapter 36 : Pembrolizumab: a breakthrough in cancer immunotherapy - p. Page 651 50. Index - p. Page 665
Drug Discovery Stories: From Bench to Bedside presents a collection of cases on the development of highly successful pharmaceuticals. It delves into the realm of drug discovery, exploring the structural biology and biological functions of the sought-after targets. The book covers the identification of promising compounds, their transformation from hits to leads through meticulous optimization, and the elucidation of how key compounds interact with the target (in essence, providing invaluable insights for drug design). Additionally, it covers essential information such as the pivotal biological and PK data of lead compounds, any noteworthy clinical results, and a comprehensive overview of other candidate compounds. The field of drug discovery and development has experienced rapid evolution, with numerous new drugs receiving approval each year. While several books have been published on this subject, there is a pressing need for a new book series that accurately reflects the current advancements in drug discovery. This book aims to not only cater to the drug discovery community but also engage other communities involved in chemical biology, synthetic chemistry, and pharmacology.
1. Drug Discovery Stories - p. Page i 2. Cover - p. Page i 3. Title page - p. Page ii 4. Table of Contents - p. Page iii 5. Copyright - p. Page iii 6. Dedication - p. Page v 7. Contents - p. Page viii 8. List of contributors - p. Page viii 9. About the editors - p. Page xiii 10. Foreword 1 - p. Page xiv 11. Foreword 2 - p. Page xv 12. List of Illustrations - p. Page xviii 13. List of Tables - p. Page xix 14. Chapter 1 : Artificial intelligence in early stages of structure-based drug discovery - p. Page xix 15. Chapter 2 : Target-based vs phenotypic drug discovery: opportunities and challenges with evidence-based application - p. Page 16 16. Chapter 3 : Hit discovery from DNA-encoded chemical library - p. Page 41 17. Chapter 4 : Discovery of lead compounds from pseudo-natural macrocycles enabled by modular biomimetic strategy - p. Page 60 18. Chapter 5 : Macrocyclization strategy in kinase drug discovery - p. Page 80 19. Chapter 6 : Cobalt-catalyzed C–H functionalization for the synthesis of chiral heterocyclic molecules - p. Page 96 20. Chapter 7 : Advancing proteolysis targeting chimeras toward clinical drug developments - p. Page 118 21. Chapter 8 : A future battle, small-molecule drugs for cancer stem cell targeted therapy - p. Page 133 22. Chapter 9 : Stem cell therapies for combating emerging and reemerging viral infections - p. Page 151 23. Chapter 10 : Targeting autophagy with pharmacological small molecules to treat human diseases - p. Page 172 24. Chapter 11 : Interferons in human papillomavirus infection: antiviral effectors or immunopathogenic role? - p. Page 188 25. Chapter 12 : Selenium and small molecules: a symbiotic partnership - p. Page 206 26. Chapter 13 : Novel combinations of CD33-targeted immunotherapies - p. Page 227 27. Chapter 14 : Novel payloads of antibody-drug conjugates - p. Page 244 28. Chapter 15 : Antibody−drug conjugates: a new generation of cancer vaccines - p. Page 265 29. Chapter 16 : mRNA vaccines: the next frontier in disease prevention - p. Page 280 30. Chapter 17 : Unravelling the drying techniques of protein biopharmaceuticals - p. Page 301 31. Chapter 18 : Lenacapavir: a first-in-class HIV-1 capsid inhibitor for the treatment of multidrug-resistant HIV infections - p. Page 333 32. Chapter 19 : Nirmatrelvir, SIM0417, and RAY1216: potent and selective SARS-CoV-2 main protease inhibitors for the potential treatment of COVID-19 - p. Page 346 33. Chapter 20 : Bavdegalutamide (ARV-110): a potent PROTAC androgen receptor degrader for the treatment of metastatic-castration resistant prostate cancer - p. Page 355 34. Chapter 21 : Darolutamide: an androgen receptor antagonist for the treatment of prostate cancer - p. Page 371 35. Chapter 22 : Palbociclib, ribociclib, and abemaciclib: potent and selective CDK4/6 inhibitors for the treatment of breast cancer - p. Page 396 36. Chapter 23 : Zanubrutinib: a breakthrough in cancer therapy targeting Bruton’s tyrosine kinase, originating from China, and benefiting the global community - p. Page 420 37. Chapter 24 : Discovery of FT-2102 (olutasidenib), an inhibitor of mutant isocitrate dehydrogenase 1, for treatment of relapsed or refractory acute myeloid leukemia - p. Page 441 38. Chapter 25 : Ziftomenib (KO-539): a potent and selective Menin inhibitor for the treatment of recurrent or refractory acute myeloid leukemia - p. Page 452 39. Chapter 26 : Pulrodemstat (CC-90011): a highly potent, selective, and reversible lysine-specific demethylase 1 (LSD1) inhibitor - p. Page 464 40. Chapter 27 : Mavacamten, a first-in-class cardiac myosin inhibitor for the treatment of hypertrophic cardiomyopathy - p. Page 480 41. Chapter 28 : Verquvo, a first-in-class soluble guanylate cyclase stimulator for the treatment of heart failure - p. Page 508 42. Chapter 29 : Tafamidis: a transthyretin stabilizer for rare cardiac amyloidosis - p. Page 531 43. Chapter 30 : Oliceridine (TRV130): a biased agonist of the μ opioid receptor as a novel analgesic - p. Page 545 44. Chapter 31 : Sotyktu (Deucravacitinib): the first tyrosine kinase 2 (TYK2) inhibitor approved for the treatment of psoriasis - p. Page 567 45. Chapter 32 : Bexagliflozin: a sodium-glucose co-transporter-2 inhibitor as anti-diabetic drug derived from phlorizin - p. Page 584 46. Chapter 33 : Antidiabetic drugs−targeted PPARγ: from full agonists to selective modulators - p. Page 599 47. Chapter 34 : Pretomanid: an antibiotic used for the treatment of multidrug-resistant tuberculosis - p. Page 621 48. Chapter 35 : Lecanemab (Leqembi): an amyloid beta monoclonal antibody approved for the treatment of Alzheimer’s disease - p. Page 640 49. Chapter 36 : Pembrolizumab: a breakthrough in cancer immunotherapy - p. Page 651 50. Index - p. Page 665
