From Plant to Patient: Thapsigargin, a Tool for Understanding …
109
165. Coats S, Williams M, Kebble B, Dixit R, Tseng L, Yao N-S, Tice DA, Soria J-C (2019)
Antibody-drug conjugates: future directions in clinical and translational strategies to improve
the therapeutic index. Clin Cancer Res 25:5441
166. Nicolaou KC, Rigol S (2019) Total synthesis in search of potent antibody-drug conjugate
payloads. From the fundamentals to the translational. Acc Chem Res 52:127
167. Halford B (2020) Antibody-drug conjugates make a comeback. Chem Eng News 98:16
168. Denmeade SR, Isaacs JT (2005) The SERCA pump as a therapeutic target: making a “smart
bomb” for prostate cancer. Cancer Biol Ther 4:14
169. Balk SP, Ko YJ, Bubley GJ (2003) Biology of prostate-specific antigen. J Clin Oncol 21:383
170. Lilja H (2003) Biology of prostate-specific antigen. Urology 62(Suppl 1):27
171. Denmeade SR, Nagy A, Gao J, Lilja H, Schally AV, Isaacs JT (1998) Enzymatic activation
of a doxorubicin-peptide prodrug by prostate-specific antigen. Cancer Res 58:2537
172. Brady SF, Pawluczyk JM, Lumma PK, Feng DM, Wai JM, Jones R, Feo-Jones D, Wong BK,
Miller-Stein C, Lin JH, Oliff A, Freidinger RM, Garsky VM (2002) Design and synthesis of
a pro-drug of vinblastine targeted at treatment of prostate cancer with enhanced efficacy and
reduced systemic toxicity. J Med Chem 45:4706
173. Denny WA (2006) Deoxyribonucleic acid topoisomerase inhibitors. Compr Med Chem II
7:111
174. Darson MF, Pacelli A, Roche P, Rittenhouse HG, Wolfert RL, Young CY, Klee GG,
Tindall DJ, Bostwick DG (1997) Human glandular kallikrein 2 (hK2) expression in prostatic
intraepithelial neoplasia and adenocarcinoma: a novel prostate cancer marker. Urology 49:857
175. Darson MF, Pacelli A, Roche P, Rittenhouse HG, Wolfert RL, Saeid MS, Young CY, Klee
GG, Tindall J, Bostwick DG (1999) Human glandular kallikrein 2 expression in prostate
adenocarcinoma and lymph node metastases. Urology 53:939
176. Janssen S, Rosen DM, Ricklis RM, Dionne CA, Lilja H, Christensen SB, Isaacs JT, Denmeade
SR (2006) Pharmacokinetics, biodistribution, and antitumor efficacy of a human glandular
kallikrein 2 (hK2)-activated thapsigargin prodrug. Prostate 66:358
177. Pinto JT, Suffoletto BP, Berzin TM, Qiao CH, Lin S, Tong WP, May F, Mukherjee B, Heston
WDW (1996) Prostate-specific membrane antigen: a novel folate hydrolase in human prostatic
carcinoma cells. Clin Cancer Res 2:1445
178. Wang H-L, Wang S-S, Song W-H, Pan Y, Yu H-P, Si T-G, Liu Y, Cui X-N, Guo Z (2015) Expression of prostate-specific membrane antigen in lung cancer cells and tumor neovasculature
endothelial cells and its clinical significance. PLoS One 10:e0125924
179. Nomura N, Pastorino S, Jiang P, Lambert G, Crawford JR, Gymnopoulos M, Piccioni D,
Juarez T, Pingle SC, Makale M, Kesari S (2014) Prostate specific membrane antigen (PSMA)
expression in primary gliomas and breast cancer brain metastases. Cancer Cell Int 14:26
180. Kasoha M, Unger C, Solomayer E-F, Bohle RM, Zaharia C, Khreich F, Wagenpfeil S, JuhaszBoess I (2017) Prostate-specific membrane antigen (PSMA) expression in breast cancer and
its metastases. Clin Exp Metast 34:479
181. Nimmagadda S, Pullambhatla M, Chen Y, Parsana P, Lisok A, Chatterjee S, Mease R, Rowe
SP, Lupold S, Pienta KJ, Pomper MG (2018) Low-level endogenous PSMA expression in
nonprostatic tumor xenografts is sufficient for in vivo tumor targeting and imaging. J Nucl
Med 486
182. Periasamy M, Kalyanasundaram A (2007) Serca pump isoforms: their role in calcium transport
and disease. Muscle Nerve 35:430
183. Casemore D, Xing X (2015) SERCA as target for cancer therapies. Int Cancer Sci Ther 2:100
184. Michelangeli F, East JM (2011) A diversity of SERCA Ca 2+ pump inhibitors, recent advances
in membrane biochemistry. Biochem Soc Symp 78:131
185. Chin TY, Lin HC, Kuo JP, Chueh SH (2007) Dual effect of thapsigargin on cell death in
porcine aortic smooth muscle cells. Am J Physiol Cell Physiol 292:C383
186. Toyoshima C, Nakasako M, Nomura H, Ogawa H (2000) Crystal structure of the calcium
pump of the of sarcoplasmic reticulum at 2.6 Å resolution. Nature 405:647
187. Bublitz M, Morth JP, Nissen P (2011) P-type ATPases at a glance. J Cell Sci 124:2515
109
165. Coats S, Williams M, Kebble B, Dixit R, Tseng L, Yao N-S, Tice DA, Soria J-C (2019)
Antibody-drug conjugates: future directions in clinical and translational strategies to improve
the therapeutic index. Clin Cancer Res 25:5441
166. Nicolaou KC, Rigol S (2019) Total synthesis in search of potent antibody-drug conjugate
payloads. From the fundamentals to the translational. Acc Chem Res 52:127
167. Halford B (2020) Antibody-drug conjugates make a comeback. Chem Eng News 98:16
168. Denmeade SR, Isaacs JT (2005) The SERCA pump as a therapeutic target: making a “smart
bomb” for prostate cancer. Cancer Biol Ther 4:14
169. Balk SP, Ko YJ, Bubley GJ (2003) Biology of prostate-specific antigen. J Clin Oncol 21:383
170. Lilja H (2003) Biology of prostate-specific antigen. Urology 62(Suppl 1):27
171. Denmeade SR, Nagy A, Gao J, Lilja H, Schally AV, Isaacs JT (1998) Enzymatic activation
of a doxorubicin-peptide prodrug by prostate-specific antigen. Cancer Res 58:2537
172. Brady SF, Pawluczyk JM, Lumma PK, Feng DM, Wai JM, Jones R, Feo-Jones D, Wong BK,
Miller-Stein C, Lin JH, Oliff A, Freidinger RM, Garsky VM (2002) Design and synthesis of
a pro-drug of vinblastine targeted at treatment of prostate cancer with enhanced efficacy and
reduced systemic toxicity. J Med Chem 45:4706
173. Denny WA (2006) Deoxyribonucleic acid topoisomerase inhibitors. Compr Med Chem II
7:111
174. Darson MF, Pacelli A, Roche P, Rittenhouse HG, Wolfert RL, Young CY, Klee GG,
Tindall DJ, Bostwick DG (1997) Human glandular kallikrein 2 (hK2) expression in prostatic
intraepithelial neoplasia and adenocarcinoma: a novel prostate cancer marker. Urology 49:857
175. Darson MF, Pacelli A, Roche P, Rittenhouse HG, Wolfert RL, Saeid MS, Young CY, Klee
GG, Tindall J, Bostwick DG (1999) Human glandular kallikrein 2 expression in prostate
adenocarcinoma and lymph node metastases. Urology 53:939
176. Janssen S, Rosen DM, Ricklis RM, Dionne CA, Lilja H, Christensen SB, Isaacs JT, Denmeade
SR (2006) Pharmacokinetics, biodistribution, and antitumor efficacy of a human glandular
kallikrein 2 (hK2)-activated thapsigargin prodrug. Prostate 66:358
177. Pinto JT, Suffoletto BP, Berzin TM, Qiao CH, Lin S, Tong WP, May F, Mukherjee B, Heston
WDW (1996) Prostate-specific membrane antigen: a novel folate hydrolase in human prostatic
carcinoma cells. Clin Cancer Res 2:1445
178. Wang H-L, Wang S-S, Song W-H, Pan Y, Yu H-P, Si T-G, Liu Y, Cui X-N, Guo Z (2015) Expression of prostate-specific membrane antigen in lung cancer cells and tumor neovasculature
endothelial cells and its clinical significance. PLoS One 10:e0125924
179. Nomura N, Pastorino S, Jiang P, Lambert G, Crawford JR, Gymnopoulos M, Piccioni D,
Juarez T, Pingle SC, Makale M, Kesari S (2014) Prostate specific membrane antigen (PSMA)
expression in primary gliomas and breast cancer brain metastases. Cancer Cell Int 14:26
180. Kasoha M, Unger C, Solomayer E-F, Bohle RM, Zaharia C, Khreich F, Wagenpfeil S, JuhaszBoess I (2017) Prostate-specific membrane antigen (PSMA) expression in breast cancer and
its metastases. Clin Exp Metast 34:479
181. Nimmagadda S, Pullambhatla M, Chen Y, Parsana P, Lisok A, Chatterjee S, Mease R, Rowe
SP, Lupold S, Pienta KJ, Pomper MG (2018) Low-level endogenous PSMA expression in
nonprostatic tumor xenografts is sufficient for in vivo tumor targeting and imaging. J Nucl
Med 486
182. Periasamy M, Kalyanasundaram A (2007) Serca pump isoforms: their role in calcium transport
and disease. Muscle Nerve 35:430
183. Casemore D, Xing X (2015) SERCA as target for cancer therapies. Int Cancer Sci Ther 2:100
184. Michelangeli F, East JM (2011) A diversity of SERCA Ca 2+ pump inhibitors, recent advances
in membrane biochemistry. Biochem Soc Symp 78:131
185. Chin TY, Lin HC, Kuo JP, Chueh SH (2007) Dual effect of thapsigargin on cell death in
porcine aortic smooth muscle cells. Am J Physiol Cell Physiol 292:C383
186. Toyoshima C, Nakasako M, Nomura H, Ogawa H (2000) Crystal structure of the calcium
pump of the of sarcoplasmic reticulum at 2.6 Å resolution. Nature 405:647
187. Bublitz M, Morth JP, Nissen P (2011) P-type ATPases at a glance. J Cell Sci 124:2515
