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NPI-0052
Published Manuscripts
1) Caspase-8 dependent Histone Acetylation by a Novel Proteasome
Inhibitor, NPI-0052: a Mechanism for Synergy in Leukemia cells; C
Miller, S Rudra, M Keating, W Wierda, M Palladino, J Chandra. BLOOD
(113, 4289-4299, 2009).
2) Discovery and Development of the Anticancer Agent Salinosporamide
A (NPI-0052), W. Fenical, P.R. Jensen, M.A. Palladino, K.S. Lam, G.K.
Lloyd, and B.C. Potts: Bioorg. Med. Chem. 2009, 17, 2175-80.
3) Leaving Groups Prolong the Duration of 20S Proteasome Inhibition
and Enhance the Potency of Salinosporamides, R.R. Manam, K.A.
McArthur, T-H. Chao, J. Weiss, J.A. Ali, V.J. Palombella, M. Groll,
G.K. Lloyd, M.A. Palladino, S.T.C. Neuteboom, V.R. Macherla, and
B.C.M. Potts, Journal of Medicinal Chemistry 52, 6711-6724, 2008.
4) Growth of Salinispora tropica Strains CNB440, CNB476, and
NPS21184 in Nonsaline, Low-sodium Media; G. Tsueng and K.S. Lam:
Appl. Microbiol. Biotechnol. 80, 873-880, 2008.
5) Proteasome Inhibition Activates EGFR and EGFR-independent
Mitogenic Kinase Signaling Pathways in Pancreatic Cancer Cells:
Implications for Combination Therapy; C.M. Sloss, F. Wang, R. Liu,
L. Xia, M. Houston, D. Ljungman, M. Palladino, J. Cusack, Jr.
Clinical Cancer Research, 14, 5116-5123, 2008.
6) Inhibition of YY1-Dependent Repressor Activity of DR5
Transcription and Expression by the Novel Proteasome Inhibitor,
NPI-0052, Contributes to its TRAIL-enhanced Apoptosis in Cancer
Cells; S. Baritaki, E. Suzuki, K. Umezawa, D. Spandidos, J.
Berenson, T.R. Daniels, M.L. Penichet, M. Palladino, B. Bonavida; J.
Immunology, 180; 6199-6210, 2008.
7) Dual Targeting of the Proteasome Regulates Survival and Homing in
Waldenstrom Macroglobulinemia; A. Roccaro, X. Jia, A. Sacco, M.
Melhem, A. Moreau, X Leleu, H. Ngo, J. Runels, A. Azab, F. Azab, N.
Burwick, M. Farag, S. Treon, M. Palladino, T. Hideshima, D. Chauhan,
K. Anderson, I. Ghobrial. Blood, 111: 4752-4763, 2008.
8) Combination of Proteasome Inhibitors Bortezomib and NPI-0052
Trigger In Vivo Synergistic Cytotoxicity in Multiple Myeloma; A.
Chauhan, A Singh, M. Brahmandam, K. Podar, T. Hideshima, P.
Richardson, N. Munshi, M. Palladino and K. Anderson. Blood
111:1654-1664, 2008.
9) A Low-Sodium Salt Formulation for the Fermentation of
Salinosporamides by Salinispora Tropica strain NPS21184. G. Tsueng
and K.S. Lam. Appl Microbiol Biotechnol, 78:821-826, 2008.
10) Defined Salt Formulations for the Growth of Salinispora Tropica
Strain NPS21184 and the Production of Salinosporamide A (NPI-0052)
and Related Analogs; G. Tsueng, S. Teisan and K.S Lam. Appl
Microbiol Biotechnol, 78:827-832, 2008.
11) Salinosporamide A (NPI-0052) Potentiates Apoptosis, Suppresses
Osteoclastogenesis, and Inhibitis Invasion Through Downmodulation of
NF kB Regulated Gene Products; K. S. Ahn, G. Sethi, T.H. Chao, S.
Neuteboom, M. Chaturvedi, M. Palladino, A. Younes, and B. Aggarwal;
Blood 110: 2286-2295, 2007.
12) NPI-0052, a Novel Proteasome Inhibitor, Induces Caspase-8 and
ROS Dependent Apoptosis Alone and in Combination with HDAC
Inhibitors in Leukemia Cells; C. Miller, K. Ban, M. Dujka, D.
McConkey, M. Palladino, and J. Chandra: Blood 110: 267-277, 2007.
13) Enantioselective Total Synthesis of (-)-Salinosporamide A
(NPI-0052); T. Ling, V. Macherla, R. Manam, K. McArthur, B. Potts.
Organic Letters, 9:2289-2292, 2007.
14) A Mechanistic and Kinetic Study of the β-Lactone Hydrolysis of
Salinosporamide A (NPI-0052), a Novel Proteasome Inhibitor; N.
Denora, B. Potts and V. Stella. Journal of Pharmaceutical Sciences,
96: 2037-2047, 2007.
15) Stabilization Effect of Resin on the Production of Potent
Proteasome Inhibitor NPI-0052 During Submerged Fermentation of
Salinispora Tropica; G. Tsueng and K.S. Lam. J Antibiotics: 60:
469-472, 2007.
16) Stereoselective Reduction of Keto-Salinosporamide to (-)-Salinosporamide
A (NPI-0052); R. Manam, V. Macherla, and B. Potts. Tetrahedron
Letters, 48: 2537-2540, 2007.
17) Unique Butyric Acid Incorporation Patterns for Salinosporamides
A and B Reveal Distinct Biosynthetic Origins; G. Tsueng, K. Reed, B.
Potts and K. Lam; Applied Microbiology and Biotechnology, 75:
999-1005, 2007.
18) Effect of Halogens on the Production of Salinosporamides by the
Obligate Marine Actinomycete Salinispora tropica; K. Lam, G. Tsueng,
K. Reed, S. Mitchell, B. Potts and J. Xu: J. Antibiotics: 60: 13-19,
2007.
19) Salinosporamides D-J from the Marine Actinomycete Salinispora
Tropica, Bromosalinosporamide and Thioester Derivatives are Potent
Inhibitors of the 20S Proteasome; K. Reed, R. Manam, S. Mitchell, J.
Xu, S. Teisan, T. Chao, G. Yazdi, S. Neuteboom, K. Lam and B. Potts;
J. Natural Products. 70: 269-276, 2007.
20) Crystal Structures of Salinosporamide A (NPI-0052) and B
(NPI-0047) in Complex with the 20S Proteasome Reveal Important
Consequences of β-Lactone Ring Opening and a Mechanism for
Irreversible Binding; M. Groll, R. Huber, and B. Potts: J. American
Chemical Society: 128: 5136-5141, 2006.
21) The Proteasome Inhibitor NPI-0052 is a More Effective Inducer of
Apoptosis than Bortezomib in Lymphocytes from Patients with Chronic
Lymphocytic Leukemia (CLL); S. Ruiz, Y. Krupnik, M. Keating, J.
Chandra, M. Palladino, and D. McConkey: Molecular Cancer
Therapeutics 5(7), 1836-1843, 2006.
22) NPI-0052 Enhances Tumoricidal Response to Conventional Cancer
Therapy in a Colon Cancer Model; J. Cusack, R. Liu, L. Xia, C, Pien,
W. Niu, V. Palombella, T. Chao, S. Neuteboom, and M. Palladino:
Clinical Cancer Research 12(22), 6758-6764, 2006.
23) A Novel Orally Active Proteasome Inhibitor Induces Apoptosis in
Multiple Myeloma Cells with Mechanisms Distinct from Bortezomib; D.
Chauhan, L. Catley, G. Li, K. Podar, T. Hideshima, M. Velankar, C.
Mitsiades, N. Mitsiades, H. Yasui, A. Letai, H. Ovaa, C. Berkers, B.
Nicholson, T. Chao, S. Neuteboom, P. Richardson, M. Palladino, and K
Anderson: Cancer Cell: 8: 407-419, 2005.
24) Structure – Activity Relationship Studies of Salinosporamide A
(NPI-0052), a Novel Marine Derived Proteasome Inhibitor; V. Macherla,
S. Mitchell, R. Manam, K. Reed, T. Chao, B. Nicholson, G.
Deyanat-Yazdi, B. Mai, P. Jensen, W. Fenical, S. Neuteboom, K. Lam,
M. Palladino, and B. Potts: J. Medicinal Chemistry: 48, 3684-3687,
2005.
NPI-0052
Published Abstracts and Posters
1) Clinical Trial of NPI-0052 in Advanced Malignancies Including
Lymphoma and Leukemia (Advanced Malignancies Arm); A.R. Townsend, M.
Millward, T. Price, P. Mainwaring, A. Spencer, A. Longenecker, M.A.
Palladino, G.K. Lloyd, M.A. Spear, P. Padrik: J Clin Oncol 27:15s,
2009 (suppl; abstract #3582)
2) Clinical Trial of the Novel Structure Proteasome Inhibitor
NPI-0052 in Patients with Relapsed and Relapsed/refractory Multiple
Myeloma (rr/MM); C. Hofmeister, P. Richardson, T. Zimmerman, M. A.
Spear, M.A. Palladino, A.M. Longenecker, G. F. Cropp, G.K. Lloyd, A.
L. Hannah, K. Anderson: J. Clin Oncol 27:15s, 2009 (suppl; abstract
#8505)
3) First-in-Human Phase 1 Study of the Novel Structure Proteasome
Inhibitor NPI-0052; P.A. Hamlin, C. Aghajanian, A. Younes, D.S.
Hong, M.A. Palladino, A.M. Longenecker, G.K. Lloyd, A. L. Hannah,
M.A. Spear, R. Kurzrock: J Clin Oncol 27:15s (suppl; abstract #3516)
4) Caspase-8 and Oxidant Dependenet Hyper-Scetylation of Histone-H3
by the Novel Proteasome Inhibitor NPI-0052; C. Miller, S. Rudra, M.
Keating, W. Weirda, M. Palladino, and J. Chandra: AACR (abstract
#5633), Denver, CO April 18-22, 2009
5) Analysis of Reactive Oxygen Species (ROS) Generation and
Caspase-8 Activation by Analogs of Proteasome Inhibitor NPI-0052; R.
Hale, C. Miller, R Manam, V. Macherla, M. Palladino, B. Potts and J.
Chandra: AACR (abstract #5634), Denver, CO, April 18-22, 2009
6) The Proteasome Inhibitor NPI-0052 Inhibitis Metastasis via
Inhibition of SNAIL-Induced EMT and Induction of the Tumor
Metastasis Suppressor RKIP; S. Baritaki, A. Chapman, K. Young, M.
Palladino, B. Bonavida: AACR (abstract #1194), Denver, CO, April
18-22, 2009
7) The Chlorine Leaving Group of the Proteasome Inhibitor NPI-0052
is Key to its Potency, Durability of Proteasome Inhibitiion and May
Influence its Efflux Rate from Tumor Cells; T Chao, B. Wahlgren, A.
Obaidat, J. Weiss, R. Manam, K. McArthur, V. Macherla, M. Palladino,
B. Hagenbuch, B. Potts, S. Enna, G.K. Lloyd, S. Neuteboom: AACR
(abstract #4539), Denver, CO, April 18 - 22, 2009
8) NPI-0052 (2nd Generation Proteasome Inhibitor) Phase 1 Trial in
Patients with Solid Tumors and Lymphomas; R. Kurzrock, P. Hamlin, M.
Gordon, D. Hong, S. Fu, A. Younes, A. Naing, A. Hannah, M. Palladino,
M. Spear, A. Longenecker, S. Neuteboom, G. Cropp, G.K. Lloyd, C.
Aghajanian, ENA-EORTC-AACR, Geneva, Sept 2008
9) Phase 1 Trial of the 2nd Generation Proteasome Inhibitor NPI-0052
in Patients with Advanced Malignancies with CLL and Lymphoma RP2D
Cohorts; A. Townsend, P. Padrik, P. Mainwaring, T. Price, L. Catley,
A. Longenecker, M. Palladino, G.K. Lloyd, G. Cropp, M. Spear, M.
Millward, ENA-EORTC-AACR, Geneva, Sept 2008
10) Clinical Trial of NPI-0052 (2nd generation proteasome inhibitor)
in Patients Having Advanced Malignancies with Expanded RP2D Cohorts
in Lymphoma and CLL; T. Price, P. Padrik, A. Townsend, P.
Mainwaring, L. Catley, A. Longenecker, G. Cropp, M. Palladino, G.K.
Lloyd, M. Spear, M. Millward, ASH (abstract #7446), San Francisco,
Dec, 2008
11) First-in-Human Phase 1 Dose Escalation Study of NPI-0052, a
Novel Proteasome Inhibitor, in Patients with Lymphoma and Solid
Tumor; P. Hamlin, C. Aghajanian, D. Hong, A. Younes, M. Palladino,
A. Longenecker, G. Cropp, G.K. Lloyd, A. Hannah, M. Spear, R.
Kurzrock, ASH (abstract #3913), San Francisco Dec, 2008
12) Phase 1 Study of the Novel Proteasome Inhibitor NPI-0052 in
Patients with Advanced Malignancies Including Leukemias; P. Padrik,
T. Price, M. Spear, A. Townsend, A. Longenecker, M. Palladino, G.K.
Lloyd, G. Cropp, M. Millward, European Society for Medical Oncology,
Geneva, Sept, 2008
13) Leaving Groups Prolong the Duration of 20S Proteasome Inhibition
and Enhance the Inhibition Profile of Salinosporamides. B. Potts, R.
Manam, V. Macherla, T. Chao, J. Weiss, M. Groll, K. McArthur, S.
Neuteboom, M. Palladino, G. K. Lloyd, European Journal of Cancer
Supplements, 6(12), 74 (abstract #237) 2008.
14) Design and Synthesis of Highly Potent Non-Halogen Leaving Group
Analogues of Salinosporamide A (NPI-0052); V. Macherla, R. Manam, K.
McArthur, J. Weiss, Ta-H. Chao, S. Neuteboom and B. Potts. ISMC,
Vienna, Austria, August 2008.
15) The Novel Proteasome Inhibitor NPI-0052 Induces the Expression
of Raf-1 Kinase Inhibitor Protein RKIP) in B-NHL via Inhibition of
the Transcription Repressor Snail: Roles of Snail and RKIP in
Sensitization to TRAIL Apoptosis; S. Baritaki, A. Chapman, K. Wu, K.
Yeung, D. Spandidos, J. Berenson, M. Palladino, B. Bonavida. ASH
(abstract #2611) 2008.
16) Pharmocodynamic and Efficacy Studies of a Novel Proteasome
Inhibitor NPI-0052 in Human Plasmacytoma Xenograft Mouse Model; A.
Singh, G. K. Lloyd, M. Palladino, D. Chauhan and K. Anderson. ASH
(abstract #3665) 2008.
17) Combination of a Novel Proteasome Inhibitor NPI-0052 and
Lenalidomide Trigger in vivo Synergistic Cytotoxicity in Multiple
Myeloma; D. Chauhan, A. V. Singh, G. Bianchi, M. Brahmandam, K.
Podar, T. Hideshima, N. Munshi, P. Richardson, M. Palladino and K.
Anderson. ASH (abstract #3662) 2008.
18) Phase 1 Clinical Trial of NPI-0052, a Novel Proteasome Inhibitor
in Patients with Multiple Myeloma; P. Richardson, C. Hofmeister, T.
Zimmerman, A. Alban Chanankhan, M. Spear, M. Palladino, A.
Longenecker, G.Cropp, G.K. Lloyd, S. Wear, A. Hannah, K. Anderson.
ASH (abstract #277), 2008.
19) Halogen and non-halogen leaving groups enhance the potency of β-lactone
proteasome inhibitors: Further investigation into the role of the
halogen of NPI-0052 (salinosporamide A); T.H Chao, R. R. Manam, B.
Hagenbuch, J. Weiss, K. McArthur, B. Wahlgren, V. Macherla, M. A.
Palladino, S.T.C. Neuteboom, S. J. Enna, G. K. Lloyd, and B. C.
Potts. Ubiquitin and Cancer: From Molecular Targets and Mechanisms
to the Clinic, an AACR Special Conference in Cancer Research,
January 22-25, 2008, San Diego, California (Poster).
20) The Pharmacodynamic Profile of NPI-0052 is Cell-Type Specific;
T. Chao, A. Barral, G. Lloyd, M. Spear, M. Palladino, S. Neuteboom.
AACR (abstract #3257), 2008,
21) Inhibition of Snail-induced EMT and Induction of the Tumor
Metastasis Suppressor/immune Cancer Gene RKIP by the Proteasome
Inhibitor NPI-0052; Roles in Metastasis and Chemo/immunosensitization;
S. Baritaki, K. Yeung, D. Chatterjee, B. Waterman, H. Chen, J.
Berenson, M. Palladino, B. Bonavida. AACR (abstract #2572), 2008
22) Overlapping Functional Activities of Proteasome Inhibitor,
NPI-0052, and HDAC Inhibitors Contribute to Synergistic Cytotoxicity
in Leukemia Cells; C. P. Miller, M. Palladino, J. Chandra. AACR
(abstract #3255), 2008
23) Dual Targeting of the Proteasome Regulates Survival and Homing
in Waldenstrom Macroglobulinemia; A. Roccaro, X. Jia, A. Sacco, M.
Melhem, A. Moreau, X Leleu, H. Ngo, J. Runels, A. Azab, F. Azab, N.
Burwick, M. Farag, S. Treon, M. Palladino, T. Hideshima, D. Chauhan,
K. Anderson, I. Ghobrial. AACR (abstract #3259), 2008
24) Phase 1 Clinical Trials of a Novel Proteasome Inhibitor
(NPI-0052) in Patients with Lymphomas and Solid Tumors; R. Kurzrock,
P. Hamlin, A. Younes, D. Hong, M. Gordon, M. Spear, M. Palladino, G.
K. Lloyd, A. Longenecker, S. Neuteboom, G. Cropp, A. Hannah, C.
Aghajanian. ASH 2007
25) Results from Phase 1 Dose Escalation Study of the Proteasome
Inhibitor NPI 0052 in Patients with Solid Tumors and Lymphomas; R.
Kurzrock, P. Hamlin, A. Younes, D. Hong, M. Gordon, A. Hannah, M.A.
Palladino, G. K. Lloyd, A.M. Longenecker, S.T.C. Neuteboom, G.F.
Cropp, M.A. Spear, C. Aghajanian. In: AACR-NCI-EORTC International
Conference, Molecular Targets and Cancer Therapeutics, 2007 Oct
22-26; San Francisco. CA, p 162. (abstract #B1), 2007.
26) From Sea Bed to Sick Bed: Discovery and Development of a Novel
Proteasome Inhibitor, NPI-0052, from a Marine Actinomycete; K.S.
Lam, Society for Industrial Microbiology, 2007
27) Combination of Proteasome Inhibitors Bortezomib and NPI-0052
Trigger in vivo Synergistic Cytotoxicity in Multiple Myeloma; D.
Chauhan, A. Singh, M. Brahmandam, K. Podar, T. Hideshima, P.
Richardson, N. Munshi, M. Palladino, K. Anderson ; ASH, Annual
Meeting, Blood 110: 2524, 2007.
28) Induction of Raf-1 Kinase Inhibitory Protein (RKIP) by the
Proteasome Inhibitor NPI-0052 and Reversal of B-NHL Resistance to
Apoptosis; S. Baritaki, K. Yeung, D. Chatterjee, M. Palladino, B.
Bonavida; ASH, Annual Meeting, Blood 110: 809, 2007.
29) Targeting Cdk4/6 in Combination Therapy Overcomes proteasome
Inhibitor Resistance in Multiple Myeloma Through Synergistic
Mitochondria Depolarization; X. Huang, T. Louie, M. Di Liberto, J.
Rice, D. Jayabalan, K. Zhang, M. Palladino, I. Chen, P. Toogood, R.
Niesvizky, M. A. S. Moore, S. Chen-Kiang; ASH, Annual Meeting, Blood
110: 667, 2007.
30) The Combination of Bortezomib and NPI-0052 Exerts Anti-Tumor
Activity in Waldenstrom Macroglobulinemia; A. Roccaro, X. Leleu, A-S
Moreau, X. Jia, A. Sacco, H. Ngo, A. Azab, F. Azab, E. Hatjiharissi,
S. Treon, T. Hideshima, M. Palladino, K. Anderson, D. Chauhan, I.
Ghobrial, ASH, Annual Meeting, Blood 110: 1516, 2007.
31) Lyophilization Development of NPI-0052 (Salinosporamide A) in
Water/tert-Butyl Alcohol Co-solvent System; J.J. Chu, C. Billstrom,
N. Reddinger, B. Mai, R. Singh and B.C.M. Potts. American
Association of Pharmaceutical Scientists (AAPS) Annual Meeting and
Exposition, November 11 – 15, 2007.
32) A Novel Parenteral Formulation Design for NPI-0052 (Salinosporamide
A), a β-Lactone Proteasome Inhibitor; J.J. Chu, C. Billstrom, N.
Reddinger, B. Mai, R. Singh and B.C.M. Potts. American Association
of Pharmaceutical Scientists (AAPS) Annual Meeting and Exposition,
November 11 – 15, 2007.
33) Stability Studies of Various Lyophilized Formulations and Dosing
Solutions of NPI-0052, a Potent 20S Proteasome Inhibitor, to Support
Parenteral Drug Product Development; N. Reddinger, B. Mai, C.
Billstrom, J.J. Chu, R. Singh, and B.C.M. Potts. American
Association of Pharmaceutical Scientists (AAPS) Annual Meeting and
Exposition, November 11 – 15, 2007.
34) A High Performance Liquid Chromatography (HPLC) Method for
Quantitative Determination of NPI-0052 (Salinosporamide A) to
Support Lyophilized Parenteral Drug Product Development; B. Mai, N.
Reddinger, J.J. Chu, R. Singh, and B. Potts. American Association of
Pharmaceutical Scientists (AAPS) Annual Meeting and Exposition,
November 11 – 15, 2007.
35) High Performance Liquid Chromatography Method Development for
Quantitation of NPI-0052 in Formulated Drug Product with
Polyvinylpyrrolidone as Excipient and Comparative Study of
Evaporative Light Scattering vs. Ultra Violet Detection; R. Singh,
N. Reddinger, B. Mai, J. Chu and B. Potts; 31st International
Symposium on High Performance Liquid Phase Separations and Related
Techniques (HPLC 2007), June 17 – 21, Ghent, Belgium,
36) Pharmaceutical Development of a Parenteral Formulation of
NPI-0052 (Salinosporamide A), a Novel Proteasome Inhibitor; R.
Singh, B. Mai, C. Billstrom, M. Palladino, and B. Potts: American
Pharmacists Association (APhA) Annual Meeting and Exposition March
16 – 19, Atlanta, GA, 2007.
37) Enantioselective Total Synthesis of (-)-Salinosporamide A
(NPI-0052) and Analogues; T. Ling, V. Macherla, R. Manam, K.
McArthur, and B. Potts. ASME, 2007.
38) Enantioselective Total Synthesis of (-)-Salinosporamide A
(NPI-0052) and Analogues; T. Ling, V. Macherla, R. Manam, K.
McArthur, and B. Potts. ACS, Boston, 2007.
39) Enantioselective Total Synthesis of (-)-Salinosporamide A
(NPI-0052) and Analogues; T. Ling, V. Macherla, R. Manam, K.
McArthur, and B. Potts. ASP, July, 2007.
40) Progress Towards an Enantioselective Total Synthesis of (-)-Salinosporamide
A (NPI-0052); T. Ling, V. Macherla, R. Manam, K. McArthur, and B.
Potts: AACR/ACS Meeting, San Diego, CA, February, 2007.
41) Stereoselective Enzymatic Conversion of Keto-Salinosporamide to
Salinosporamide A (NPI-0052); R. Manam, V. Macherla, and B. Potts:
AACR/ACS Meeting, San Diego, CA. February, 2007.
42) The Novel Proteasome Inhibitor, NPI-0052, Synergizes with HDAC
Inhibitors to Trigger Apoptosis in Leukemia Cells; C. Miller and J.
Chandra, AACR, Annual Meeting, Proceedings Abstract #2486, 2007.
43) Rituximab-Mediated Sensitization of Resistant B-NHL Cell Lines
to the Proteasome Inhibitor NPI-0052 -Induced Apoptosis: Pivotal
Role of PTEN Induction and Inhibition of Bcl-xL; E. Suzuk, M.
Palladino, and B. Bonavida, AACR, Annual Meeting, Proceedings
Abstract #1453, 2007.
44) Sensitization of B-NHL Resistant Tumor Cells Overexpressing
Bcl-xL to TRAIL-Induced Apoptosis by the Novel Proteasome Inhibitor
Salinosporamide A (NPI-0052); E. Suzuk, M. Palladino, G. Cheng and
B. Bonavida. AACR, Annual Meeting, Proceedings Abstract 1445, 2007.
45) Proteasome Inhibitor NPI-0052 Exhibits a Distinct Biological
Profile Compared to Non-leaving Group Analogs; B. Potts, T. Chao, J.
Ali, A. Singh, R. Singh, S. Neuteboom, V. Palombella, D. Chauhan, K.
Anderson and M. Palladino. AACR, Annual Meeting, Proceedings
Abstract #4948, 2007.
46) A Novel Proteasome Inhibitor, NPI-0052 is Active in Hodgkin and
Mantle Cell Lymphoma Cell Lines; D. Buglio, G. Georgakis, V. Yazbeck,
T. Chao, S. Neuteboom, M. Palladino, and A. Younes. AACR, Annual
Meeting, Proceedings Abstract #1454, 2007.
47) The Proteasome Inhibitor NPI-0052 Reduces Tumor Growth and
Overcomes Resistance of Prostate Cancer to rhTRAIL via Inhibition of
the NF-kB Pathway; A. Barral, T. Chao, S. Kanabolooki, G.
Deyanat-Yazdi, B. Nicholson, D. McConkey, M. Palladino, and S.
Neuteboom. AACR, Annual Meeting, Proceedings Abstract #1465, 2007.
48) Novel NF-B Inhibitors NPI-1342/NPI-1387 and Proteasome
Inhibitor NPI-0052 Overcome Resistance of Pancreatic Carcinoma to
rhTRAIL; S. Khanbolooki, S. Pino, R. Andtbacka, T. Chao, S.
Neuteboom, M. Palladino, D. McConkey. AACR, 2006.
49) The Proteasome Inhibitor NPI-0052 Sensitizes Pancreatic Cancer
Cells to TRAIL In Vitro and In Vivo; R. Andtbacka, S. Khanbolooki,
M. Pino, K. Zhu, and D. McConkey: AACR, 2006.
50) Rituximab Sensitizes Resistant B-NHL Cell Lines to the
Proteasome Inhibitor NPI-0052 – Induced Apoptosis; E. Suzuki, MB.
Bonavida; AACR, 2006.
51) Salinosporamide A, a Novel Orally Active Proteasome Inhibitor
NPI-0052 Enhances Tumoricidal Response to Multidrug Chemo-and
Molecular Therapy Regimens in a Pancreatic Cancer Xenograft Model;
J. Cusack, R. Liu, L. Xia, S. Neuteboom, and M. Palladino: ASCO,
2006.
52) Inhibition of the Pan-Bcl-2 Family by the Small Molecule
GX15-070 Induces Apoptosis in Mantle Cell Lymphoma (MCL) Cells and
Enhances the Activity of Two Proteasome Inhibitors (NPI-0052 and
Bortezomib) and Doxorubicin Chemotherapy; V. Yazbeck, G. Georgakis,
Y. Li., D. McConkey, M. Andreeff, and A. Younes: ASH, 2006.
53) Induction of RKIP and Inhibition of the Transcription Repressor
YY1 in B-NHL by the Novel Proteasome Inhibitor NPI-0052 and
Sensitization to TRAIL-Induced Apoptosis; E. Suzuki, S. Huerta-Yepez,
S. Baritaki, M. Palladino, and B. Bonavida: ASH, 2006.
54) The Proteasome Inhibitor NPI-0052 in Combination with Bortezomib
Induces Antitumor Activity in Waldenstrom’s Macroblobulinemia; X.
Jia, XLeleu, A. Moreau, E. Hatjiharisi, H. Ngo, G. O’Sullivan, J.
Runnels, D. McMillin, S. Treon, C. Mitsiades, T. Hideshima, M.
Palladino, K. Anderson, D. Chauhan and I. Ghobrial ASH, 2006.
55) NPI-0052 (Salinosporamide A) is a Potent, Novel Proteasome
Inhibitor that enhances the Tumoricidal Response to Conventional
Multidrug Chemo – and Molecular Therapy in a Colon Cancer Xenograft
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