S. Elmore

发表

An inhibitor of Bcl-2 family proteins induces regression of solid tumours

S. Korsmeyer, A. Letai, P. Hajduk, 2005, Nature.

Discovery and Design of Novel HSP90 Inhibitors Using Multiple Fragment‐based Design Strategies

Jean M. Severin, P. Hajduk, J. R. Huth, 2007, Chemical biology & drug design.

Navitoclax, a targeted high-affinity inhibitor of BCL-2, in lymphoid malignancies: a phase 1 dose-escalation study of safety, pharmacokinetics, pharmacodynamics, and antitumour activity.

W. Wilson, A. LaCasce, M. Czuczman, 2010, The Lancet. Oncology.

Discovery of a potent inhibitor of the antiapoptotic protein Bcl-xL from NMR and parallel synthesis.

P. Hajduk, A. Petros, S. Fesik, 2006, Journal of medicinal chemistry.

ABT-263: a potent and orally bioavailable Bcl-2 family inhibitor.

C. Tse, S. Fesik, Eric F. Johnson, 2008, Cancer research.

ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets

L. Lam, C. Tse, Cheol‐Min Park, 2013, Nature Medicine.

Discovery of a novel small molecule binding site of human survivin.

Jun Chen, Saul H Rosenberg, Kenneth M Comess, 2007, Bioorganic & medicinal chemistry letters.

Non-peptidic small molecule inhibitors of XIAP.

Chaohong Sun, R. Meadows, E. Olejniczak, 2005, Bioorganic & medicinal chemistry letters.

Circulating Biomarkers of Cell Death After Treatment with the BH-3 Mimetic ABT-737 in a Preclinical Model of Small-Cell Lung Cancer

T. Ward, C. Dive, D. Micha, 2008, Clinical Cancer Research.

A small-molecule inhibitor of Bcl-XL potentiates the activity of cytotoxic drugs in vitro and in vivo.

Wang Shen, Mary K Joseph, Saul H Rosenberg, 2006, Cancer research.

Discovery and structure-activity relationship of antagonists of B-cell lymphoma 2 family proteins with chemopotentiation activity in vitro and in vivo.

A. Petros, S. Fesik, S. Ng, 2006, Journal of medicinal chemistry.

Inhibitors of Anti-apoptotic Proteins for Cancer Therapy

Cheol‐Min Park, S. Elmore, T. Oost, 2005 .

Preclinical Development The Bcl-2 / Bcl-XL / Bcl-w Inhibitor , Navitoclax , Enhances the Activity of Chemotherapeutic Agents In Vitro and In Vivo

C. Tse, H. Maecker, S. Rosenberg, 2011 .

Preclinical Characterization of BET Family Bromodomain Inhibitor ABBV-075 Suggests Combination Therapeutic Strategies.

L. Lam, Xin Lu, S. Rosenberg, 2017, Cancer research.

Discovery of N-(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor.

Chaohong Sun, L. Hasvold, Chang H. Park, 2017, Journal of Medicinal Chemistry.

Safety, Pharmacokinetics, Pharmacodynamics, and Activity of Navitoclax, a Targeted High Affinity Inhibitor of BCL-2, in Lymphoid Malignancies

W. Wilson, M. Czuczman, J. Leonard, 2011 .

A Phase 1/2a Study Evaluating the Safety, Pharmacokinetics, and Efficacy of ABT-263 in Subjects with Refractory or Relapsed Lymphoid Malignancies.

W. Wilson, A. Tulpule, K. Dunleavy, 2007 .

Design, synthesis, and computational studies of inhibitors of Bcl-XL.

A. Petros, Cheol‐Min Park, R. Henry, 2006, Journal of the American Chemical Society.

Synthesis and characterization of non-steroidal ligands for the glucocorticoid receptor: selective quinoline derivatives with prednisolone-equivalent functional activity.

M. Nakane, S. Elmore, P. Kym, 2001, Journal of medicinal chemistry.

Structure-Guided Rescaffolding of Selective Antagonists of BCL-XL.

Brian J. Smith, J. Baell, G. Nikolakopoulos, 2014, ACS medicinal chemistry letters.

An Enantioselective Approach to the Taxanes: Direct access to functionalized cis‐tricyclo[9.3.1.03,8]pentadecanes via α‐hydroxy ketone and Wagner‐Meerwein rearrangements

S. Elmore, R. Rogers, L. Paquette, 1992 .

Setting the Bridgehead Oxidation Level in trans‐Tricyclo[9.3.1.03,8]pentadecanes as a Prelude to the Dual Synthesis of Taxol and Taxusin

S. Elmore, L. Paquette, K. Combrink, 1992 .

A convenient means for controlling the oxidation level of bridgehead carbon C-1 in functionalized tricyclo[9.3.1.03,8]pentadecanes

S. Elmore, L. Paquette, K. Combrink, 1991 .

Impact of substituent modifications on the atropselectivity characteristics of an anionic oxy-Cope ring expansion

S. Elmore, R. Rogers, L. Paquette, 1991 .

Potent and selective small-molecule MCL-1 inhibitors demonstrate on-target cancer cell killing activity as single agents and in combination with ABT-263 (navitoclax)

C. Tse, D. Anderson, Daniel J. Anderson, 2015, Cell Death and Disease.

Correction to Structure-Guided Design of a Series of MCL-1 Inhibitors with High Affinity and Selectivity.

Scott A. Erickson, C. Tse, A. Petros, 2015, Journal of medicinal chemistry.

Discovery of an orally bioavailable small molecule inhibitor of prosurvival B-cell lymphoma 2 proteins.

Saul H Rosenberg, Xiaohong Song, Milan Bruncko, 2008, Journal of medicinal chemistry.

Nonsteroidal selective glucocorticoid modulators: the effect of C-10 substitution on receptor selectivity and functional potency of 5-allyl-2,5-dihydro-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines.

S. Elmore, M. Nakane, J. Miner, 2003, Journal of medicinal chemistry.

Differentiation of in vitro transcriptional repression and activation profiles of selective glucocorticoid modulators.

David D. Anderson, M. Nakane, S. Elmore, 2004, Bioorganic & medicinal chemistry letters.

Nonsteroidal selective glucocorticoid modulators: the effect of C-5 alkyl substitution on the transcriptional activation/repression profile of 2,5-dihydro-10-methoxy-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines.

S. Elmore, D. Anderson, B. Green, 2001, Journal of medicinal chemistry.

The first thermally-induced retro-oxy-cope rearrangement

S. Elmore, L. Paquette, 1991 .

From D -Camphor to the Taxanes. Highly Concise Rearrangement- Based Approaches to Taxusin and Taxol

S. Elmore, L. Paquette, Hui-Ling Wang, 1998 .

A-ring oxygenation studies in bridgehead hydroxyl-substituted trans-tricyclo[9.3.1.03,8]pentadecan-14-one congeners of taxol

S. Elmore, L. Paquette, 1993 .

Exploiting selective BCL-2 family inhibitors to dissect cell survival dependencies and define improved strategies for cancer therapy

Dolores Diaz, Jun Chen, Deepak Sampath, 2015, Science Translational Medicine.

Chapter 17. Selective glucocorticoid receptor modulators

S. Elmore, M. Kort, M. Coghlan, 2002 .

Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL.

Mary K Joseph, Saul H Rosenberg, Xiaohong Song, 2007, Journal of medicinal chemistry.

Fragment-Based, Structure-Enabled Discovery of Novel Pyridones and Pyridone Macrocycles as Potent Bromodomain and Extra-Terminal Domain (BET) Family Bromodomain Inhibitors.

A. Petros, Chaohong Sun, P. Kovar, 2017, Journal of medicinal chemistry.

Stereocontrolled Oxygenation of Camphor Derivatives as a Prelude to the Complete .beta.-Ring Functionalization of Potential Precursors to Taxol and Structural Analogs Thereof

S. Elmore, L. Paquette, 1995 .

Bcl-2 family proteins are essential for platelet survival

C. Tse, M. L. Smith, S. Rosenberg, 2007, Cell Death and Differentiation.

Mcl-1 is critical for survival in a subgroup of non-small-cell lung cancer cell lines

L. Lam, L. Roberts, J. Leverson, 2011, Oncogene.

Influence of Bcl-2 family members on the cellular response of small-cell lung cancer cell lines to ABT-737.

C. Tse, S. Fesik, S. Ng, 2007, Cancer research.

Expanding the Repertoire for “Large Small Molecules”: Prodrug ABBV-167 Efficiently Converts to Venetoclax with Reduced Food Effect in Healthy Volunteers

Ahmad Y. Sheikh, Richard S. Hong, Geoff G. Z. Zhang, 2021, Molecular Cancer Therapeutics.

Expression of Bcl-2 Pro-Survival Family Proteins Predicts Pharmacological Responses to ABT-199, a Novel and Selective Bcl-2 Antagonist, in Multiple Myeloma Models

F. Peale, Leslie B. Lee, W. Fairbrother, 2012 .

A novel antiinflammatory maintains glucocorticoid efficacy with reduced side effects.

M. Nakane, S. Elmore, R. Turner, 2003, Molecular endocrinology.

Identification of Expression Signatures Predictive of Sensitivity to the Bcl-2 Family Member Inhibitor ABT-263 in Small Cell Lung Carcinoma and Leukemia/Lymphoma Cell Lines

Viswanath Devanarayan, Saul H. Rosenberg, Paul E. Kroeger, 2010, Molecular Cancer Therapeutics.

The Bcl-2 Family Antagonist ABT-737 Significantly Inhibits Multiple Animal Models of Autoimmunity

Christian Goess, S. Mathieu, S. Rosenberg, 2009, The Journal of Immunology.

Discovery of potent antagonists of the antiapoptotic protein XIAP for the treatment of cancer.

Saul H Rosenberg, Chaohong Sun, R. Meadows, 2004, Journal of medicinal chemistry.

Inhibitor , Navitoclax , Enhances the Activity of Chemotherapeutic Agents in vitro and in vivo

C. Tse, H. Maecker, S. Rosenberg, 2011 .

Structure-guided design of a series of MCL-1 inhibitors with high affinity and selectivity.

Scott A. Erickson, C. Tse, A. Petros, 2015, Journal of medicinal chemistry.

The Bcl-2/Bcl-XL/Bcl-w Inhibitor, Navitoclax, Enhances the Activity of Chemotherapeutic Agents In Vitro and In Vivo

C. Tse, H. Maecker, S. Rosenberg, 2011, Molecular Cancer Therapeutics.

CPD Damage Recognition by Transcribing RNA Polymerase II

S. Korsmeyer, D. Vaux, S. Lowe, 2007 .

Discovery of a Potent and Selective BCL-XL Inhibitor with in Vivo Activity.

Brian J. Smith, C. Tse, A. Petros, 2014, ACS medicinal chemistry letters.

Activity of the Bcl-2 Family Inhibitor ABT-263 in a Panel of Small Cell Lung Cancer Xenograft Models

C. Tse, S. Fesik, S. Rosenberg, 2008, Clinical Cancer Research.

MCL-1 Is a Key Determinant of Breast Cancer Cell Survival: Validation of MCL-1 Dependency Utilizing a Highly Selective Small Molecule Inhibitor

Xin Lu, J. Leverson, W. N. Pappano, 2015, Molecular Cancer Therapeutics.

ABT-263 and rapamycin act cooperatively to kill lymphoma cells in vitro and in vivo

C. Tse, S. Fesik, S. Chemburkar, 2008, Molecular Cancer Therapeutics.

Structure-Based Design of A-1293102, a Potent and Selective BCL-XL Inhibitor.

Chaohong Sun, Z. Tao, P. Kovar, 2021, ACS medicinal chemistry letters.

The Bcl-2 inhibitor ABT-263 enhances the response of multiple chemotherapeutic regimens in hematologic tumors in vivo

Saul H. Rosenberg, Stephen W. Fesik, C. Tse, 2010, Cancer Chemotherapy and Pharmacology.

Discovery of A-1331852, a First-in-Class, Potent, and Orally-Bioavailable BCL-XL Inhibitor

Xiaohong Song, Z. Tao, P. Kovar, 2020, ACS medicinal chemistry letters.

Structure-activity studies for a novel series of tricyclic substituted hexahydrobenz[e]isoindole alpha(1A) adrenoceptor antagonists as potential agents for the symptomatic treatment of benign prostatic hyperplasia (BPH).

S. Elmore, M. Wendt, S. Condon, 2000, Journal of medicinal chemistry.

N-aryl-benzimidazolones as novel small molecule HSP90 inhibitors.

Jun Chen, Saul H Rosenberg, Xiaohong Song, 2010, Bioorganic & medicinal chemistry letters.

Discovery of a potent and selective Bcl-2 inhibitor using SAR by NMR.

Renaldo Mendoza, Saul H Rosenberg, Cheol-Min Park, 2010, Bioorganic & medicinal chemistry letters.

Methylpyrrole inhibitors of BET bromodomains.

A. Petros, Chaohong Sun, N. Soni, 2017, Bioorganic & medicinal chemistry letters.

The pursuit of differentiated ligands for the glucocorticoid receptor.

S. Elmore, P. Kym, M. Kort, 2003, Current topics in medicinal chemistry.

ABT-263: a potent and orally bioavailable Bcl-2 family inhibitor.

S. Fesik, Eric F. Johnson, S. Rosenberg, 2008, Cancer research.

MCL-1 Is a Key Determinant of Breast Cancer Cell Survival: Validation of MCL-1 Dependency Utilizing a Highly Selective Small Molecule Inhibitor

Xin Lu, J. Leverson, S. Elmore, 2015, Molecular Cancer Therapeutics.

The Bcl-2/Bcl-XL/Bcl-w Inhibitor, Navitoclax, Enhances the Activity of Chemotherapeutic Agents In Vitro and In Vivo

H. Maecker, S. Rosenberg, J. Leverson, 2011, Molecular Cancer Therapeutics.

ABT-263 and rapamycin act cooperatively to kill lymphoma cells in vitro and in vivo

S. Fesik, S. Chemburkar, S. Rosenberg, 2008, Molecular Cancer Therapeutics.

Fragment-Based, Structure-Enabled Discovery of Novel Pyridones and Pyridone Macrocycles as Potent Bromodomain and Extra-Terminal Domain (BET) Family Bromodomain Inhibitors.

A. Petros, P. Kovar, Chang H. Park, 2017, Journal of medicinal chemistry.

Methylpyrrole inhibitors of BET bromodomains.

A. Petros, N. Soni, P. Kovar, 2017, Bioorganic & medicinal chemistry letters.

Chang H. Park, D. Albert, Emily J. Faivre, 2017, Journal of medicinal chemistry.

Discovery and structure-activity relationship of antagonists of B-cell lymphoma 2 family proteins with chemopotentiation activity in vitro and in vivo.

A. Petros, S. Fesik, S. Ng, 2006, Journal of medicinal chemistry.