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Signaling Pathways

The antibody-drug conjugate (ADC), a humanized or human monoclonal antibody conjugated with highly cytotoxic small molecules (payloads) through chemical linkers, is a novel therapeutic format and has great potential to make a paradigm shift in cancer chemotherapy. The three components of the ADC together give rise to a powerful oncolytic agent capable of delivering normally intolerable cytotoxins directly to cancer cells, which then internalize and release the cell-destroying drugs. At present, two ADCs, Adcetris and Kadcyla, have received regulatory approval with >40 others in clinical development.

ADCs are administered intravenously in order to prevent the mAb from being destroyed by gastric acids and proteolytic enzymes. The mAb component of the ADC enables it to circulate in the bloodstream until it finds and binds to tumor-specific cell surface antigens present on target cancer cells. Linker chemistry is an important determinant of the safety, specificity, potency and activity of ADCs. Linkers are designed to be stable in the blood stream (to conform to the increased circulation time of mAbs) and labile at the cancer site to allow rapid release of the cytotoxic drug. First generation ADCs made use of early cytotoxins such as the anthracycline, doxorubicin or the anti-metabolite/antifolate agent, methotrexate. Current cytotoxins have far greater potency and can be divided into three main groups: auristatins, maytansines and calicheamicins.

The development of site-specific conjugation methodologies for constructing homogeneous ADCs is an especially promising path to improving ADC design, which will open the way for novel cancer therapeutics.

References:

[1] Tsuchikama K, et al. Protein Cell. 2016 Oct 14. DOI:10.1007/s13238-016-0323-0.

[2] Peters C, et al. Biosci Rep. 2015 Jun 12;35(4). pii: e00225. doi: 10.1042/BSR20150089.

Products for  Signaling Pathways

  1. Cat.No. Product Name Information
  2. GN10814 Quercitrin Quercitrin  Chemical Structure
  3. GN10812 Acacetin Acacetin  Chemical Structure
  4. GN10810 Cordycepin Cordycepin  Chemical Structure
  5. GN10809 Tanshinone IIA sulfonate sodium Tanshinone IIA sulfonate sodium  Chemical Structure
  6. GN10805 Protopanaxdiol Protopanaxdiol  Chemical Structure
  7. GN10804 Isovitexin Isovitexin  Chemical Structure
  8. GN10802 Brazilin Brazilin  Chemical Structure
  9. GN10801 Senkyunolide I Senkyunolide I  Chemical Structure
  10. GN10800 20(S)-NotoginsenosideR2 20(S)-NotoginsenosideR2  Chemical Structure
  11. GN10799 Ginsenoside Rg3 Ginsenoside Rg3  Chemical Structure
  12. GN10797 Tangeretin Tangeretin  Chemical Structure
  13. GN10792 Caffeic acid Caffeic acid  Chemical Structure
  14. GN10791 Catharanthine Catharanthine  Chemical Structure
  15. GN10788 Cucurbitacin IIb Cucurbitacin IIb  Chemical Structure
  16. GN10784 Rhoifolin Rhoifolin  Chemical Structure
  17. GN10783 (R) Ginsenoside Rh2 (R) Ginsenoside Rh2  Chemical Structure
  18. GN10782 Genistin Genistin  Chemical Structure
  19. GN10780 Cephalomannine Cephalomannine  Chemical Structure
  20. GN10779 Reserpine Reserpine  Chemical Structure
  21. GN10778 Picroside II Picroside II  Chemical Structure
  22. GN10776 Obacunone Obacunone  Chemical Structure
  23. GN10768 Leonurine hydrochloride Leonurine hydrochloride  Chemical Structure
  24. GN10764 Homovanillic acid Homovanillic acid  Chemical Structure
  25. GN10762 Gypenoside XLIX Gypenoside XLIX  Chemical Structure
  26. GN10759 Sanggenone C Sanggenone C  Chemical Structure
  27. GN10752 Pachymic acid Pachymic acid  Chemical Structure
  28. GN10751 Dictamnine Dictamnine  Chemical Structure
  29. GN10747 Lannaconitine Lannaconitine  Chemical Structure
  30. GN10745 (+)-Bicuculline (+)-Bicuculline  Chemical Structure
  31. GN10742 Homoharringtonine Homoharringtonine  Chemical Structure
  32. GN10741 Garcinone D Garcinone D  Chemical Structure
  33. GN10740 Tetrahydropalmatine Tetrahydropalmatine  Chemical Structure
  34. GN10737 Tanshinone IIA Tanshinone IIA  Chemical Structure
  35. GN10734 Polyphyllin B Polyphyllin B  Chemical Structure
  36. GN10733 Carnosic acid Carnosic acid  Chemical Structure
  37. GN10732 Oroxin B Oroxin B  Chemical Structure
  38. GN10727 Forsythoside B Forsythoside B  Chemical Structure
  39. GN10720 Gentiopicrin Gentiopicrin  Chemical Structure
  40. GN10718 Andrographolide Andrographolide  Chemical Structure
  41. GN10717 Sanguinarine Sanguinarine  Chemical Structure
  42. GN10716 Epiberberine Epiberberine  Chemical Structure
  43. GN10715 Catharanthine Tartrate Catharanthine Tartrate  Chemical Structure
  44. GN10709 Polyphyllin A Polyphyllin A  Chemical Structure
  45. GN10706 Diosimin Diosimin  Chemical Structure
  46. GN10705 Alantolactone Alantolactone  Chemical Structure
  47. GN10702 Asiatic acid Asiatic acid  Chemical Structure
  48. GN10698 Cynarin Cynarin  Chemical Structure
  49. GN10697 Dehydroandrographolide Dehydroandrographolide  Chemical Structure
  50. GN10696 Garcinone C Garcinone C  Chemical Structure
  51. GN10695 Notoginsenoside R1 Notoginsenoside R1  Chemical Structure
  52. GN10693 Rutin Rutin  Chemical Structure
  53. GN10692 Oridonin Oridonin  Chemical Structure
  54. GN10686 Ginsenoside Rh2 Ginsenoside Rh2  Chemical Structure
  55. GN10685 Anemarsaponin B Anemarsaponin B  Chemical Structure
  56. GN10683 Tanshinone I Tanshinone I  Chemical Structure
  57. GN10681 Sophocarpine Sophocarpine  Chemical Structure
  58. GN10680 Puerarin Puerarin  Chemical Structure
  59. GN10678 Cinnamyl alcohol Cinnamyl alcohol  Chemical Structure
  60. GN10676 Palmitic acid Palmitic acid  Chemical Structure
  61. GN10673 Liquiritigenin Liquiritigenin  Chemical Structure
  62. GN10669 Glucosamine sulfate Glucosamine sulfate  Chemical Structure
  63. GN10668 Coenzyme Q10 Coenzyme Q10  Chemical Structure
  64. GN10667 Calycosin Calycosin  Chemical Structure
  65. GN10666 Isoalantolactone Isoalantolactone  Chemical Structure
  66. GN10664 Honokiol Honokiol  Chemical Structure
  67. GN10663 Coumarin Coumarin  Chemical Structure
  68. GN10662 Cichoric Acid Cichoric Acid  Chemical Structure
  69. GN10654 (+)-Corynoline (+)-Corynoline  Chemical Structure
  70. GN10652 Norisoboldine Norisoboldine  Chemical Structure
  71. GN10650 Ziyuglycoside II Ziyuglycoside II  Chemical Structure
  72. GN10649 Polygalaxanthone III Polygalaxanthone III  Chemical Structure
  73. GN10648 Rosmarinic acid Rosmarinic acid  Chemical Structure
  74. GN10647 Artemisinine Artemisinine  Chemical Structure
  75. GN10646 Engeletin Engeletin  Chemical Structure
  76. GN10645 Jaceosidin Jaceosidin  Chemical Structure
  77. GN10639 Methyl protodioscin Methyl protodioscin  Chemical Structure
  78. GN10638 Artemether Artemether  Chemical Structure
  79. GN10634 Myricetin Myricetin  Chemical Structure
  80. GN10633 Scutellarein Scutellarein  Chemical Structure
  81. GN10632 Betulin Betulin  Chemical Structure
  82. GN10629 5,7-dihydroxychromone 5,7-dihydroxychromone  Chemical Structure
  83. GN10627 Atractylenolide I Atractylenolide I  Chemical Structure
  84. GN10625 7-Epitaxol 7-Epitaxol  Chemical Structure
  85. GN10624 Scutellarin Scutellarin  Chemical Structure
  86. GN10623 Cholic acid Cholic acid  Chemical Structure
  87. GN10622 Shikimic acid Shikimic acid  Chemical Structure
  88. GN10618 Biochanin A Biochanin A  Chemical Structure
  89. GN10616 Timosaponin A3 Timosaponin A3  Chemical Structure
  90. GN10614 Ginsenoside Rg2 Ginsenoside Rg2  Chemical Structure
  91. GN10613 Hesperidin Hesperidin  Chemical Structure
  92. GN10612 (+)- Praeruptorin C (+)- Praeruptorin C  Chemical Structure
  93. GN10609 Coptisine Sulfate Coptisine Sulfate  Chemical Structure
  94. GN10607 Nuciferine Nuciferine  Chemical Structure
  95. GN10605 (+)-Catechin hydrate (+)-Catechin hydrate  Chemical Structure
  96. GN10603 Sennoside B Sennoside B  Chemical Structure
  97. GN10599 Procyanidin B2 Procyanidin B2  Chemical Structure
  98. GN10592 Platycodin D Platycodin D  Chemical Structure
  99. GN10590 Bakuchiol Bakuchiol  Chemical Structure
  100. GN10585 Tetramethylpyrazine Tetramethylpyrazine  Chemical Structure
  101. GN10584 Ginsenoside Rk1 Ginsenoside Rk1  Chemical Structure

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