TY - CHAP
T1 - Drug Discovery and Development for Kinetoplastid Diseases
AU - Caffrey, Conor R.
AU - Steverding, Dietmar
AU - Ferreira, Rafaela S.
AU - de Oliveira, Renata B.
AU - O'Donoghue, Anthony J.
AU - Monti, Ludovica
AU - Ballatore, Carlo
AU - Bachovchin, Kelly A.
AU - Ferrins, Lori
AU - Pollastri, Michael P.
AU - Zorn, Kimberley M.
AU - Foil, Daniel
AU - Clark, Alex M.
AU - Mottin, Melina
AU - Andrade, Carolina H.
AU - de Siqueira-Neto, Jair L.
AU - Ekins, Sean
PY - 2021/4/26
Y1 - 2021/4/26
N2 - We review the disease, biology and biochemistry of kinetoplastids, as well as the new drugs and drug candidates that have entered the clinic in the last decade. We also describe examples of the pre-clinical exploration of small molecules against various protein targets, (e.g., cysteine proteases, the proteasome and tubulin), as well as cutting-edge molecular and computational strategies, and technologies being brought to bear to discover and develop new anti-trypanosomal drugs. For comprehensive descriptions of the disease, biology and drug therapies prior to 2011, the reader is encouraged to review the chapter by P. M. Woster that appeared in 2010 in the seventh edition of Burger’s Medicinal Chemistry, Drug Discovery, and Development, with the title Antiprotozoal/Antiparasitic Agents.
AB - We review the disease, biology and biochemistry of kinetoplastids, as well as the new drugs and drug candidates that have entered the clinic in the last decade. We also describe examples of the pre-clinical exploration of small molecules against various protein targets, (e.g., cysteine proteases, the proteasome and tubulin), as well as cutting-edge molecular and computational strategies, and technologies being brought to bear to discover and develop new anti-trypanosomal drugs. For comprehensive descriptions of the disease, biology and drug therapies prior to 2011, the reader is encouraged to review the chapter by P. M. Woster that appeared in 2010 in the seventh edition of Burger’s Medicinal Chemistry, Drug Discovery, and Development, with the title Antiprotozoal/Antiparasitic Agents.
U2 - 10.1002/0471266949.bmc235.pub2
DO - 10.1002/0471266949.bmc235.pub2
M3 - Chapter (peer-reviewed)
SN - 978-1-119-53030-5
VL - 7
SP - 255
EP - 344
BT - Burger's Medicinal Chemistry, Drug Discovery and Development
A2 - Abraham, Donald J.
A2 - Myers, Michael
PB - Wiley
CY - New York
ER -