Scientific and Medical Publications

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Cardiovascular | Skeletal | Smooth | Oncology | Other

Cardiovascular

Greenberg BH, Chou W, Saikali KG, Escandon R, Lee JH, Chen MM, Malik F, Wolff AA, Shaburishvili T. Phase II Safety Study Evaluating the Novel Cardiac Myosin Activator, CK-1827452, in Patients with Ischemic Cardiomyopathy and Angina. 2009 Heart Failure Society of America Annual Meeting (HFSA), Boston, MA. September 2009. Poster presentation

Goldman JH, Teerlink JR, Saikali KG, Malik F, Wolff AA. Echocardiographic Detection of Increases in Ejection Fraction in Patients with Heart Failure Receiving the Selective Cardiac Myosin Activator, CK-1827452. 2009 Heart Failure Society of America Annual Meeting (HFSA), Boston, MA. September 2009. Poster presentation

Malik FI, Saikali KG, Chen MM, Lee JH, Goldman JH. An Analysis of the Response to CK-1827452, a Selective Cardiac Myosin Activator, in Stable Heart Failure Patients Stratified by Baseline Cardiac Function. 2009 Heart Failure Society of America Annual Meeting(HFSA), Boston, MA. September 2009. Poster presentation

Greenberg BH, Chou W, Saikali KG, Escandon R, Lee JH, Chen MM, Malik F, Wolff AA, Shaburishvili T. Phase II Safety Study Evaluating the Novel Cardiac Myosin Activator, CK-1827452, in Patients with Ischemic Cardiomyopathy and Angina. European Society of Cardiology (ESC) Congress 2009, Barcelona, Spain. August 2009. Poster presentation

Goldman JH, Teerlink JR, Saikali KG, Malik F, Wolff AA. Echocardiographic Detection of Increases in Ejection Fraction in Patients with Heart Failure Receiving the Selective Cardiac Myosin Activator, CK-1827452. European Society of Cardiology (ESC) Congress 2009, Barcelona, Spain. August 2009. Poster presentation

Goldman JH, Teerlink JR, Saikali KG, Malik F and Wolff AA. Echocardiographic Detection of Increases in Ejection Fraction in Patients with Heart Failure Receiving the Selective Cardiac Myosin Activator, CK-1827452. 2009 European Society of Cardiology, Heart Failure Congress, Nice, France. June 2009. Poster presentation

Greenberg BH, Chou W, Saikali KG, Escandon R, Lee JH, Chen MM, Malik F, Wolff AA, Shaburishvili T, and the CY 1221 Investigators. Phase II Safety Study Evaluating the Novel Cardiac Myosin Activator, CK-1827452, in Patients with Ischemic Cardiomyopathy and Angina. 2009 European Society of Cardiology, Heart Failure Congress, Nice, France. June 2009. Poster presentation

Senior R, Malik FI, Saikali KG, Lee JH, Chen MM, Brand G, Wolff AA, and the CY 1121 Investigators. The Selective Cardiac Myosin Activator, CK-1827452, Increases Systolic Function in a Concentration-Dependent Manner in Patients with Stable Heart Failure. 2009 Annual American College of Cardiology (ACC), Orlando, FL. March 2009. Poster presentation

Teerlink John R. A novel approach to improve cardiac performance: cardiac myosin activators.
Heart Failure Reviews, February 21, 2009. Article and Link to Website

Parker JD, Michaels AD, Kass DA, Wolff AA, Felker GM and Malik FI. Rationale and Design for a Phase II Study Evaluating the Effect of the Cardiac Myosin Activator, CK-1827452, on Cardiac Function, Hemodynamics, and Myocardial Oxygen Consumption in Patients with Heart Failure. 2008 Annual Heart Failure Society of America (HFSA) Conference. Toronto, Ontario, Canada. September 2008. Poster presentation

Cleland JGF, et al. First Clinical Trial of the Selective Cardiac Myosin Activator, CK-1827452, in Heart Failure: Effect of Dose and Plasma Concentration on Systolic Function. European Society of Cardiology (ESC) Congress 2008. August, 2008. Poster presentation

Shen Y, Zhang Y, Morgans DJ, Vatner SF, Malik F. A Novel Inotropic Agent That Activates Cardiac Myosin and Increases Cardiac Contractility Without Increasing MVO2 in Heart Failure with Left Ventricular Hypertrophy. American College of Cardiology Conference, Chicago, IL. March, 2008. Poster presentation

Anderson RL, Pokrovskii M, Suekawa K, Rodriguez HM, Elias, KA. The Cardiac Myosin Activator CK-1827452-Induced Myocyte Contractility is Unchanged in the Presence of β-Blockade. 2007 American Society of Cell Biology (ASCB) Conference, Washington, DC. December, 2007. Poster presentation

Jerling M, Chew T, Escandon R, Lee J, Saikali K, Venables E, Clarke C, Malik F, Wolff A. Oral Bioavailability of the Selective Cardiac Myosin Activator CK-1827452: Chronic Oral Inotropic Therapy for Heart Failure. 2007 Annual Heart Failure Society of America Meeting, Washington, DC. September, 2007. Poster presentation

Malik FI, Saikali KG, Clarke CP, Teerlink JR, Wolff AA. Systolic Ejection Time is a Sensitive Indicator of Left Ventricular Systolic Function During Treatment with the Selective Cardiac Myosin Activator, CK-1827452. 2007 Annual Heart Failure Society of America Meeting, Washington, DC. September, 2007. Poster presentation

Anderson R, Pokrovskii M, Elias K. Effects of Cardiac Myosin Activators on Excitation-Contraction (E-C) Coupling in Ventricular Myocytes. Biophysical Society 51st Annual Meeting, Baltimore, MD. March, 2007. Poster presentation

Rodriguez H, Kawas R, Malik F, Sakowicz R, Hartman J. The Cardiac Myosin Activator, CK-1827452, Accelerates the Enzymatic Step Gating Entry of Myosin into its Force Generating State. Biophysical Society 51st Annual Meeting, Baltimore, MD. March, 2007. Poster presentation

Anderson RL, Pokrovskii M, Elias KA. Effects of the Cardiac Myosin Activator CK-1316719 on Excitation-Contraction (E-C) Coupling in Ventricular Myocytes. 46th Annual American Society for Cell Biology Meeting, San Diego, CA. December, 2006. Poster presentation

Baliga R, Rodriguez HM, Guo D, Hartman JJ, Pierce DW, Sakowicz R, Morgan BP, Malik F, Finer JT. A Sensitive Assay for the Basal ATPase Activity of Cardiac Myosin. Society of Biomolecular Sciences Annual Meeting, Seattle (September 2006). Poster presentation

Anderson RL, Kawas RF, Pokrovskii MV, Godinez G, Lee KH, Mak J, Hartman JJ, Morgan BP, Morgans Jr., DJ, Malik F, Sakowicz R, Elias KA. Cardiac Myosin Activator CK-1316719 Increases Myofibril ATPase Activity and Myocyte Contractility in a Rat Model of Heart Failure. Heart Failure Society of America (HFSA), September, 2006. Poster presentation

Shen YT, Vatner SF, Morgans DJ, Malik F. Activating Cardiac Myosin, a Novel Inotropic Mechanism to Improve Cardiac Function in Conscious Dogs with Congestive Heart Failure. Heart Failure Society of America (HFSA), September, 2006. Poster presentation

Anderson RL, Sueoka SH, Lee KH, Rodriguez HM, Kawas R, Godinez G, Morgan BP, Sakowicz R, Morgans Jr, DJ, Malik F, Elias KA. In Vitro and In Vivo Characterization CK-1827452, a Selective Cardiac Myosin Activator. Heart Failure Society of America (HFSA), September, 2006. Poster presentation

Rodriguez HM, Sylvester S, Kawas R, Malik F, Sakowicz R. Activation of the Cardiac Sarcomere by a Small Molecule Agent, CK-1213296. Biophysical Society Annual Meeting. February, 2006. Poster presentation

Rodriguez HM, Sylvester S, Hartman J, Shen YT, Kass DA, Vatner SF, Malik F, Sakowicz R. A Detailed Kinetic Analysis of the Cardiac Myosin Activator, CK-1213296, Suggests It Improves Cardiac Contractility by Accelerating Transition from the Weak to Strongly Bound States. Molecular Mechanisms of Cardiac Disease and Regeneration. February, 2006. Poster presentation

Lenzi D, Fritsch A, Alexander G, Hansen R, Cong G, Zink W, Godinez G, Pham A, Trautman J, Pierce DW, Malik F, Finer JT. A Multiplexed and Automated Imaging Assay of Cardiac Myocyte Contractility. American Society of Cell Biology (ASCB) December, 2005. Poster presentation

Anderson RL, Sueoka SH, Rodriguez HM, Lee KH, Cox DR, Kawas R, Morgan BP, Sakowicz R, Morgans Jr DJ, Malik F, Elias KA. In Vitro and In Vivo Efficacy of the Cardiac Myosin Activator CK-1827452. American Society of Cell Biology (ASCB) December, 2005. Poster presentation

Malik F, Elias KA, Finer JT, Morgan BP, Sakowicz R, Anderson R, Baliga R, Conn L, Cox D, Garard M, Hartman J, Irvine J, Kawas R, Kraynack E, Kuklov A, Lee KH, Lu P, Muci A, Pierce DW, Rodriguez H, Suehiro I, Sueoka SH, Sylvester S, Tochimoto T, Valdez C, Wang W, Katori T, Kass DA, Shen YT, Vatner SF, and Morgans DJ . Direct Activation of Cardiac Myosin by CK-1827452 Improves Cardiac Function in a Dog Heart Failure Model. Heart Failure Society of America Meeting, September 2005. Poster presentation

Malik F, Shen Y, Katori T, Sueoka SH, Anderson R, Cox D, Garard M, Hartman J, Kim S, Kraynack E, Kuklov A, Lee KH, Lu P, Muci A, Niu C, Rodriguez H, Suehiro I, Sylvester S, Tochimoto T, Elias KA, Morgan BP, Sakowicz R, Kass DA, Vatner SF, Morgans DJ. Direct Activation of Cardiac Myosin, A Novel Mechanism for Improving Cardiac Function. American Heart Association (AHA) Keystone, July 2005. Poster presentation

Anderson R, Niu C, Elias K. The Cardiac Myosin Activator, CK-1122534, Overcomes the Myosin II Inhibitors 2, 3-Butanedione-2-Monoxime and (-)-S-Blebbistatin without Affecting the Ca2+ Transient in Ventricular Myocytes. American Society of Cell Biology, December 2004. Poster presentation

Niu C, Anderson R, Cox D, Qian X, Morgan B, Malik F, Morgans Jr D, Elias K. The Cardiac Myosin Activator, CK-1122534, Increases Contractility in Adult Cardiac Myocytes without Altering the Calcium Transient. American Society of Cell Biology, December 2004. Poster presentation

Niu C, Cox D, Lee K, Sylvester S, Sueoka S, Qian X, Feng B, Malik F, Morgans Jr D, Hartman J, Sakowicz R, Elias K. Cellular Responses of the Myosin Activator CK-0689705 in Normal and Heart Failure Models. American Society of Cell Biology, December 2004. Poster presentation

Rodriguez H, Sylvester S, Qian X, Morgan B, Morgans Jr D, Malik F, Sakowicz R. Activation of Cardiac Sarcomere ATPase by CK-1122534, a Small Molecule Agent that Specifically Targets Cardiac Myosin. American Society of Cell Biology, December 2004. Poster presentation

Rodriguez H, Sylvester S, Sakowicz R. Interaction of Myosin with Blebbistatin Reported by Fluorescence Spectroscopy. American Society of Cell Biology, December 2004. Poster presentation

Niu C, Anderson RL, Cox DR, Morgan BP, Morgans Jr DJ, Malik F, Elias KA. The Cardiac Myosin Activator, CK1122534, Increases Contractility in Adult Cardiac Myocytes But Does Not Affect the Transient or Depend on Second Messenger Signaling. American Heart Association, November 2004. Poster presentation

Skeletal

Chou W, Hansen R, Saikali KG, Russell A, Chen MM, Vijayakumar V, Stoltz R, Baudry S, Enoka R, Morgans D, Wolff AA, Malik F. CK-2017357, a Novel Activator of Fast Skeletal Muscle, Increases Isometric Force Evoked by Electrical Stimulation of the Anterior Tibialis Muscle in Healthy Male Subjects. XII International Congress on Neuromuscular Diseases, Naples, Italy. July 2010. Poster presentation

Aaron C Hinken, Lena Driscoll, Ken Lee, Jim J Hartman, David Marquez, Richard Hansen, Alex Muci, Bradley Morgan, David J Morgans Jr, Alan J Russell, Fady Malik. The Fast Skeletal Troponin Activator, CK-2017357, Reduces Muscle Fatigue in an in situ Model of Vascular Insufficiency. Society for Vascular Medicine’s 2010 Annual Meeting: 21st Annual Scientific Sessions, Cleveland, OH. April 2010. Poster presentation

Aaron C Hinken, Lena C Driscoll, Ken Lee, Jim J Hartman, David Marquez, Richard Hansen, Alex Muci, Bradley Morgan, Fady Malik, Alan J Russell. Fast Skeletal Troponin Activator, CK-1909178, Reduces Muscle Fatigue in a Model of Peripheral Artery Disease in situ. Biophysical Society 54th Annual Meeting,San Francisco, CA. February 2010. Poster presentation

Raja Kawas, Alan Russell, Alex Muci, Bradley Morgan, Fady Malik, Jim Hartman. The Small Molecule Skeletal Sarcomere Activator, CK-2017357, is a Calcium Sensitizer that Binds Selectively to the Fast Skeletal Troponin Complex. Biophysical Society 54th Annual Meeting, San Francisco, CA. February 2010. Poster presentation

Russell AJ, Lee K, Hartman JJ, Marquez D, Hansen R, Muci A, Morgan B, Jia Z, Morgans DJ, Malik F. The Fast Skeletal Troponin Activator, CK-2017357, Increases Skeletal Muscle Force and Reduces Muscle Fatigue in vitro and in situ. 5th Cachexia Conference, Barcelona, Spain. December 2009. Poster presentation

Russell AJ, Lee K, Jia Z, Muci A, Browne W, Tomlinson M, Hartman JJ, Hansen R, Hinken AC, Albertus D, Claflin D, Morgans DJ., Morgan B, Malik F. The Fast Skeletal Troponin Activator, CK-2017357, Increases Skeletal Muscle Force in vitro and in situ. 2009 Experimental Biology Conference, New Orleans, LA. April 2009. Poster presentation

Lee K, Hartman J, Hansen R, Clarke D, Hinken A, Muci A, Morgan B, Vijayakumar V, Jia Z, Malik F, Russell A. The Fast Skeletal Troponin Activator, CK-1909178, Increases Skeletal Muscle Force in-vitro and in-situ. Biophysical Society 53rd Annual Meeting, Boston, MA. March 2009. Poster presentation

Kawas R, Russell A, Rodriguez H, Suekawa K, Muci A, Morgan B, Malik F, Hartman J. The Small Molecule Skeletal Sarcomere Activator, CK-1909178, is a Calcium Sensitizer that Binds Selectively to the Fast Skeletal Troponin Complex. Biophysical Society 53rd Annual Meeting. Boston, MA. March 2009. Poster presentation

Marquez D, Tomlinson M, Lievers J, Hartman J, Russell A, Hansen R. An Automated Apparatus for Isometric Force Analysis of Skinned Muscle Fibers. Biophysical Society 53rd Annual Meeting. Boston, MA. March 2009. Poster presentation

Smooth

Zhiheng Jia, Guillermo Godinez, Nickie Durham, Xi Wang, Chihyuan Chuang, Pu-Ping Lu, Wenyue Wang, Bing Yao, Jeffrey Warrington, Sheila Clancy, James J Hartman, David J Morgans Jr, Bradley P Morgan, Xiangping Qian, Fady I Malik, Malar Pannirselvam. The Direct Smooth Muscle Myosin Inhibitor, CK-2018571, Represents a Novel Therapeutic Mechanism for Bronchodilation. American Thoracic Society's 2010 International Conference, May 2010, New Orleans, LA. Poster presentation

Sheila Clancy, Zhiheng Jia , Malar Pannirselvam, Xiangping Qian, Bradley Morgan, Fady Malik, Jim Hartman. The Small Molecule Smooth Muscle Myosin Inhibitor, CK-2018571, Selectively Inhibits ATP Hydrolysis and Relaxes Smooth Muscle in vitro. Biophysical Society 54th Annual Meeting,San Francisco, CA. February 2010. Poster presentation

David Ho, Xin Zhao, Li Chen, You-Tang Shen, Xiangping Qian, David J. Morgans, Stephen F. Vatner, Fady I. Malik. Inhibition of Smooth Muscle Myosin, a Novel Therapeutic Approach for Pulmonary Hypertension. American Heart Association (AHA) 2009 Scientific Sessions. Orlando, FL. November 2009. Poster presentation

Qian X, Wang X, Hartman JJ, Jia Z, Clancy S, Yao B, Chuang C, Lu P, Pannirselvam M, Morgans DJ, Morgan BP, Malik FI. A Direct Inhibitor of Smooth Muscle Myosin as a Novel Therapeutic Approach for the Treatment of Systemic Hypertension. American Society of Hypertension 24th Annual Scientific Meeting and Exposition. San Francisco, CA. May 2009. Poster presentation

Oncology

Hu Z, Mao, J, Huang G, Kuo W, Lenburg ME, Gu S, Korkola JE, Ziyad S, Bayani N, Feiler HS, Wang JN, Weber B, Wooster R, Gray JW. A Systems Analysis of Mitotic Apparatus Inhibitors Defines a Response Network for Breast Cancer. 32nd Annual San Antonio Breast Cancer Symposium (SABCS), San Antonio, TX. December 2009. Poster presentation

O'Connor OA, Gerecitano J, Van Deventer H, Afanasyev B, Hainsworth J, Chen MM, Saikali K, Seroogy J, Escandon R, Wolff A, Conlan MG. A Pase I/II Trial of the Kinesin Spindle Protein (KSP) Inhibitor SB-743921 Dosed Q14D without and with Prophylactic G-CSF in Non-Hodgkin Lymphoma (NHL) or Hodgkin Lymphoma (HL). American Society of Hematology 51st Annual Meeting and Exposition. December 2009. Poster presentation

Yin H, Kiefer J, Chow D, Que Q, Dastrup E, Weber B, Wooster R, Mousses S. RNAi-directed Identification of Chemosensitizers of CENP-E Inhibitor GSK923295. AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics, Boston, Massachusetts, November 2009.Poster presentation

Degenhardt Y, Zhang X, Moy C, Conway T, McNeil L, Jing J, Greshock J, Wegrzyn R, Kershner K, Yin H, Mousses S, Wooster R, Lampkin T, Bachman K. Synergistic Interaction Between CENP-E Inhibitor GSK923295 and MEK Inhibitor GSK1120212. AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics, Boston, Massachusetts, November 2009.Poster presentation

Smith MA, Morton CL, Hernan C, Gorlick R, Kang M, Keir ST, Kolb EA, Lock RB, Maris JM, Houghton PJ. Pediatric Preclinical Testing Program (PPTP) evaluation of the CENP-E inhibitor GSK923295A. 2009 American Society of Clinical Oncology (ASCO), Orlando, FL. May 2009. Poster presentation

Gómez H, Philco M, Castaneda C, Pimentel P, Escandón R, Seroogy J, Saikali K, Wolff AA, Conlan MG. A Phase I/II Trial of Ispinesib, a Kinesin Spindle Protein Inhibitor, Dosed Q14D in Patients with Advanced Breast Cancer Previously Untreated with Chemotherapy for Metastatic Disease or Recurrence. 2009 American Society of Clinical Oncology (ASCO), Orlando, FL. May 2009. Poster presentation

Gerecitano J, O’Connor OA, Van Deventer H, Hainsworth J, Leonard JP, Afanasyev B,Chen MM, Seroogy J, Saikali K, Escandon R, Wolff AA, Conlan MG. A Phase I/II Trial of the Kinesin Spindle Protein (KSP) Inhibitor SB-743921 Dosed q14d without and with Prophylactic G-CSF in Non-Hodgkin Lymphoma (NHL) or Hodgkin Lymphoma (HL), 2009 American Society of Clinical Oncology (ASCO), Orlando, FL. May 2009. Poster presentation

Johnson BM, Sutton D, Fleming RA, Lager JJ. Exploratory Methods for Assessment of Therapeutic Exposures and Schedules of GSK923295A, a Novel Mitotic Checkpoint Inhibitor. 2009 American Association of Cancer Research (AACR), Denver, CO. April 2009. Poster presentation

Hu Z, Kuo W, Das D, Ziyad S, Gu S, Bhattacharya S, Wyrobek A, Wang NJ, Felier HS, Wooster R, Weber B, Gray JW. Small Molecular Inhibitor of the Centromere-Associated Protein E (CENP-E), GSK923295A Inhibits Cell Growth in Breast Cancer Cells. 2009 American Association of Cancer Research (AACR), Denver, CO. April 2009. Poster presentation

Gómez H, Castaneda C, Philco M, Pimentel P, Falcón S, Escandón R, Saikali K, Conlan M, Seroogy J, Wolff A. A Phase I-II Trial of Ispinesib, a Kinesin Spindle Protein Inhibitor, Dosed Every Two Weeks in Patients with Locally Advanced or Metastatic Breast Cancer Previously Untreated with Chemotherapy for Metastatic Disease or Recurrence. 31st Annual San Antonio Breast Cancer Symposium (SABCS). San Antonio, TX. December 2008. Poster presentation

Purcell JW, Reddy M, Davis J, Martin S, Samayoa K, Vo H, Thomsen K, Bean P, Wood KW, and Cases S. Ispinesib (SB-715992) a Kinesin Spindle Protein (KSP) Inhibitor has Single Agent Activity and Enhances the Efficacy of Standard-of-Care Therapies in Pre-Clinical Models of Breast Cancer. 31st Annual San Antonio Breast Cancer Symposium (SABCS). San Antonio, TX. December 2008. Poster presentation

J. Gerecitano, O.A. O’Connor, H. Van Deventer, J. Hainsworth, J.P. Leonard, A. Goy, B. Afanasyev, M.M. Chen, K. Saikali, M.G. Conlan, R. Escandon, and A. Wolff. A Phase I/II Trial of the Kinesin Spindle Protein (KSP) Inhibitor SB-743921 Administered on Days 1 and 15 Every 28 Days without and with Prophylactic G-CSF in Non-Hodgkin or Hodgkin Lymphoma. 2008 American Society of Hematology (ASH) Annual Meeting and Exposition. December 2008. Poster presentation

Gomez H, Philco M, Falcón S, Escandón R, Saikali K, Conlan M, Wolff A. A Phase I-II Open-Label Trial of Ispinesib, a Kinesin Spindle Protein (KSP) Inhibitor, Dosed Every Two Weeks in Patients with Locally Advanced or Metastatic Breast Cancer Previously Untreated with Chemotherapy for Metastatic Disease or Recurrence. 2008 American Society of Clinical Oncology (ASCO) Breast Cancer Symposium. September, 2008. Poster presentation

Fleming RA, Holen KD, Cyr TL, Johnson BM, Gauvin JLS, Lager JJ, Williams B, Alberti DB, Weber BL, Grilley-Olson JE, Chung V. A Phase I Dose Escalation and Pharmacokinetic Study of the Novel Mitotic Checkpoint Inhibitor GSK923295A in Patients with Solid Tumors. EORTC-NCI-AACR International Conference on Molecular Targets and Cancer, Geneva Palexpo, Geneva, Switzerland. October 2008. Poster presentation

Sutton D, Fleming RA, Wood KW, Jackson JR. 2-[18F] fluoro-2-deoxy-d-glucose Positron Emission Tomography is an Early Biomarker for Tumor Growth Inhibition of Human Colo205 Xenografts by the Novel and Selective CENP-E Inhibitor, GSK923295A. EORTC-NCI-AACR International Conference on Molecular Targets and Cancer, Geneva Palexpo, Geneva, Switzerland. October 2008. Poster presentation

Sutton D, Liu Q, Moss KG, Wood KW, Jackson JR. GSK923295A, a Novel and Selective CENP-E Inhibitor, Induces Pharmacodynamic Effects and Anti-tumor Activity in Human Colo205 Xenografts. EORTC-NCI-AACR International Conference on Molecular Targets and Cancer, Geneva Palexpo, Geneva, Switzerland. October 2008. Poster presentation

Zain J, Bongero D, Goy A, Orlowski RZ, Hainsworth J, Afanasayev B, Chen MM, Escandon R, Mao Y, O’Connor OA. Translational Development of the Novel Kinesin Spindle Protein (KSP/Eg5) Inhibitor SB-743921 (SB-921) in Lymphoma: From Preclinical Models to Phase 1 Studies. EORTC-NCI-AACR International Conference on Molecular Targets and Cancer, Geneva Palexpo, Geneva, Switzerland. October 2008. Poster presentation

O’Connor OA, Goy A, Orlowski RZ, Hainsworth J, Leonard JP, Gerecitano J, Van Deventer H, Afanasyev B, Osmanov D, Chen MM, Wolff A. A Phase I-II Trial of the Kinesin Spindle Protein (KSP) Inhibitor SB-743921 on Days 1 and 15 Every 28 Days in Non-Hodgkin or Hodgkin Lymphoma. 10th International Conference on Malignant Lymphoma. Lugano, Switzerland June, 2008. Poster presentation

Philco M, Gómez H, Falcón S, Escandón R, Saikali K, Wolff A. A Phase I-II Open-Label Trial of Ispinesib on an Alternate Dosing Schedule in Chemotherapy-Naïve Patients with Locally Advanced or Metastatic Breast Cancer (MBC). American Society of Clinical Oncology, Chicago, IL. June, 2008. Poster presentation

O'Connor OA, Goy A, Orlowski RZ, Hainsworth J, Leonard JP, Gerecitano J, Van Deventer H, Afanasyev B, Osmanov D, Chen MM, Wolff A. A Phase I-II Trial of the Kinesin Spindle Protein (KSP) Inhibitor SB-743921 on Days 1 and 15 Every 28 Days in Non-Hodgkin or Hodgkin Lymphoma. American Society of Clinical Oncology, Chicago, IL. June, 2008. Poster presentation

Wood AC, Cole KA, Courtright JP, Balamuth NJ, Wang Q, Cornwell WD, Greshock J, Opsitnick N, Sutton D, Gilmartin A, Jackson JR, Wood K, Zhao H, Weber, BL, Wooster RF, Maris JM. Targeted Inhibition of the Centromere-Associated Protein E (CENP-E) with GSK923295A is Effective in Preclinical Models of Human Neuroblastoma. Annual Meeting of the American Association for Cancer Research (AACR), San Diego, CA. April, 2007. Poster presentation

O'Connor OA, Goy A, Orlowski RZ, Hainsworth J, Leonard JP, Afanasyev B, Osmanov D, Reyno L, Chen MM, Escandon R. A Phase I-II Study to Determine the Safety, Pharmacokinetics and Potential Efficacy of the Kinesin Spindle Protein (KSP) Inhibitor SB-743921 on Days 1 and 15 of a 28 Day Schedule in Patients with Non-Hodgkin’s or Hodgkin’s Lymphoma. 49th American Society of Hematology Annual Meeting, Atlanta GA. December 2007. Poster presentation

Chua PR, Desai R, Schauer SP, Cornwell W, Gilmartin A, Sutton D, Wood KW. Differential Response of Tumor Cell Lines to Inhibition of the Mitotic Checkpoint Regulator and Mitotic Kinesin, CENP-E. AACR-NCI-EORTC International Conference on Molecular Targets and Cancer, San Francisco CA. October 2007. Poster presentation

Sutton D, Gilmartin AG, Kusnierz AM, Sung CM, Luo L, Carson JD, Laquerre SG, Cornwell W, King AG, Knight SD, Dhanak D, Bergnes G, Qian X, Chua P, Wood KW, Huang PS, Weber BL, Copeland RA, Jackson JR. A Potent and Selective Inhibitor of the Mitotic Kinesin CENP-E (GSK923295A) Demonstrates a Novel Mechanism of Inhibiting Tumor Cell Proliferation and Shows Activity Against a Broad Panel of Human Tumor Cell Lines in vitro. AACR-NCI-EORTC International Conference on Molecular Targets and Cancer, San Francisco CA. October 2007. Poster presentation

Shahin M, Braly P, Rose P, Malpass T, Bailey H, Alvarez RD, Hodge J, Bowen C, Buller R. A Phase II, Open-Label Study of Ispinesib (SB-715992) in Patients with Platinum/Taxane Refractory or Resistant Relapsed Ovarian Cancer. American Society of Clinical Oncology, Chicago, IL. June, 2007. Poster presentation

Chen Q, Pamarthi V, Kuhn D, Voorhees P, Strader J, Orlowski R. Inhibition of Kinesin Spindle Protein Induces Apoptosis and Overcomes Drug Resistance in Models of Multiple Myeloma. Annual Meeting of the American Association for Cancer Research (AACR), Los Angeles, CA. April, 2007. Poster presentation

Sutton D, Diamond M, Faucette L, Giardiniere M, Zhang S, Vidal J, Dhanak D, Knight S, Bergnes G, Qian X, Wood K, Morgans D, Huang P, Jackson J. GSK-923295, a Potent and Selective CENP-E Inhibitor, Has Broad Spectrum Activity Against Human Tumor Xenografts in Nude Mice. Annual Meeting of the American Association for Cancer Research (AACR), Los Angeles, CA. April, 2007. Poster presentation

Lad L, Luo L, Wood K, Hartman J, Copeland R, Sakowicz R. Detailed Biochemical Analysis of the CENP-E Inhibitor GSK-923295. Annual Meeting of the American Association for Cancer Research (AACR), Los Angeles, CA. April, 2007. Poster presentation

Roof D, Bergnes G, Wang J, Yang Z, Ashcraft L, Collibee S, Ramchandani S, Fan J, Desai R, Moon-Crompton A, Xu D, Morgan B, Keon B, Vacin C, Lila T, Vaisberg E, De Hostos E, Chua P, Purcell J, Trautman J, Morgans D, Wood K, Adams C. Cell-based Discovery and Anti-tumor Activity of a Novel Mitotic Inhibitor. Annual Meeting of the American Association for Cancer Research (AACR), Los Angeles, CA. April, 2007. Poster presentation

Ramchandani S, Schauer S, Adams C, de la Rosa R, Freedman R, Mak J, Beraud C, Lee Y, Sakowicz R, Wood K, Belmont L. Functional Studies of Human Kip3D (Kif18a) Kinesin. 46th Annual American Society for Cell Biology Meeting, San Diego, CA. December, 2006. Poster presentation

Guo D, Baliga R, Pierce DW, Belmont L, Finer JT. A Novel Mechanism for Kinesin Spindle Protein (KSP) Modulation: Small Molecular Activators of KSP Basal ATPase. 46th Annual American Society for Cell Biology Meeting, San Dieago, CA. December, 2006. Poster presentation

de Hostos RL, Lee Y, Sakowicz R, Belmont L. Characterization of Motor=Domain Mutants of the Mitotic Kinesin RAB6KIFL (MKLP2, KIF20A). 46th Annual American Society for Cell Biology Meeting, San Diego, CA. December, 2006. Poster presentation

Chen Q, Pamarthi V, Kuhn DJ, Voorhees PM, Strader JS, Orlowski RZ. Inhibition of Kinesin Spindle Protein Induces Apoptosis and Overcomes Drug Resistance in Models of Multiple Myeloma. December, 2006. Poster presentation

Houghton PJ, Maris JM, Friedman HS, Keir ST, Lock RB, Gorlick R, Kolb EA, Reynolds CP, Morton C, Smith MA,. Pediatric Preclinical Testing Program (PPTP) Evaluation of the KSP Inhibitor Ispinesib (SB-715992). 18th EORTC-NCI-AACR Symposium on "Molecular Targets and Cancer Therapeutics," Prague, Czech Republic. November 2006. Poster presentation

Belmont LD, Sutton D, Wood KW. Sequence dependent anti-tumor activity of bortezomib and the KSP inhibitor, SB-743921, in a solid tumor xenograft model. 18th Annual EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics, Prague, Czech Republic . November, 2006. Poster presentation

Rodon J, E. Till, Patnaik A, Takimot C, Kathmanz S, Williams D, Vasist L, Bowen C, Hodge J, Dar M, Tolcher A. Phase I Study of lspinesib in Combination with Capecitabine in Patients with Advanced Solid Tumors. 18th Annual EORTC-NCI-AACR Symposium on Molecular Targets and Cancer Therapeutics, Prague, Czech Republic . November, 2006. Poster presentation

Tang PA, Siu LL, Chen EX, Hotte SJ, Chia S, Schwarz JK, Colevas AD, Johnson C, Pond GR, Winquist E. A Phase II study of ispinesib in patients with recurrent and/or metastatic head and neck squamous cell carcinoma. 31st ESMO Congress, Istanbul, Turkey. September, 2006. Poster presentation

Jackson JR, Gilmartin A, Dhanak D, Knight S, Luo L, Sutton D, Caulder E, Diamond M, Giardiniere M, Zhang S, Huang P;. A second generation KSP inhibitor, SB-743921, is a highly potent and effective therapeutic in preclinical models of cancer. AACR Molecular Diagnostics in Cancer Therapeutics Conference, Chicago, IL. September, 2006. Poster presentation

E.I. Heath, A. Alousi, J.P.Eder, M. Valdivieso, L.S. Vasist, L. Appleman, P. Bhargava, A.D.Colevas, P.M.LoRusso, G. Shapiro. A Phase I Dose Escalation Trial of Ispinesib (SB-715992) Administered Days 1-3 of a 21-day Cycle in Patients with Advanced Solid Tumors. American Society of Clinical Oncology (ASCO), June, 2006. Poster presentation

S. F. Jones, E.R. Plummer, H. A. Burris III, A Razak, A. Meluch, C.J. Bowen, D.D. Williams, L.S. Vasist, J.P. Hodge, M.M. Dar, A.H. Calvert. Phase I Study of Ispinesib in Combination with Carboplatin in Patients with Advanced Solid Tumors. American Society of Clinical Oncology (ASCO), June, 2006. Poster presentation

A.B. El-Khoueiry, S. Iqbal, D.A. Singh, S. D’Andre, R.K. Ramanathan, S. Shibata, D. Y. Yang, H.J. Lenz, T. Synold, D.R. Gandara. A Randomized Phase II Non-Comparative Study of Ispinesib Given Weekly or Every Three weeks in Metastatic Colorectal Cancer. A California Cancer Consortium Study (CCC-P). American Society of Clinical Oncology (ASCO), June, 2006. Poster presentation

Miller K, Ng C, Ang P, Brufsky AM, Lee SC, Dees EC, Piccart M, Verrill M, Wardley A, Loftiss J, Bal J, Yeoh S, Hodge J, Williams D, Dar M, Kathman S, and Ho PT C. Phase II, Open Label Study of Ispinesib in Patients with Locally Advanced or Metastatic Breast Cancer. San Antonio Breast Cancer Symposium (SABCS), December, 2005. Poster presentation

Sutton D, Zhang SY, Gilmartin A, Wood KW, Jackson JR, Huang P. Mitotic Arrest in Tumors as a Pharmacodynamic Marker for Inhibition of the Mitotic Kinesin KSP by Ispinesib, a novel KSP inhibitor. AACR-NCI-EORTC, November 2005. Poster presentation

Jackson JR, Auger KR, Gilmartin A, Eng WK, Luo L, Concha N, Parrish C, Sutton D, Diamond M, Giardiniere M, Zhang SY, Huang P. A Resistance Mechanism for the KSP Inhibitor Ispinesib Implicates Point Mutations in the Compound Binding Site. AACR-NCI-EORTC, November 2005. Poster presentation

Sutton D, Diamond M, Onori J, Zhang SY, Giardiniere M, Faucette L, Belmont L, Wood KW, Jackson JR, Huang P. Cisplatin Enhances the Activity of Ispinesib, a Novel KSP Inhibitor, Against Murine P388 Lymphocytic Leukemia. AACR-NCI-EORTC, November 2005. Poster presentation

Sutton D, Zhang SY, Diamond M, Giardiniere M, Faucette L, King AG, Chen YJ, Wood KW, Jackson JR, Huang P. Relationship Between the Antitumor Activity of Ispinesib, a Novel KSP Inhibitor, and Neutropenia in a Human Xenograft Model. AACR-NCI-EORTC, November 2005. Poster presentation

Blagden S, Seebaran G, Molife R, Payne M, Reid A, Protheroe A, Kathman S, Williams D, Bowen C, Hodge J, Dar M, de Bono1 J, Middleton M. Phase I Study Of Ispinesib In Combination With Docetaxel in Patients With Advanced Solid Tumors. AACR-NCI-EORTC, November 2005. Poster presentation

Calvo E, Chu Q, Til E, Rowinsky E, Patnaik A, Takimoto C, Kathman S, Williams D, Bowen C, Hodge J, Dar M, Tolcher A. Phase I Study Of Ispinesib In Combination With Capecitabine in Patients With Advanced Solid Tumors. AACR-NCI-EORTC, November 2005. Poster presentation

Holen KD, Belan CP, Wilding G, Ramalingam S, Volkman1 JL, Ramanathan RK, Bowen CJ, Williams DD, Hodge JP, Dar MM, Ho PTC. Phase I Study to Determine Tolerability & Pharmacokinetics (PK) of SB-743921, a Novel Kinesin Spindle Protein (KSP) Inhibitor. American Society of Clinical Oncology (ASCO), May 2005. Poster presentation

Brejc K, Yu M, Lee Y, Belmont L, Hartman J, Guo J, Lichtsteiner S, Wood K, Sakowicz R. Structure of Human Kip3d – Unconventional Microtubule Depolymerizing Kinesin. American Society of Cell Biology (ASCB), December 2004. Poster presentation

Williams DD, Kathman SJ, Chu QSC, Holen KD, Rowinsky EK, Wilding G, Mudd Jr PN, Herendeen JM, Orr JB, Pandite LN. A Phase I Study (KSP10001) of SB-715992, a Novel Kinesin Protein Spindle (KSP) Inhibitor: Pharmacokinetic (PK)/ Pharmacodynamic (PD) Modeling of Absolute Neutrophil Counts (ANC). EORTC-NCI-AACR, September 2004. Poster presentation

Chu Q, Holen KD, Rowinsky EK, Wilding G, Volkman JL, Orr JB, Williams DD, Hodge JP, Kerfoot CA, Sabry J. A Phase I Trial of Novel Kinesin Spindle Protein (KSP) Inhibitor, SB-715992 Administered Intravenously Once Every 21 Days. American Society of Clinical Oncology (ASCO), June 2004. Poster presentation

Chu Q, Holen KD, Rowinsky EK, Alberti DB, Monroe P, Volkam JL, Hodge JP, Bush P, Pandite L, Williams D, Hoke F, Sabry J, HO PTC, Wilding G. A Phase I Study to Determine the Safety and Pharmacokinetics of IV Administered SB-715992, A Novel Kinesin Spindle Protein (KSP) Inhibitor, in Patients with Solid Tumors. American Society of Clinical Oncology (ASCO). May 2003. Poster presentation

Hedge P, Cogswell J, Carrick K, Jackson JR, Wood KW, Eng WK, Brawner M, Huang PS, Gergsma D. Differential Gene Expression Analysis of Kinesin Spindle Protein in Human Solid Tumors. American Society of Clinical Oncology (ASCO). May 2003. Poster presentation

LoRusso JB, Jones JB, Gadgeel1 S, Willcutt N, Helmke1 W, Orr J, Hodge J, Williams D, Pandite L, Sabry J, Ho P, Burris III H. A Phase I Study To Determine the Safety and Pharmacokinetics of Intravenous Administration of SB-715992, a Novel Kinesin Spindle Protein (KSP) Inhibitor, on a Once Weekly for Three Consecutive Weeks Schedule in Patients With Refractory Solid Tumors. European Cancer Conference (ECCO), September 2003. Poster presentation

Mak J, Freedman R, Beraud C. Utilization of Gene Expression Profiles to Identify Mitotic Kinesins. American Association for Cancer Research (AACR). April 2002. Poster presentation

Bergnes G, Ha E, Feng B, Yao B, Smith WW, Tochimoto T, Lewis ER, Lee YY, Moody R, Turincio RA, Finer JT, Wood KW, Sakowicz R, Crompton AM, Chabala JC, Morgans Jr DJ, Sigal NH, Sabry JH. Mitotic Kinesin-Targeted Antitumor Agents: Discovery, Lead Optimization and Anti-Tumor Activity of a Series of Novel Quinazolinones as Inhibitors of Kinesin Spindle Protein (KSP). American Association for Cancer Research (AACR), April 2002. Poster presentation

Gonzales P, Bienek A, Boehme M, Rivali C, Roth S, Wynne H, Piazza G, Weitman S, Wood K, Crompton A, Moody R, Schauer S, Feng B, Bergnes G, Sigal N, Morgans D. Breadth of Anti-tumor Activity of CK0238273 (SB-715992), a Novel Inhibitor of the Mitotic Kinesin KSP. American Association for Cancer Research (AACR), April 2002. Poster presentation

Jackson JR, Gilmartin AG, Williams T, McCabe FL, Caulder E, Inlow L, Whitacre M, Mattern M, Bergnes G, Feng B, Smith WW, Morgans D, Ward K, Smith B, Wood KW, Moody RS, Belmont L, Schauer S, Johnson RK, Winkler JD. A Pharmacodynamic Marker of Mitosis Demonstrates the Anti-mitotic Activity of SB-715992, an Inhibitor of the Mitotic Kinesin KSP. American Association for Cancer Research (AACR), April 2002. Poster presentation

Johnson RK, McCabe FL, Cauder E, Innlow L, Whitacre M, Winkler JD, Bergnes G, Feng B, Smith WW, Morgans D, Wood K, Jackson JR. SB-715992, a Potent and Selective Inhibitor of KSP Mitotic Kinesin, Demonstrates Broad-spectrum Activity in Advanced Murine Tumors and Human Tumor Xenografts. American Association for Cancer Research (AACR), April 2002. Poster presentation

Lee Y, Ji Z, Sakowicz R. Inhibitors of the Mitotic Kinesin KSP: Biochemical Mechanism of Action. American Association for Cancer Research (AACR), April 2002. Poster presentation

Turner J, Anderson R, Guo J, Beraud C, Fletterick R, Sakowicz R.
Crystal Structure of the Mitotic Spindle Kinesin Eg5 Reveals a Novel Conformation of the Neck-linker
J Biol Chem., 2001 Jul 6; 276(27):25496-502. Abstract on Medline

Sakowicz R, Berdelis MS, Ray K, Blackburn CL, Hopmann C, Faulkner DJ, Goldstein LS.
A Marine Natural Product Inhibitor of Kinesin Motors
Science, 1998 Apr 10; 280(5361):292-5. Abstract on Medline

Other Publications

Lila T, Chua PR, Vacin C, Collibee S, Clarke D, Roof D, Morgan BP, Maxon ME, Pierce DW, Finer JT. Image-Based Identification of Small-Molecule Inhibitors of Yeast Pathogen Morphogenesis. American Society of Cell Biology (ASCB) December, 2005. Poster presentation

Baliga R, Guo D, Chua PR, Stephens T, Yu M, Pierce DW, Sakowicz R, Lichtsteiner S, Maxon ME, Finer JT. Microtubule Depolymerization Activity of a Kip3 Kinesin: Results from a Novel High-Throughput Microtubule Depolymerization Assay. American Society of Cell Biology (ASCB) December, 2005. Poster presentation

Tomasevic N, Russell A, Pierce DW, Jia Z, Sakowicz R. Identification and Biochemical Characterization of Small Molecule Arp2/3 Complex Inhibitors. American Society of Cell Biology (ASCB) December, 2005. Poster presentation

Baliga R, Guo D, Tomasevic N, Jia Z, de Hostos E , Brejc K, Sakowicz R, Lichtsteiner S, Pierce SW, Finer JT. A Comparison of Two High-Throughput Assays for FtsZ Inhibitors. American Society of Cell Biology (ASCB) December, 2005. Poster presentation

Tanaka M, Bateman R, Rauh D, Vaisberg E, Ramachandani S, Zhang C, Hansen KC, Burlingame AL, Trautman JK, Shokat KV, Adams CL. An Unbiased Cell Morphology-Based Screen for New, Biologically Active Small Molecules.
PLOS Biology, May 2005.

Baliga R, Guo D, Yu M, Hekmat-Nejad M, Sakowicz R, Pierce D, Finer J. A High Throughput Screen for Inhibitors of Microtubule Depolymerizing Enzyme from Plasmodium Falciparum. American Society of Cell Biology (ASCB), December 2004. Poster presentation

Hekmat-Nejad M, Sakowicz R. Regulation of Atpase Activity of Internal Motor Kinesin, pKinI: Binding to Microtubule Lattice is Non-Productive. American Society of Cell Biology (ASCB), December 2004. Poster presentation

Tomasevic N, Chua P, Jia Z, Speer J, Stephens T, Hartman J, Suekawa K, Freedman R, Maxon M, Sakowicz R. Identification and Characterization of Candida Albicans Formins. American Society of Cell Biology (ASCB), December 2004. Poster presentation

Tomasevic N, Jia Z, Russell A, Fujii T, Hartman J, Clancy S, Beraud C, Wang M, Wood K, Sakowic R. Regulation of WASP and N-WASP by Different Activators. American Society of Cell Biology,(ASCB), December 2004. Poster presentation

Tomasevic N, Jia Z, Speer J, Wang M, Belmont L, Hartman J, Sakowicz R. Vasodilator-Stimulated Phosphoprotein (VASP) Promotes Arp2/3 Complex Mediated Actin Polymerization, Prevents Branching and Stabilizes Actin Filaments. American Society of Cell Biology (ASCB), December 2004. Poster presentation