Publications by authors named "Paul Kirschmeier"

60Publications

Concurrent Dexamethasone Limits the Clinical Benefit of Immune Checkpoint Blockade in Glioblastoma.

Authors:
J Bryan Iorgulescu Prafulla C Gokhale Maria C Speranza Benjamin K Eschle Michael J Poitras Margaret K Wilkens Kara M Soroko Chhayheng Chhoeu Aine Knott Yan Gao Mary Jane Lim-Fat Gregory J Baker Dennis M Bonal Quang-Dé Nguyen Gareth R L Grant Keith L Ligon Peter K Sorger E Antonio Chiocca Ana C Anderson Paul T Kirschmeier Arlene H Sharpe Gordon J Freeman David A Reardon

Clin Cancer Res 2021 Jan 25;27(1):276-287. Epub 2020 Nov 25.

Department of Medical Oncology, Dana-Farber Cancer Institute, Boston, Massachusetts.

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January 2021

Dynamic single-cell RNA sequencing identifies immunotherapy persister cells following PD-1 blockade.

Authors:
Kartik Sehgal Andrew J Portell Elena V Ivanova Patrick H Lizotte Navin R Mahadevan Jonathan R Greene Amir Vajdi Carino Gurjao Tyler Teceno Luke J Taus Tran C Thai Shunsuke Kitajima Derek Liu Tetsuo Tani Moataz Noureddine Christie J Lau Paul T Kirschmeier David Liu Marios Giannakis Russell W Jenkins Prafulla C Gokhale Silvia Goldoni Maria Pinzon-Ortiz William D Hastings Peter Hammerman Juan J Miret Cloud P Paweletz David A Barbie

J Clin Invest 2020 Nov 5. Epub 2020 Nov 5.

Department of Medical Oncology, Dana-Farber Cancer Institute, Boston, United States of America.

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November 2020

Genomic and pathological heterogeneity in clinically diagnosed small cell lung cancer in never/light smokers identifies therapeutically targetable alterations.

Authors:
Atsuko Ogino Jihyun Choi Mika Lin Margaret K Wilkens Antonio Calles Man Xu Anika E Adeni Emily S Chambers Marzia Capelletti Mohit Butaney Nathanael S Gray Prafulla C Gokhale Sangeetha Palakurthi Paul Kirschmeier Geoffrey R Oxnard Lynette M Sholl Pasi A Jänne

Mol Oncol 2021 Jan 25;15(1):27-42. Epub 2020 Nov 25.

Department of Medical Oncology, Dana-Farber Cancer Institute, Boston, MA, USA.

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January 2021

Treatment-Induced Tumor Dormancy through YAP-Mediated Transcriptional Reprogramming of the Apoptotic Pathway.

Authors:
Kari J Kurppa Yao Liu Ciric To Tinghu Zhang Mengyang Fan Amir Vajdi Erik H Knelson Yingtian Xie Klothilda Lim Paloma Cejas Andrew Portell Patrick H Lizotte Scott B Ficarro Shuai Li Ting Chen Heidi M Haikala Haiyun Wang Magda Bahcall Yang Gao Sophia Shalhout Steffen Boettcher Bo Hee Shin Tran Thai Margaret K Wilkens Michelle L Tillgren Mierzhati Mushajiang Man Xu Jihyun Choi Arrien A Bertram Benjamin L Ebert Rameen Beroukhim Pratiti Bandopadhayay Mark M Awad Prafulla C Gokhale Paul T Kirschmeier Jarrod A Marto Fernando D Camargo Rizwan Haq Cloud P Paweletz Kwok-Kin Wong David A Barbie Henry W Long Nathanael S Gray Pasi A Jänne

Cancer Cell 2020 01;37(1):104-122.e12

Department of Medical Oncology, Dana-Farber Cancer Institute and Harvard Medical School, Boston, MA 02215, USA; Belfer Center for Applied Cancer Science, Dana-Farber Cancer Institute, Boston, MA 02215, USA; Lowe Center for Thoracic Oncology, Dana-Farber Cancer Institute, 450 Brookline Avenue, LC4114, Boston, MA 02215, USA. Electronic address:

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January 2020

The CHK1 Inhibitor Prexasertib Exhibits Monotherapy Activity in High-Grade Serous Ovarian Cancer Models and Sensitizes to PARP Inhibition.

Authors:
Kalindi Parmar Bose S Kochupurakkal Jean-Bernard Lazaro Zhigang C Wang Sangeetha Palakurthi Paul T Kirschmeier Chunyu Yang Larissa A Sambel Anniina Färkkilä Elizaveta Reznichenko Hunter D Reavis Connor E Dunn Lee Zou Khanh T Do Panagiotis A Konstantinopoulos Ursula A Matulonis Joyce F Liu Alan D D'Andrea Geoffrey I Shapiro

Clin Cancer Res 2019 10 13;25(20):6127-6140. Epub 2019 Aug 13.

Center for DNA Damage and Repair, Dana-Farber Cancer Institute, Boston, Massachusetts.

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October 2019

The Combined Effect of FGFR Inhibition and PD-1 Blockade Promotes Tumor-Intrinsic Induction of Antitumor Immunity.

Authors:
Sangeetha Palakurthi Mari Kuraguchi Sima J Zacharek Enrique Zudaire Wei Huang Dennis M Bonal Jeffrey Liu Abha Dhaneshwar Kristin DePeaux Martha R Gowaski Dyane Bailey Samuel N Regan Elena Ivanova Catherine Ferrante Jessie M English Aditya Khosla Andrew H Beck Julie A Rytlewski Catherine Sanders Sylvie Laquerre Mark A Bittinger Paul T Kirschmeier Kathryn Packman Pasi A Janne Christopher Moy Kwok-Kin Wong Raluca I Verona Matthew V Lorenzi

Cancer Immunol Res 2019 Sep 22;7(9):1457-1471. Epub 2019 Jul 22.

Janssen, Pharmaceutical Companies of Johnson & Johnson, Spring House, Pennsylvania.

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September 2019

Olaparib and α-specific PI3K inhibitor alpelisib for patients with epithelial ovarian cancer: a dose-escalation and dose-expansion phase 1b trial.

Authors:
Panagiotis A Konstantinopoulos William T Barry Michael Birrer Shannon N Westin Karen A Cadoo Geoffrey I Shapiro Erica L Mayer Roisin E O'Cearbhaill Robert L Coleman Bose Kochupurakkal Christin Whalen Jennifer Curtis Sarah Farooq Weixiu Luo Julia Eismann Mary K Buss Carol Aghajanian Gordon B Mills Sangeetha Palakurthi Paul Kirschmeier Joyce Liu Lewis C Cantley Scott H Kaufmann Elizabeth M Swisher Alan D D'Andrea Eric Winer Gerburg M Wulf Ursula A Matulonis

Lancet Oncol 2019 04 14;20(4):570-580. Epub 2019 Mar 14.

Dana-Farber Cancer Institute, Boston, MA, USA.

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April 2019

Suppression of Myeloid Cell Arginase Activity leads to Therapeutic Response in a NSCLC Mouse Model by Activating Anti-Tumor Immunity.

Authors:
Juan J Miret Paul Kirschmeier Shohei Koyama Mingrui Zhu Yvonne Y Li Yujiro Naito Min Wu Venkat S Malladi Wei Huang William Walker Sangeetha Palakurthi Glenn Dranoff Peter S Hammerman Chad V Pecot Kwok-Kin Wong Esra A Akbay

J Immunother Cancer 2019 02 6;7(1):32. Epub 2019 Feb 6.

Department of Pathology, University of Texas Southwestern Medical Center, Dallas, TX, USA.

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February 2019

Targeting MYC dependency in ovarian cancer through inhibition of CDK7 and CDK12/13.

Authors:
Mei Zeng Nicholas P Kwiatkowski Tinghu Zhang Behnam Nabet Mousheng Xu Yanke Liang Chunshan Quan Jinhua Wang Mingfeng Hao Sangeetha Palakurthi Shan Zhou Qing Zeng Paul T Kirschmeier Khyati Meghani Alan L Leggett Jun Qi Geoffrey I Shapiro Joyce F Liu Ursula A Matulonis Charles Y Lin Panagiotis A Konstantinopoulos Nathanael S Gray

Elife 2018 11 13;7. Epub 2018 Nov 13.

Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, United States.

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November 2018

Suppression of STING Associated with LKB1 Loss in KRAS-Driven Lung Cancer.

Authors:
Shunsuke Kitajima Elena Ivanova Sujuan Guo Ryohei Yoshida Marco Campisi Shriram K Sundararaman Shoichiro Tange Yoichiro Mitsuishi Tran C Thai Sayuri Masuda Brandon P Piel Lynette M Sholl Paul T Kirschmeier Cloud P Paweletz Hideo Watanabe Mamiko Yajima David A Barbie

Cancer Discov 2019 01 8;9(1):34-45. Epub 2018 Oct 8.

Department of Medical Oncology, Dana-Farber Cancer Institute, Boston, Massachusetts.

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January 2019

A High-Throughput Immune-Oncology Screen Identifies EGFR Inhibitors as Potent Enhancers of Antigen-Specific Cytotoxic T-lymphocyte Tumor Cell Killing.

Authors:
Patrick H Lizotte Ruey-Long Hong Troy A Luster Megan E Cavanaugh Luke J Taus Stephen Wang Abha Dhaneshwar Naomi Mayman Aaron Yang Meghana Kulkarni Lauren Badalucco Erica Fitzpatrick Hsiang-Fong Kao Mari Kuraguchi Mark Bittinger Paul T Kirschmeier Nathanael S Gray David A Barbie Pasi A Jänne

Cancer Immunol Res 2018 12 21;6(12):1511-1523. Epub 2018 Sep 21.

Belfer Center for Applied Cancer Science, Boston, Massachusetts.

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December 2018

Overcoming Resistance to Dual Innate Immune and MEK Inhibition Downstream of KRAS.

Authors:
Shunsuke Kitajima Hajime Asahina Ting Chen Sujuan Guo Laura Gutierrez Quiceno Jillian D Cavanaugh Ashley A Merlino Shoichiro Tange Hideki Terai Jong Wook Kim Xiaoen Wang Shan Zhou Man Xu Stephen Wang Zehua Zhu Tran C Thai Chiaki Takahashi Yujin Wang Richard Neve Susanna Stinson Pablo Tamayo Hideo Watanabe Paul T Kirschmeier Kwok-Kin Wong David A Barbie

Cancer Cell 2018 09;34(3):439-452.e6

Department of Medical Oncology, Dana-Farber Cancer Institute, Boston, MA 02215, USA. Electronic address:

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September 2018

Unraveling the clinicopathological features driving the emergence of mutations in metastatic breast cancer.

Authors:
Yanan Kuang Bilal Siddiqui Jiani Hu Matthew Pun MacIntosh Cornwell Gilles Buchwalter Melissa E Hughes Nikhil Wagle Paul Kirschmeier Pasi A Jänne Cloud P Paweletz Nancy U Lin Ian E Krop William T Barry Eric P Winer Myles Brown Rinath Jeselsohn

NPJ Breast Cancer 2018 2;4:22. Epub 2018 Aug 2.

2Department of Medical Oncology, Dana Farber-Cancer Institute, Boston, MA 02215 USA.

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August 2018

Amplification of Wild-type Imparts Resistance to Crizotinib in Exon 14 Mutant Non-Small Cell Lung Cancer.

Authors:
Magda Bahcall Mark M Awad Lynette M Sholl Frederick H Wilson Man Xu Stephen Wang Sangeetha Palakurthi Jihyun Choi Elena V Ivanova Giulia C Leonardi Bryan C Ulrich Cloud P Paweletz Paul T Kirschmeier Masayuki Watanabe Hideo Baba Mizuki Nishino Rebecca J Nagy Richard B Lanman Marzia Capelletti Emily S Chambers Amanda J Redig Paul A VanderLaan Daniel B Costa Yu Imamura Pasi A Jänne

Clin Cancer Res 2018 12 2;24(23):5963-5976. Epub 2018 Aug 2.

Lowe Center for Thoracic Oncology, Dana-Farber Cancer Institute and Harvard Medical School, Boston, Massachusetts.

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December 2018

MK-8353: Discovery of an Orally Bioavailable Dual Mechanism ERK Inhibitor for Oncology.

Authors:
Sobhana Babu Boga Yongqi Deng Liang Zhu Yang Nan Alan B Cooper Gerald W Shipps Ronald Doll Neng-Yang Shih Hugh Zhu Robert Sun Tong Wang Sunil Paliwal Hon-Chung Tsui Xiaolei Gao Xin Yao Jagdish Desai James Wang Abdul Basit Alhassan Joseph Kelly Mehul Patel Kiran Muppalla Subrahmanyam Gudipati Li-Kang Zhang Alexei Buevich David Hesk Donna Carr Priya Dayananth Stuart Black Hong Mei Kathleen Cox Bradley Sherborne Alan W Hruza Li Xiao Weihong Jin Brian Long Gongjie Liu Stacey A Taylor Paul Kirschmeier William T Windsor Robert Bishop Ahmed A Samatar

ACS Med Chem Lett 2018 Jul 14;9(7):761-767. Epub 2018 Jun 14.

Merck & Co., Inc., 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, United States.

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July 2018

Discovery of 3(S)-thiomethyl pyrrolidine ERK inhibitors for oncology.

Authors:
Sobhana Babu Boga Abdul-Basit Alhassan Alan B Cooper Ronald Doll Neng-Yang Shih Gerald Shipps Yongqi Deng Hugh Zhu Yang Nan Robert Sun Liang Zhu Jagdish Desai Mehul Patel Kiran Muppalla Xiaolei Gao James Wang Xin Yao Joseph Kelly Subrahmanyam Gudipati Sunil Paliwal Hon-Chung Tsui Tong Wang Bradley Sherborne Li Xiao Alan Hruza Alexei Buevich Li-Kang Zhang David Hesk Ahmed A Samatar Donna Carr Brian Long Stuart Black Priya Dayananth William Windsor Paul Kirschmeier Robert Bishop

Bioorg Med Chem Lett 2018 06 26;28(11):2029-2034. Epub 2018 Apr 26.

Discovery Chemistry, Merck & Co., Inc., 2015 Galloping Hill Rd, Kenilworth, NJ 07033, United States.

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June 2018

Development of MK-8353, an orally administered ERK1/2 inhibitor, in patients with advanced solid tumors.

Authors:
Stergios J Moschos Ryan J Sullivan Wen-Jen Hwu Ramesh K Ramanathan Alex A Adjei Peter C Fong Ronnie Shapira-Frommer Hussein A Tawbi Joseph Rubino Thomas S Rush Da Zhang Nathan R Miselis Ahmed A Samatar Patrick Chun Eric H Rubin James Schiller Brian J Long Priya Dayananth Donna Carr Paul Kirschmeier W Robert Bishop Yongqi Deng Alan Cooper Gerald W Shipps Blanca Homet Moreno Lidia Robert Antoni Ribas Keith T Flaherty

JCI Insight 2018 02 22;3(4). Epub 2018 Feb 22.

Massachusetts General Hospital Cancer Center, Boston, Massachusetts, USA.

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February 2018

Recurrent ubiquitin B silencing in gynecological cancers establishes dependence on ubiquitin C.

Authors:
Alexia T Kedves Scott Gleim Xiaoyou Liang Dennis M Bonal Frederic Sigoillot Fred Harbinski Sneha Sanghavi Christina Benander Elizabeth George Prafulla C Gokhale Quang-De Nguyen Paul T Kirschmeier Robert J Distel Jeremy Jenkins Michael S Goldberg William C Forrester

J Clin Invest 2017 12 13;127(12):4554-4568. Epub 2017 Nov 13.

Chemical Biology and Therapeutics, Novartis Institutes for Biomedical Research, Cambridge, Massachusetts, USA.

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December 2017

Profiling of PD-1 Blockade Using Organotypic Tumor Spheroids.

Authors:
Russell W Jenkins Amir R Aref Patrick H Lizotte Elena Ivanova Susanna Stinson Chensheng W Zhou Michaela Bowden Jiehui Deng Hongye Liu Diana Miao Meng Xiao He William Walker Gao Zhang Tian Tian Chaoran Cheng Zhi Wei Sangeetha Palakurthi Mark Bittinger Hans Vitzthum Jong Wook Kim Ashley Merlino Max Quinn Chandrasekar Venkataramani Joshua A Kaplan Andrew Portell Prafulla C Gokhale Bart Phillips Alicia Smart Asaf Rotem Robert E Jones Lauren Keogh Maria Anguiano Lance Stapleton Zhiheng Jia Michal Barzily-Rokni Israel Cañadas Tran C Thai Marc R Hammond Raven Vlahos Eric S Wang Hua Zhang Shuai Li Glenn J Hanna Wei Huang Mai P Hoang Adriano Piris Jean-Pierre Eliane Anat O Stemmer-Rachamimov Lisa Cameron Mei-Ju Su Parin Shah Benjamin Izar Manisha Thakuria Nicole R LeBoeuf Guilherme Rabinowits Viswanath Gunda Sareh Parangi James M Cleary Brian C Miller Shunsuke Kitajima Rohit Thummalapalli Benchun Miao Thanh U Barbie Vivek Sivathanu Joshua Wong William G Richards Raphael Bueno Charles H Yoon Juan Miret Meenhard Herlyn Levi A Garraway Eliezer M Van Allen Gordon J Freeman Paul T Kirschmeier Jochen H Lorch Patrick A Ott F Stephen Hodi Keith T Flaherty Roger D Kamm Genevieve M Boland Kwok-Kin Wong David Dornan Cloud Peter Paweletz David A Barbie

Cancer Discov 2018 02 3;8(2):196-215. Epub 2017 Nov 3.

Department of Medical Oncology, Dana-Farber Cancer Institute, Boston, Massachusetts.

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February 2018

Phase 1 safety, pharmacokinetic and pharmacodynamic study of the cyclin-dependent kinase inhibitor dinaciclib administered every three weeks in patients with advanced malignancies.

Authors:
Monica M Mita Alain C Mita Jennifer L Moseley Jennifer Poon Karen A Small Ying-Ming Jou Paul Kirschmeier Da Zhang Yali Zhu Paul Statkevich Kamelesh K Sankhala John Sarantopoulos James M Cleary Lucian R Chirieac Scott J Rodig Rajat Bannerji Geoffrey I Shapiro

Br J Cancer 2017 Oct 31;117(9):1258-1268. Epub 2017 Aug 31.

Early Drug Development Center, Department of Medical Oncology, Dana-Farber Cancer Institute, 450 Brookline Avenue, Boston, MA 02215, USA.

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October 2017

Establishment of Patient-Derived Tumor Xenograft Models of Epithelial Ovarian Cancer for Preclinical Evaluation of Novel Therapeutics.

Authors:
Joyce F Liu Sangeetha Palakurthi Qing Zeng Shan Zhou Elena Ivanova Wei Huang Ioannis K Zervantonakis Laura M Selfors Yiping Shen Colin C Pritchard Mei Zheng Vilmos Adleff Eniko Papp Huiying Piao Marian Novak Susan Fotheringham Gerburg M Wulf Jessie English Paul T Kirschmeier Victor E Velculescu Cloud Paweletz Gordon B Mills David M Livingston Joan S Brugge Ursula A Matulonis Ronny Drapkin

Clin Cancer Res 2017 Mar 29;23(5):1263-1273. Epub 2016 Aug 29.

Department of Obstetrics and Gynecology, Penn Ovarian Cancer Research Center, University of Pennsylvania, Philadelphia, Pennsylvania.

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March 2017

Bias-Corrected Targeted Next-Generation Sequencing for Rapid, Multiplexed Detection of Actionable Alterations in Cell-Free DNA from Advanced Lung Cancer Patients.

Authors:
Cloud P Paweletz Adrian G Sacher Chris K Raymond Ryan S Alden Allison O'Connell Stacy L Mach Yanan Kuang Leena Gandhi Paul Kirschmeier Jessie M English Lee P Lim Pasi A Jänne Geoffrey R Oxnard

Clin Cancer Res 2016 Feb 12;22(4):915-22. Epub 2015 Oct 12.

Lowe Center for Thoracic Oncology, Dana-Farber Cancer Institute, Boston, Massachusetts.

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February 2016

Pathological glycogenesis through glycogen synthase 1 and suppression of excessive AMP kinase activity in myeloid leukemia cells.

Authors:
Haymanti Bhanot Mamatha M Reddy Atsushi Nonami Ellen L Weisberg Dennis Bonal Paul T Kirschmeier Sabrina Salgia Klaus Podar Ilene Galinsky Tirumala K Chowdary Donna Neuberg Giovanni Tonon Richard M Stone John Asara James D Griffin Martin Sattler

Leukemia 2015 Jul 23;29(7):1555-1563. Epub 2015 Feb 23.

Department of Medical Oncology, Boston, MA, 02215, USA.

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July 2015

Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase.

Authors:
Yongqi Deng Gerald W Shipps Alan Cooper Jessie M English D Allen Annis Donna Carr Yang Nan Tong Wang Hugh Y Zhu Cheng-Chi Chuang Priya Dayananth Alan W Hruza Li Xiao Weihong Jin Paul Kirschmeier William T Windsor Ahmed A Samatar

J Med Chem 2014 Nov 22;57(21):8817-26. Epub 2014 Oct 22.

Merck Research Laboratories , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.

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November 2014

Evaluating TBK1 as a therapeutic target in cancers with activated IRF3.

Authors:
Asli Muvaffak Qi Pan Haiyan Yan Rafael Fernandez Jongwon Lim Brian Dolinski Thi T Nguyen Peter Strack Stephen Wu Rossana Chung Weiqun Zhang Chris Hulton Steven Ripley Heather Hirsch Kumiko Nagashima Kwok-Kin Wong Pasi A Jánne Cynthia Seidel-Dugan Leigh Zawel Paul T Kirschmeier Richard E Middleton Erick J Morris Yan Wang

Mol Cancer Res 2014 Jul 21;12(7):1055-66. Epub 2014 Apr 21.

Merck Research Laboratories, Boston, Massachusetts

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July 2014

New class of azaheptapyridine FPT inhibitors as potential cancer therapy agents.

Authors:
Hugh Y Zhu Jagdish Desai Alan B Cooper James Wang Dinananth F Rane Paul Kirschmeier Corey Strickland Ming Liu Amin A Nomeir Viyyoor M Girijavallabhan

Bioorg Med Chem Lett 2014 Feb 2;24(4):1228-31. Epub 2014 Jan 2.

Merck Research Laboratories, 2015 Galloping Hill Rd, Kenilworth, NJ 07033, USA.

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February 2014

Noninvasive detection of response and resistance in EGFR-mutant lung cancer using quantitative next-generation genotyping of cell-free plasma DNA.

Authors:
Geoffrey R Oxnard Cloud P Paweletz Yanan Kuang Stacy L Mach Allison O'Connell Melissa M Messineo Jason J Luke Mohit Butaney Paul Kirschmeier David M Jackman Pasi A Jänne

Clin Cancer Res 2014 Mar 15;20(6):1698-1705. Epub 2014 Jan 15.

Department of Medical Oncology, Brigham and Women's Hospital & Harvard Medical School Boston, MA.

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March 2014

Modulating the interaction between CDK2 and cyclin A with a quinoline-based inhibitor.

Authors:
Yongqi Deng Gerald W Shipps Lianyun Zhao M Arshad Siddiqui Janeta Popovici-Muller Patrick J Curran Jose S Duca Alan W Hruza Thierry O Fischmann Vincent S Madison Rumin Zhang Charles W McNemar Todd W Mayhood Rosalinda Syto Allen Annis Paul Kirschmeier Emma M Lees David A Parry William T Windsor

Bioorg Med Chem Lett 2014 Jan 23;24(1):199-203. Epub 2013 Nov 23.

Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. Electronic address:

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January 2014

A first-in-human, phase 1, dose-escalation study of dinaciclib, a novel cyclin-dependent kinase inhibitor, administered weekly in subjects with advanced malignancies.

Authors:
John J Nemunaitis Karen A Small Paul Kirschmeier Da Zhang Yali Zhu Ying-Ming Jou Paul Statkevich Siu-Long Yao Rajat Bannerji

J Transl Med 2013 Oct 16;11:259. Epub 2013 Oct 16.

Mary Crowley Cancer Research Centers, 1700 Pacific Avenue, Suite 1100, Dallas, TX 75201, USA.

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October 2013

Discovery of a novel ERK inhibitor with activity in models of acquired resistance to BRAF and MEK inhibitors.

Authors:
Erick J Morris Sharda Jha Clifford R Restaino Priya Dayananth Hugh Zhu Alan Cooper Donna Carr Yongi Deng Weihong Jin Stuart Black Brian Long Jenny Liu Edward Dinunzio William Windsor Rumin Zhang Shuxia Zhao Minilik H Angagaw Elaine M Pinheiro Jagdish Desai Li Xiao Gerald Shipps Alan Hruza James Wang Joe Kelly Sunil Paliwal Xiaolei Gao Boga Sobhana Babu Liang Zhu Pierre Daublain Ling Zhang Bart A Lutterbach Marc R Pelletier Ulrike Philippar Phieng Siliphaivanh David Witter Paul Kirschmeier W Robert Bishop Daniel Hicklin D Gary Gilliland Lata Jayaraman Leigh Zawel Stephen Fawell Ahmed A Samatar

Cancer Discov 2013 Jul 24;3(7):742-50. Epub 2013 Apr 24.

Discovery Oncology Merck Research Laboratories, Merck Research Laboratories, Rahway, New Jersey, USA.

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July 2013

SCH 1473759, a novel Aurora inhibitor, demonstrates enhanced anti-tumor activity in combination with taxanes and KSP inhibitors.

Authors:
Andrea D Basso Ming Liu Kimberly Gray Seema Tevar Suining Lee Lianzhu Liang Abdul Ponery Elizabeth B Smith Frederick J Monsma Tao Yu Yonglian Zhang Angela D Kerekes Sara Esposite Yushi Xiao Jayaram R Tagat Daniel J Hicklin Paul Kirschmeier

Cancer Chemother Pharmacol 2011 Oct 5;68(4):923-33. Epub 2011 Feb 5.

Department of Oncology, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.

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October 2011

SCH 2047069, a novel oral kinesin spindle protein inhibitor, shows single-agent antitumor activity and enhances the efficacy of chemotherapeutics.

Authors:
Andrea D Basso Ming Liu Chaoyang Dai Kimberly Gray Lissette Nale Seema Tevar Suining Lee Lianzhu Liang Abdul Ponery Bohdan Yaremko Elizabeth Smith Huadong Tang Payal R Sheth M Arshad Siddiqui Daniel J Hicklin Paul Kirschmeier

Mol Cancer Ther 2010 Nov 26;9(11):2993-3002. Epub 2010 Oct 26.

Department of Oncology, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07093, USA.

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November 2010

Discovery of Dinaciclib (SCH 727965): A Potent and Selective Inhibitor of Cyclin-Dependent Kinases.

Authors:
Kamil Paruch Michael P Dwyer Carmen Alvarez Courtney Brown Tin-Yau Chan Ronald J Doll Kerry Keertikar Chad Knutson Brian McKittrick Jocelyn Rivera Randall Rossman Greg Tucker Thierry Fischmann Alan Hruza Vincent Madison Amin A Nomeir Yaolin Wang Paul Kirschmeier Emma Lees David Parry Nicole Sgambellone Wolfgang Seghezzi Lesley Schultz Frances Shanahan Derek Wiswell Xiaoying Xu Quiao Zhou Ray A James Vidyadhar M Paradkar Haengsoon Park Laura R Rokosz Tara M Stauffer Timothy J Guzi

ACS Med Chem Lett 2010 Aug 17;1(5):204-8. Epub 2010 May 17.

Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, New Jersey 07033.

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August 2010

Dinaciclib (SCH 727965), a novel and potent cyclin-dependent kinase inhibitor.

Authors:
David Parry Timothy Guzi Frances Shanahan Nicole Davis Deepa Prabhavalkar Derek Wiswell Wolfgang Seghezzi Kamil Paruch Michael P Dwyer Ronald Doll Amin Nomeir William Windsor Thierry Fischmann Yaolin Wang Martin Oft Taiying Chen Paul Kirschmeier Emma M Lees

Mol Cancer Ther 2010 Aug 27;9(8):2344-53. Epub 2010 Jul 27.

Merck Research Laboratory-Palo Alto, 901 California Avenue, Palo Alto, CA 94304-1104, USA.

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August 2010

Semi-synthetic aristolactams--inhibitors of CDK2 enzyme.

Authors:
Vinod R Hegde Scott Borges Haiyan Pu Mahesh Patel Vincent P Gullo Bonnie Wu Paul Kirschmeier Michael J Williams Vincent Madison Thierry Fischmann Tze-Ming Chan

Bioorg Med Chem Lett 2010 Feb 7;20(4):1384-7. Epub 2010 Jan 7.

Schering Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.

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February 2010

Discovery of C-imidazole azaheptapyridine FPT inhibitors.

Authors:
Hugh Y Zhu Alan B Cooper Jagdish Desai George Njoroge Paul Kirschmeier W Robert Bishop Corey Strickland Alan Hruza Ronald J Doll Viyyoor M Girijavallabhan

Bioorg Med Chem Lett 2010 Feb 6;20(3):1134-6. Epub 2009 Dec 6.

Schering Plough Research Institute, 2015 Galloping Hill Rd, Kenilworth, NJ 07033, USA.

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February 2010

Continuous and intermittent dosing of lonafarnib potentiates the therapeutic efficacy of docetaxel on preclinical human prostate cancer models.

Authors:
Gongjie Liu Stacey A Taylor Cindy H Marrinan Yunsheng Hsieh W Robert Bishop Paul Kirschmeier Brian J Long

Int J Cancer 2009 Dec;125(11):2711-20

Schering-Plough Research Institute, Biological Research - Oncology, Kenilworth, NJ 07033, USA.

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December 2009

Rho Family GTPase modification and dependence on CAAX motif-signaled posttranslational modification.

Authors:
Patrick J Roberts Natalia Mitin Patricia J Keller Emily J Chenette James P Madigan Rachel O Currin Adrienne D Cox Oswald Wilson Paul Kirschmeier Channing J Der

J Biol Chem 2008 Sep 9;283(37):25150-63. Epub 2008 Jul 9.

Lineberger Comprehensive Cancer Center, Division of Pharmacotherapy and Experimental Therapeutics, Department of Pharmacology, University of North Carolina, Chapel Hill, NC 27599, USA.

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September 2008

Combining the farnesyltransferase inhibitor lonafarnib with paclitaxel results in enhanced growth inhibitory effects on human ovarian cancer models in vitro and in vivo.

Authors:
Stacey A Taylor Cindy H Marrinan Gongjie Liu Lissette Nale W Robert Bishop Paul Kirschmeier Ming Liu Brian J Long

Gynecol Oncol 2008 Apr 31;109(1):97-106. Epub 2008 Jan 31.

Schering-Plough Research Institute, Biological Research-Oncology, 2015 Galloping Hill Road, K15-2-2700, Kenilworth, NJ 07033, USA.

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April 2008

Enhancement of the antitumor activity of tamoxifen and anastrozole by the farnesyltransferase inhibitor lonafarnib (SCH66336).

Authors:
Gonjgie Liu Cindy H Marrinan Stacey A Taylor Stuart Black Andrea D Basso Paul Kirschmeier W Robert Bishop Ming Liu Brian J Long

Anticancer Drugs 2007 Sep;18(8):923-31

Department of Biological Research - Oncology, Schering-Plough Research Institute, Kenilworth, New Jersey 07033, USA.

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September 2007

Phase I and pharmacokinetic study of the oral farnesyltransferase inhibitor lonafarnib administered twice daily to pediatric patients with advanced central nervous system tumors using a modified continuous reassessment method: a Pediatric Brain Tumor Consortium Study.

Authors:
Mark W Kieran Roger J Packer Arzu Onar Susan M Blaney Peter Phillips Ian F Pollack J Russell Geyer Sri Gururangan Anu Banerjee Stewart Goldman Christopher D Turner Jean B Belasco Alberto Broniscer Yali Zhu Emily Frank Paul Kirschmeier Paul Statkevich Antoine Yver James M Boyett Larry E Kun

J Clin Oncol 2007 Jul;25(21):3137-43

Dana-Farber Cancer Institute and Children's Hospital Boston, Boston, MA 02115, USA.

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July 2007

AKT1, AKT2 and AKT3-dependent cell survival is cell line-specific and knockdown of all three isoforms selectively induces apoptosis in 20 human tumor cell lines.

Authors:
Sandra Koseoglu Zhuomei Lu Chandra Kumar Paul Kirschmeier Jun Zou

Cancer Biol Ther 2007 May 9;6(5):755-62. Epub 2007 Feb 9.

Department of Tumor Biology, Schering-Plough Research Institute, Kenilworth, New Jersey, USA.

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May 2007

Identification of overexpression of orphan G protein-coupled receptor GPR49 in human colon and ovarian primary tumors.

Authors:
Terrill McClanahan Sandra Koseoglu Kathleen Smith Jeffrey Grein Eric Gustafson Stuart Black Paul Kirschmeier Ahmed A Samatar

Cancer Biol Ther 2006 Apr 19;5(4):419-26. Epub 2006 Apr 19.

DNAX Research Institute, Schering-Plough Research Institute, Kenilworth, New Jersey 07333, USA.

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April 2006

Lipid posttranslational modifications. Farnesyl transferase inhibitors.

Authors:
Andrea D Basso Paul Kirschmeier W Robert Bishop

J Lipid Res 2006 Jan 8;47(1):15-31. Epub 2005 Nov 8.

Schering-Plough Research Institute, Kenilworth, NJ 07033, USA.

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January 2006

The farnesyl transferase inhibitor (FTI) SCH66336 (lonafarnib) inhibits Rheb farnesylation and mTOR signaling. Role in FTI enhancement of taxane and tamoxifen anti-tumor activity.

Authors:
Andrea D Basso Asra Mirza Gongjie Liu Brian J Long W Robert Bishop Paul Kirschmeier

J Biol Chem 2005 Sep 8;280(35):31101-8. Epub 2005 Jul 8.

Department of Tumor Biology, Schering-Plough Research Institute, Kenilwort, New Jersey 07033, USA.

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September 2005

Integrative genomics revealed RAI3 is a cell growth-promoting gene and a novel P53 transcriptional target.

Authors:
Qun Wu Wei Ding Asra Mirza Tish Van Arsdale Iris Wei W Robert Bishop Andrea Basso Terri McClanahan Lin Luo Paul Kirschmeier Eric Gustafson Marco Hernandez Suxing Liu

J Biol Chem 2005 Apr 18;280(13):12935-43. Epub 2005 Jan 18.

Schering-Plough Research Institute, Kenilworth, New Jersey 07033, USA.

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April 2005

Bridgehead modification of trihalocycloheptabenzopyridine leads to a potent farnesyl protein transferase inhibitor with improved oral metabolic stability.

Authors:
F George Njoroge Bancha Vibulbhan Xiongwei Shi Corey Strickland Paul Kirschmeier Robert Bishop Amin Nomeir Viyyoor Girijavallabhan

Bioorg Med Chem Lett 2004 Dec;14(23):5899-902

Schering-Plough Research Institute, 2015 Galloping Hill Road, K-15-3-3545, Kenilworth, NJ 07033, USA.

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December 2004

Farnesyl protein transferase inhibitors targeting the catalytic zinc for enhanced binding.

Authors:
F George Njoroge Bancha Vibulbhan Patrick Pinto Corey Strickland Paul Kirschmeier W Robert Bishop V Girijavallabhan

Bioorg Med Chem Lett 2004 Dec;14(23):5877-80

Schering-Plough Research Institute, 2015 Galloping Hill Road, K-15-3-3545, Kenilworth, NJ 07033, USA.

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December 2004

Farnesyltransferase inhibitors as anticancer agents: critical crossroads.

Authors:
Ronald J Doll Paul Kirschmeier W Robert Bishop

Curr Opin Drug Discov Devel 2004 Jul;7(4):478-86

Department of Chemical Research, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033-1300, USA.

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July 2004

Development of a fluorescence polarization bead-based coupled assay to target different activity/conformation states of a protein kinase.

Authors:
Zhuomei Lu Zhizhang Yin Linda James Rosalinda Syto Jill M Stafford Sandra Koseoglu Todd Mayhood Joseph Myers William Windsor Paul Kirschmeier Ahmed A Samatar Bruce Malcolm Tammy C Turek-Etienne C Chandra Kumar

J Biomol Screen 2004 Jun;9(4):309-21

Department of Tumor Biology, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.

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June 2004

Phase I study of the farnesyltransferase inhibitor lonafarnib with paclitaxel in solid tumors.

Authors:
Fadlo R Khuri Bonnie S Glisson Edward S Kim Paul Statkevich Peter F Thall Michael L Meyers Roy S Herbst Reginald F Munden Craig Tendler Yali Zhu Sandra Bangert Elizabeth Thompson Charles Lu Xue-Mei Wang Dong M Shin Merrill S Kies Vali Papadimitrakopoulou Frank V Fossella Paul Kirschmeier W Robert Bishop Waun Ki Hong

Clin Cancer Res 2004 May;10(9):2968-76

Winship Cancer Institute, Emory University, Atlanta, Georgia 30322, USA.

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May 2004

Farnesyl transferase inhibitors: mechanism of action, translational studies and clinical evaluation.

Authors:
W Robert Bishop Paul Kirschmeier Charles Baum

Cancer Biol Ther 2003 Jul-Aug;2(4 Suppl 1):S96-104

Department of Biological Research-Oncology, Shering Plough Research Institute, Kenilworth, New Jersey 07033, USA.

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February 2004

Global transcriptional program of p53 target genes during the process of apoptosis and cell cycle progression.

Authors:
Asra Mirza Qun Wu Luquan Wang Terri McClanahan W Robert Bishop Ferdous Gheyas Wei Ding Beth Hutchins Tish Hockenberry Paul Kirschmeier Jonathan R Greene Suxing Liu

Oncogene 2003 Jun;22(23):3645-54

Tumor Biology Department, Schering-Plough Research Institute, 2015 Galloping Hill Road, K-15-4 (4600), Kenilworth, NJ 07033, USA.

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June 2003

Sch-66336 (sarasar) and other benzocycloheptapyridyl farnesyl protein transferase inhibitors: discovery, biology and clinical observations.

Authors:
Arthur G Taveras Paul Kirschmeier Charles M Baum

Curr Top Med Chem 2003 ;3(10):1103-14

Department of Medicinal Chemistry, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, New Jersey 07033, USA.

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June 2003

Preclinical and clinical evaluation of farnesyltransferase inhibitors.

Authors:
Charles Baum Paul Kirschmeier

Curr Oncol Rep 2003 Mar;5(2):99-107

Schering-Plough Research Institute, 2015 Galloping Hill Road, K-15-3-3200, Kenilworth, NJ 07033-1300, USA.

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March 2003

Exploring the role of bromine at C(10) of (+)-4-[2-[4-(8-chloro-3,10-dibromo- 6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11(R)-yl)-1-piperidinyl]-2- oxoethyl]-1-piperidinecarboxamide (Sch-66336): the discovery of indolocycloheptapyridine inhibitors of farnesyl protein transferase.

Authors:
Arthur G Taveras Cynthia Aki Jianping Chao Ronald J Doll Tarik Lalwani Viyyoor Girijavallabhan Corey L Strickland William T Windsor Patricia Weber Frank Hollinger Mark Snow Robert Patton Paul Kirschmeier Linda James Ming Liu Amin Nomeir

J Med Chem 2002 Aug;45(18):3854-64

Department of Chemistry and Tumor Biology, Schering-Plough Research Institute, Kenilworth, New Jersey 07033, USA.

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August 2002

Transcriptional regulation during p21WAF1/CIP1-induced apoptosis in human ovarian cancer cells.

Authors:
Qun Wu Paul Kirschmeier Tish Hockenberry Tong-Yuan Yang Diana L Brassard Luquan Wang Terri McClanahan Stuart Black Giovanni Rizzi Mary Lynn Musco Asra Mirza Suxing Liu

J Biol Chem 2002 Sep 22;277(39):36329-37. Epub 2002 Jul 22.

Tumor Biology Department, Schering-Plough Research Institute, Kenilworth, New Jersey 07033, USA.

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September 2002

Human survivin is negatively regulated by wild-type p53 and participates in p53-dependent apoptotic pathway.

Authors:
Asra Mirza Marnie McGuirk Tish N Hockenberry Qun Wu Hena Ashar Stuart Black Shu Fen Wen Luquan Wang Paul Kirschmeier W Robert Bishop Loretta L Nielsen Cecil B Pickett Suxing Liu

Oncogene 2002 Apr;21(17):2613-22

Tumor Biology Department, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, New Jersey, NJ 07033, USA.

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April 2002

Synthesis of 5,6-dihydro-11H-benzo[5,6]-cyclohepta[1,2-b]pyridin-11-ylidene)-1-piperidine-N-cyanoguanidine derivatives as inhibitors of ras farnesyl protein transferase.

Authors:
Alan B Cooper Corey L Strickland James Wang Jagdish Desai Paul Kirschmeier Robert Patton W Robert Bishop Patricia C Weber V Girijavallabhan

Bioorg Med Chem Lett 2002 Feb;12(4):601-5

Schering-Plough Research Institute, Department of Chemistry, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.

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February 2002

Inhibitors of farnesyl protein transferase and MEK1,2 induce apoptosis in fibroblasts transformed with farnesylated but not geranylgeranylated H-Ras.

Authors:
Diana L Brassard Jessie M English Michael Malkowski Paul Kirschmeier T L Nagabhushan W Robert Bishop

Exp Cell Res 2002 Feb;273(2):138-46

Biotechnology Development, Schering-Plough Research Institute, Union, New Jersey 07083, USA.

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February 2002