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Bortezomib

  

Bortezomib is a dipeptide boronic acid analogue with antineoplastic activity. Bortezomib reversibly inhibits the 26S proteasome, a large protease complex that degrades ubiquinated proteins. By blocking the targeted proteolysis normally performed by the proteasome, bortezomib disrupts various cell signaling pathways, leading to cell cycle arrest, apoptosis, and inhibition of angiogenesis. Specifically, the agent inhibits nuclear factor (NF)-kappaB, a protein that is constitutively activated in some cancers, thereby interfering with NF-kappaB-mediated cell survival, tumor growth, and angiogenesis. In vivo, bortezomib delays tumor growth and enhances the cytotoxic effects of radiation and chemotherapy. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

  

MedKoo Code#:  100100

Name:  Bortezomib

CAS#:  179324-69-7

 

Synonym:  Synonym: PS-341.  US brand name: VELCADE. Code names: LDP 341;
MLN341; PS-341.

 

IUPAC/Chemical name:

((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxamido)propanamido)butyl)boronic acid

 

Chemical structure

Theoretical analysis

 

  

MedKoo Code#: 100100
Name:  Bortezomib
CAS#:  179324-69-7

Chemical Formula: C19H25BN4O4

Exact Mass: 384.19689

Molecular Weight: 384.24

Elemental Analysis: C, 59.39; H, 6.56; B, 2.81; N, 14.58; O, 16.66

  

 

 

Availability and price

Bortezomib (99%) is in stock.

25 mg  / $350.00

100 mg / $850.00

For quotation, question, and order, please send email to sales@medkoo.com to describe your needs. A representative will respond your email shortly. We offer significant discount for larger quantity order.

 

Quality control data:

Product will be shipped with supporting analytical data.

 

 

Information about this agent

Bortezomib is "indicated" (recommended) for single-agent use in the treatment of patients with multiple myeloma who have received at least two prior therapies and are progressing on their most recent therapy. Clinical investigations have been completed or are under way to evaluate the safety and efficacy of bortezomib alone or in combination with chemotherapy in multiple myeloma, both at relapse and presentation, as well as in other cancer types.

 

Bortezomib (VELCADE®, formerly PS-341) was approved for the treatment of patients with relapsed or refractory multiple myeloma in May 2003 by the US Food and Drug Administration and in April 2004 by the Committee for Proprietary Medicinal Products of the European Union. In December 2006 the FDA approved Bortezomib for treatment of mantle cell lymphoma.

 

Bortezomib binds to the proteasome and does so "reversibly" (this is a chemical term that means that the bortezomib molecule can come free under different micro-cellular chemical conditions.) Normal healthy (non-cancer) cells are not as prone to damage from this binding after the Bortezomib comes off, as cancer cells are. Malignant cells suffer a breakdown even after inhibition of the proteasome for a short time.

 

According to http://en.wikipedia.org/wiki/Bortezomib, Bortezomib was originally synthesized in 1995 (MG-341) at a company called Myogenics, which soon changed its name to ProScript. After promising preclinical results, the drug (PS-341) was tested in a small Phase I clinical trial on patients with multiple myeloma cancer. ProScript ran out of money and was bought by Leukosite in May 1999. Leukosite in turn was bought by Millennium Pharmaceuticals in October 1999. At this point in time, the project had low priority amongst other projects at the company. This changed significantly when one of the first volunteers to receive the drug in the clinical trial achieved a complete response and was still alive four years later. At the time this was a remarkable result. Later clinical experimentation indicates the possibility of a complete response in 15% of patients in a similar condition, when treated with bortezomib. In May 2003, seven years after the initial synthesis, bortezomib (Velcade) was approved in the United States by the Food and Drug Administration (FDA) for use in multiple myeloma, based on the results from the SUMMIT Phase II trial.

References

Recent publication related to this agent:

1. Pandit, Bulbul; Gartel, Andrei L. New potential anti-cancer agents synergize with bortezomib and ABT-737 against prostate cancer. Prostate (Hoboken, NJ, United States) (2010), 70(8), 825-833. CODEN: PRSTDS ISSN:0270-4137. AN 2010:795910

2. Sonnemann, Juergen; Gressmann, Stephanie; Becker, Sabine; Wittig, Susan; Schmudde, Mareike; Beck, James F. The histone deacetylase inhibitor vorinostat induces calreticulin exposure in childhood brain tumour cells in vitro. Cancer Chemotherapy and Pharmacology (2010), 66(3), 611-616. CODEN: CCPHDZ ISSN:0344-5704. AN 2010:760155

3. Roccaro, Aldo M.; Sacco, Antonio; Aujay, Monette; Ngo, Hai T.; Azab, Abdel Kareem; Azab, Feda; Quang, Phong; Maiso, Patricia; Runnels, Judith; Anderson, Kenneth C.; Demo, Susan; Ghobrial, Irene M. Selective inhibition of chymotrypsin-like activity of the immunoproteasome and constitutive proteasome in Waldenstrom macroglobulinemia. Blood (2010), 115(20), 4051-4060. CODEN: BLOOAW ISSN:0006-4971. AN 2010:725333

4. Lecis, D.; Drago, C.; Manzoni, L.; Seneci, P.; Scolastico, C.; Mastrangelo, E.; Bolognesi, M.; Anichini, A.; Kashkar, H.; Walczak, H.; Delia, D. Novel SMAC-mimetics synergistically stimulate melanoma cell death in combination with TRAIL and Bortezomib. British Journal of Cancer (2010), 102(12), 1707-1716. CODEN: BJCAAI ISSN:0007-0920. AN 2010:710420

5. Zhang, Lidong; Littlejohn, James E.; Cui, Yu; Cao, Xiaobo; Peddaboina, Chander; Smythe, W. Roy. Characterization of bortezomib-adapted I-45 mesothelioma cells. Molecular Cancer (2010), 9 No pp. given. CODEN: MCOACG ISSN:1476-4598. AN 2010:665321

6. Brooks, Alan D.; Jacobsen, Kristen M.; Li, Wenqing; Shanker, Anil; Sayers, Thomas J. Bortezomib Sensitizes Human Renal Cell Carcinomas to TRAIL Apoptosis through Increased Activation of Caspase-8 in the Death-Inducing Signaling Complex. Molecular Cancer Research (2010), 8(5), 729-738. CODEN: MCROC5 ISSN:1541-7786. AN 2010:612515

7. Li, Chunyang; Chen, Shuzhen; Yue, Ping; Deng, Xingming; Lonial, Sagar; Khuri, Fadlo R.; Sun, Shi-Yong. Proteasome Inhibitor PS-341 (Bortezomib) Induces Calpain-dependent I B Degradation. Journal of Biological Chemistry (2010), 285(21), 16096-16104. CODEN: JBCHA3 ISSN:0021-9258. AN 2010:608756

8. Bruna, Jordi; Udina, Esther; Ale, Albert; Vilches, Jorge J.; Vynckier, Ann; Monbaliu, Johan; Silverman, Lee; Navarro, Xavier. Neurophysiological, histological and immunohistochemical characterization of bortezomib-induced neuropathy in mice. Experimental Neurology (2010), 223(2), 599-608. CODEN: EXNEAC ISSN:0014-4886. AN 2010:550282

9. Lee, Sujin; Yagita, Hideo; Sayers, Thomas J.; Celis, Esteban. Optimized combination therapy using bortezomib, TRAIL and TLR agonists in established breast tumors. Cancer Immunology Immunotherapy (2010), 59(7), 1073-1081. CODEN: CIIMDN ISSN:0340-7004. AN 2010:541563

10. Grisendi, Giulia; Bussolari, Rita; Cafarelli, Luigi; Petak, Istvan; Rasini, Valeria; Veronesi, Elena; De Santis, Giorgio; Spano, Carlotta; Tagliazzucchi, Mara; Barti-Juhasz, Helga; Scarabelli, Laura; Bambi, Franco; Frassoldati, Antonio; Rossi, Giulio; Casali, Christian; Morandi, Uliano; Horwitz, Edwin M.; Paolucci, Paolo; Conte, Pier Franco; Dominici, Massimo. Adipose-Derived Mesenchymal Stem Cells as Stable Source of Tumor Necrosis Factor-Related Apoptosis-Inducing Ligand Delivery for Cancer Therapy. Cancer Research (2010), 70(9), 3718-3729. CODEN: CNREA8 ISSN:0008-5472. AN 2010:533421

11. Carozzi, Valentina A.; Chiorazzi, Alessia; Canta, Annalisa; Lapidus, Rena G.; Slusher, Barbara S.; Wozniak, Krystyna M.; Cavaletti, Guido. Glutamate carboxypeptidase inhibition reduces the severity of chemotherapy-induced peripheral neurotoxicity in rat. Neurotoxicity Research (2010), 17(4), 380-391. CODEN: NURRFI ISSN:1029-8428. AN 2010:520015

12. Luo, Peihua; Lin, Meihua; Lin, Meili; Zhu, Difeng; Wang, Zhen; Shen, Jingshan; Yang, Bo; He, Qiaojun. Bortezomib induces apoptosis in human neuroblastoma CHP126 cells. Pharmazie (2010), 65(3), 213-218. CODEN: PHARAT ISSN:0031-7144. AN 2010:510915

13. Russo, A.; Bronte, G.; Fulfaro, F.; Cicero, G.; Adamo, V.; Gebbia, N.; Rizzo, S. Bortezomib: a new pro-apoptotic agent in cancer treatment. Current Cancer Drug Targets (2010), 10(1), 55-67. CODEN: CCDTB9 ISSN:1568-0096. CAN 152:582651 AN 2010:496378

14. Fuchs, Dominik; Daniel, Volker; Sadeghi, Mahmoud; Opelz, Gerhard; Naujokat, Cord. Salinomycin overcomes ABC transporter-mediated multidrug and apoptosis resistance in human leukemia stem cell-like KG-1a cells. Biochemical and Biophysical Research Communications (2010), 394(4), 1098-1104. CODEN: BBRCA9 ISSN:0006-291X. AN 2010:494291

15. Khan, Omar; Fotheringham, Susan; Wood, Victoria; Stimson, Lindsay; Zhang, Chunlei; Pezzella, Francesco; Duvic, Madeleine; Kerr, David J.; La Thangue, Nicholas B. HR23B is a biomarker for tumor sensitivity to HDAC inhibitor-based therapy. Proceedings of the National Academy of Sciences of the United States of America (2010), 107(14), 6532-6537, S6532/1-S6532/2. CODEN: PNASA6 ISSN:0027-8424. CAN 152:583400 AN 2010:478505

16. Sung, Bokyung; Ahn, Kwang Seok; Aggarwal, Bharat B. Noscapine, a Benzylisoquinoline Alkaloid, Sensitizes Leukemic Cells to Chemotherapeutic Agents and Cytokines by Modulating the NF- B Signaling Pathway. Cancer Research (2010), 70(8), 3259-3268. CODEN: CNREA8 ISSN:0008-5472. AN 2010:470279

17. Ouyang, Guifang; Lin, Maofang. Combined effects of bortezomib and daunorubicin on multiple myeloma cell KM3 in vitro. Zhongguo Shiyan Xueyexue Zazhi (2009), 17(6), 1468-1471. CODEN: ZSXZAF ISSN:1009-2137. AN 2010:463340

18. Moriuchi, Makiko; Ohmachi, Ken; Kojima, Minoru; Tsuboi, Kosuke; Ogawa, Yoshiaki; Nakamura, Naoya; Ando, Kiyoshi. Three cases of bortezomib-resistant multiple myeloma with extramedullary masses. Tokai Journal of Experimental and Clinical Medicine (2010), 35(1), 17-20. CODEN: TJEMDR ISSN:0385-0005. AN 2010:453450

19. Rao, Rekha; Nalluri, Srilatha; Kolhe, Ravindra; Yang, Yonghua; Fiskus, Warren; Chen, Jianguang; Ha, Kyungsoo; Buckley, Kathleen M.; Balusu, Ramesh; Coothankandaswamy, Veena; Joshi, Atul; Atadja, Peter; Bhalla, Kapil N. Treatment with Panobinostat Induces Glucose-Regulated Protein 78 Acetylation and Endoplasmic Reticulum Stress in Breast Cancer Cells. Molecular Cancer Therapeutics (2010), 9(4), 942-952. CODEN: MCTOCF ISSN:1535-7163. CAN 152:560313 AN 2010:434958

20. Meregalli, Cristina; Canta, Annalisa; Carozzi, Valentina A.; Chiorazzi, Alessia; Oggioni, Norberto; Gilardini, Alessandra; Ceresa, Cecilia; Avezza, Federica; Crippa, Luca; Marmiroli, Paola; Cavaletti, Guido. Bortezomib-induced painful neuropathy in rats: A behavioral, neurophysiological and pathological study in rats. European Journal of Pain (Oxford, United Kingdom) (2010), 14(4), 343-350. CODEN: EJPAFJ ISSN:1090-3801. AN 2010:434842

21. Genin, E.; Reboud-Ravaux, M.; Vidal, J. Proteasome inhibitors: recent advances and new perspectives in medicinal chemistry. Current Topics in Medicinal Chemistry (Sharjah, United Arab Emirates) (2010), 10(3), 232-256. CODEN: CTMCCL ISSN:1568-0266. CAN 152:516315 AN 2010:423458

22. O'Connor, Owen A.; Portlock, Carol; Moskowitz, Craig; Hamlin, Paul; Straus, David; Gerecitano, John; Gonen, Mithat; Dumitrescu, Otilia; Sarasohn, Debra; Butos, John; Neylon, Ellen; MacGregor Cortelli, Barbara; Blumel, Susan; Evens, Andrew M.; Zelenetz, Andrew D.; Wright, John; Cooper, Brenda; Winter, Jane; Vose, Julie. Time to treatment response in patients with follicular lymphoma treated with bortezomib is longer compared with other histologic subtypes. Clinical Cancer Research (2010), 16(2), 719-726. CODEN: CCREF4 ISSN:1078-0432. AN 2010:419963

23. Paoluzzi, Luca; Scotto, Luigi; Marchi, Enrica; Zain, Jasmine; Seshan, Venkatraman E.; O'Connor, Owen A. Romidepsin and belinostat synergize the antineoplastic effect of bortezomib in mantle cell lymphoma. Clinical Cancer Research (2010), 16(2), 554-565. CODEN: CCREF4 ISSN:1078-0432. AN 2010:419948

24. Haglund, Caroline; Aaleskog, Anna; Hakansson, Lena Douhan; Hoeglund, Martin; Jacobsson, Stefan; Larsson, Rolf; Lindhagen, Elin. The FMCA-GM assays, high throughput non-clonogenic alternatives to CFU-GM in preclinical hematotoxicity testing. Toxicology Letters (2010), 194(3), 102-107. CODEN: TOLED5 ISSN:0378-4274. CAN 152:516424 AN 2010:370092

25. Psallidas, Ioannis; Karabela, Sophia P.; Moschos, Charalampos; Sherrill, Taylor P.; Kollintza, Androniki; Magkouta, Sophia; Theodoropoulou, Panagiota; Roussos, Charis; Blackwell, Timothy S.; Kalomenidis, Ioannis; Stathopoulos, Georgios T. Specific effects of bortezomib against experimental malignant pleural effusion: a preclinical study. Molecular Cancer (2010), 9 No pp. given. CODEN: MCOACG ISSN:1476-4598. AN 2010:368278

26. Albero, M. P.; Vaquer, J. M.; Andreu, E. J.; Villanueva, J. J.; Franch, L.; Ivorra, C.; Poch, E.; Agirre, X.; Prosper, F.; Perez-Roger, I. Bortezomib decreases Rb phosphorylation and induces caspase-dependent apoptosis in Imatinib-sensitive and -resistant Bcr-Abl1-expressing cells. Oncogene (2010), 29(22), 3276-3286. CODEN: ONCNES ISSN:0950-9232. CAN 152:560300 AN 2010:366094

27. Campbell, Richard A.; Sanchez, Eric; Steinberg, Jeffrey; Shalitin, Dror; Li, Zhi-Wei; Chen, Haiming; Berenson, James R. Vorinostat enhances the antimyeloma effects of melphalan and bortezomib. European Journal of Haematology (2010), 84(3), 201-211. CODEN: EJHAEC ISSN:0902-4441. AN 2010:335556

28. Petruzziello, Fara; Zeppa, Pio; Catalano, Lucio; Cozzolino, Immacolata; Gargiulo, Giuseppe; Musto, Pellegrino; D'Auria, Fiorella; Liso, Vincenzo; Rizzi, Rita; Caruso, Nadia; Califano, Catello; Piro, Eugenio; Musso, Maurizio; Bonanno, Vincenza; Pia Falcone, Antonietta; Tafuto, Salvatore; Raimondo, Francesco; Laurentiis, Michelino; Pane, Fabrizio; Palombini, Lucio; Rotoli, Bruno. Amyloid in bone marrow smears of patients affected by multiple myeloma. Annals of Hematology (2010), 89(5), 469-474. CODEN: ANHEE8 ISSN:0939-5555. AN 2010:332295

29. Amschler, Katharina; Schoen, Michael P.; Pletz, Nadin; Wallbrecht, Katrin; Erpenbeck, Luise; Schoen, Margarete. NF- B Inhibition through Proteasome Inhibition or IKK Blockade Increases the Susceptibility of Melanoma Cells to Cytostatic Treatment through Distinct Pathways. Journal of Investigative Dermatology (2010), 130(4), 1073-1086. CODEN: JIDEAE ISSN:0022-202X. AN 2010:326986

30. Casafont, Inigo; Berciano, Maria T.; Lafarga, Miguel. Bortezomib induces the formation of nuclear poly(A) RNA granules enriched in Sam68 and PABPN1 in sensory ganglia neurons. Neurotoxicity Research (2010), 17(2), 167-178. CODEN: NURRFI ISSN:1029-8428. AN 2010:321963

31. Dick, Lawrence R.; Fleming, Paul E. \Building on bortezomib: second-generation proteasome inhibitors as anti-cancer therapy. Drug Discovery Today (2010), 15(5/6), 243-249. CODEN: DDTOFS ISSN:1359-6446. AN 2010:318415

32. Koschny, Ronald; Holland, Heidrun; Sykora, Jaromir; Erdal, Hande; Krupp, Wolfgang; Bauer, Manfred; Bockmuehl, Ulrike; Ahnert, Peter; Meixensberger, Juergen; Stremmel, Wolfgang; Walczak, Henning; Ganten, Tom M. Bortezomib sensitizes primary human esthesioneuroblastoma cells to TRAIL-induced apoptosis. Journal of Neuro-Oncology (2010), 97(2), 171-185. CODEN: JNODD2 ISSN:0167-594X. AN 2010:318328

33. Miller, Susanne C.; Huang, Ruili; Sakamuru, Srilatha; Shukla, Sunita J.; Attene-Ramos, Matias S.; Shinn, Paul; Van Leer, Danielle; Leister, William; Austin, Christopher P.; Xia, Menghang. Identification of known drugs that act as inhibitors of NF- B signaling and their mechanism of action. Biochemical Pharmacology (2010), 79(9), 1272-1280. CODEN: BCPCA6 ISSN:0006-2952. CAN 152:541287 AN 2010:304337

34. Hagenbuchner, Judith; Ausserlechner, Michael J.; Porto, Verena; David, Reinhard; Meister, Bernhard; Bodner, Martin; Villunger, Andreas; Geiger, Kathrin; Obexer, Petra. The Anti-apoptotic Protein BCL2L1/Bcl-xL Is Neutralized by Pro-apoptotic PMAIP1/Noxa in Neuroblastoma, Thereby Determining Bortezomib Sensitivity Independent of Prosurvival MCL1 Expression. Journal of Biological Chemistry (2010), 285(10), 6904-6912. CODEN: JBCHA3 ISSN:0021-9258. CAN 152:397431 AN 2010:252674

35. Kupperman, Erik; Lee, Edmund C.; Cao, Yueying; Bannerman, Bret; Fitzgerald, Michael; Berger, Allison; Yu, Jie; Yang, Yu; Bruzzese, Frank; Liu, Jane; Blank, Jonathan; Garcia, Khristofer; Tsu, Christopher; Dick, Larry; Fleming, Paul; Yu, Li; Manfredi, Mark; Rolfe, Mark; Bolen, Joe. Evaluation of the Proteasome Inhibitor MLN9708 in Preclinical Models of Human Cancer. Cancer Research (2010), 70(5), 1970-1980. CODEN: CNREA8 ISSN:0008-5472. CAN 152:517050 AN 2010:251104

36. Seeger, Jens Michael; Schmidt, Patrick; Brinkmann, Kerstin; Hombach, Andreas A.; Coutelle, Oliver; Zigrino, Paola; Wagner-Stippich, Diana; Mauch, Cornelia; Abken, Hinrich; Kroenke, Martin; Kashkar, Hamid. The Proteasome Inhibitor Bortezomib Sensitizes Melanoma Cells toward Adoptive CTL Attack. Cancer Research (2010), 70(5), 1825-1834. CODEN: CNREA8 ISSN:0008-5472. CAN 152:446019 AN 2010:251089

37. Armstrong, Jane L.; Flockhart, Ross; Veal, Gareth J.; Lovat, Penny E.; Redfern, Christopher P. F. Regulation of endoplasmic reticulum stress-induced cell death by ATF4 in neuroectodermal tumor cells. Journal of Biological Chemistry (2010), 285(9), 6091-6100. CODEN: JBCHA3 ISSN:0021-9258. CAN 152:378285 AN 2010:222084

38. Zhu, Yongqiang; Zhu, Xinrong; Wu, Gang; Ma, Yuheng; Li, Yuejie; Zhao, Xin; Yuan, Yunxia; Yang, Jie; Yu, Sen; Shao, Feng; Li, Runtao; Ke, Yanrong; Lu, Aijun; Liu, Zhenming; Zhang, Liangren. Synthesis, in vitro and in vivo biological evaluation, docking studies, and structure-activity relationship (SAR) discussion of dipeptidyl boronic acid proteasome inhibitors composed of  -amino acids. Journal of Medicinal Chemistry (2010), 53(5), 1990-1999. CODEN: JMCMAR ISSN:0022-2623. CAN 152:358291 AN 2010:199697

39. Pedeboscq, Stephane; L'Azou, Beatrice; Passagne, Isabelle; De Giorgi, Francesca; Ichas, Francois; Liguoro, Dominique; Pometan, Jean-Paul; Cambar, Jean. Anticancer drugs exert differential apoptotic and cytotoxic effects on glioblastoma primary cultures with various EGFR and bcl-2 profiles. Journal of Experimental Therapeutics and Oncology (2009), 8(2), 105-116. CODEN: JETOFX ISSN:1359-4117. AN 2010:192268

40. Gasparetto, Cristina; Gockerman, Jon P.; Diehl, Louis F.; de Castro, Carlos M.; Moore, Joseph O.; Long, Gwynn D.; Horwitz, Mitchell E.; Keogh, George; Chute, John P.; Sullivan, Keith M.; Neuwirth, Rachel; Davis, Patricia H.; Sutton, Linda M.; Anderson, Russell D.; Chao, Nelson J.; Rizzieri, David. "Short course" bortezomib plus melphalan and prednisone as induction prior to transplant or as frontline therapy for nontransplant candidates in patients with previously untreated multiple myeloma. Biology of Blood and Marrow Transplantation (2010), 16(1), 70-77. CODEN: BBMTF6 ISSN:1083-8791. AN 2010:191870

41. Ling, Xiang; Calinski, Diane; Chanan-Khan, Asher A.; Zhou, Muxiang; Li, Fengzhi. Cancer cell sensitivity to bortezomib is associated with survivin and p53 status but not cancer cell types. Journal of Experimental & Clinical Cancer Research (2010), 29 No pp. given. CODEN: JECRDN ISSN:1756-9966. AN 2010:175140

42. Guenterberg, Kristan D.; Grignol, Valerie P.; Raig, Ene T.; Zimmerer, Jason M.; Chan, Anthony N.; Blaskovits, Farriss M.; Young, Gregory S.; Nuovo, Gerard J.; Mundy, Bethany L.; Lesinski, Gregory B.; Carson, William E., III. Interleukin-29 Binds to Melanoma Cells Inducing Jak-STAT Signal Transduction and Apoptosis. Molecular Cancer Therapeutics (2010), 9(2), 510-520. CODEN: MCTOCF ISSN:1535-7163. CAN 152:451922 AN 2010:173813

43. Thomas, Sheeba K.; Richards, Tiffany A.; Weber, Donna M. Novel agents for relapsed and/or refractory multiple myeloma. Cancer Journal (Hagerstown, MD, United States) (2009), 15(6), 485-493. CODEN: CAJOCB ISSN:1528-9117. AN 2010:171336

44. Chauhan, Dharminder; Singh, Ajita V.; Ciccarelli, Bryan; Richardson, Paul G.; Palladino, Michael A.; Anderson, Kenneth C. Combination of novel proteasome inhibitor NPI-0052 and lenalidomide trigger in vitro and in vivo synergistic cytotoxicity in multiple myeloma. Blood (2010), 115(4), 834-845. CODEN: BLOOAW ISSN:0006-4971. AN 2010:165189

45. Di Bella, Nicholas; Taetle, Raymond; Kolibaba, Kathryn; Boyd, Thomas; Raju, Robert; Barrera, David; Cochran, Ernest W., Jr.; Dien, Philip Y.; Lyons, Roger; Schlegel, Peter J.; Vukelja, Svetislava J.; Boston, Julie; Boehm, Kristi A.; Wang, Yunfei; Asmar, Lina. Results of a phase 2 study of bortezomib in patients with relapsed or refractory indolent lymphoma. Blood (2010), 115(3), 475-480. CODEN: BLOOAW ISSN:0006-4971. AN 2010:153313

46. Benson, Don M., Jr.; Panzner, Kathryn; Hamadani, Mehdi; Hofmeister, Craig C.; Bakan, Courtney E.; Smith, Megan K.; Elder, Pat; Krugh, David; O'Donnell, Lynn; Devine, Steven M. Effects of induction with novel agents versus conventional chemotherapy on mobilization and autologous stem cell transplant outcomes in multiple myeloma. Leukemia & Lymphoma (2010), 51(2), 243-251. CODEN: LELYEA ISSN:1042-8194. AN 2010:138845

47. Corso, Alessandro; Barbarano, Luciana; Mangiacavalli, Silvia; Spriano, Mauro; Alessandrino, Emilio P.; Cafro, Anna Maria; Pascutto, Cristiana; Varettoni, Marzia; Bernasconi, Paolo; Grillo, Giovanni; Carella, Angelo M.; Montalbetti, Luigi; Lazzarino, Mario; Morra, Enrica. Bortezomib plus dexamethasone can improve stem cell collection and overcome the need for additional chemotherapy before autologous transplant in patients with myeloma. Leukemia & Lymphoma (2010), 51(2), 236-242. CODEN: LELYEA ISSN:1042-8194. AN 2010:138841

48. Chen, Szu-Ting; Thomas, Simmy; Gaffney, Kevin J.; Louie, Stan G.; Petasis, Nicos A.; Schoenthal, Axel H. Cytotoxic effects of celecoxib on Raji lymphoma cells correlate with aggravated endoplasmic reticulum stress but not with inhibition of cyclooxygenase-2. Leukemia Research (2010), 34(2), 250-253. CODEN: LEREDD ISSN:0145-2126. AN 2010:135366

49. Dimopoulos, Meletios A.; Richardson, Paul G.; Schlag, Rudolf; Khuageva, Nuriet K.; Shpilberg, Ofer; Kastritis, Efstathios; Kropff, Martin; Petrucci, Maria T.; Delforge, Michel; Alexeeva, Julia; Schots, Rik; Masszi, Tamas; Mateos, Maria-Victoria; Deraedt, William; Liu, Kevin; Cakana, Andrew; van de Velde, Helgi; San Miguel, Jesus F. VMP (bortezomib, melphalan, and prednisone) is active and well tolerated in newly diagnosed patients with multiple myeloma with moderately impaired renal function, and results in reversal of renal impairment: cohort analysis of the phase III VISTA study. Journal of Clinical Oncology (2009), 27(36), 6086-6093. CODEN: JCONDN ISSN:0732-183X. AN 2010:122324

50. Lundqvist, Andreas; Su, Su; Rao, Sheila; Childs, Richard. Cutting edge: bortezomib-treated tumors sensitized to NK cell apoptosis paradoxically acquire resistance to antigen-specific T cells. Journal of Immunology (2010), 184(3), 1139-1142. CODEN: JOIMA3 ISSN:0022-1767. CAN 152:303692 AN 2010:105113

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4. Tang, Weiping; Bradner, James Elliot; Schreiber, Stuart L. Deacetylase inhibitors for proliferative diseases therapy. PCT Int. Appl. (2010), 72pp. CODEN: PIXXD2 WO 2010011296 A2 20100128 CAN 152:207088 AN 2010:110311

5. Kalesse, Markus; Malek, Nisar; Frank, Ronald; Brodmann, Tobias; Buelow, Leila; Rentsch, Andreas; Girbig, Anna-Katharina; Eggert, Ulrike. Method for producing intermediates for the production of novel macrocycles that are inhibitors of the proteasomic degradation of p27, such as argyrin and derivatives thereof, and uses of said macrocycles. PCT Int. Appl. (2010), 63pp. CODEN: PIXXD2 WO 2010006682 A1 20100121 CAN 152:184292 AN 2010:84637

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