Nuclear (PET/SPECT) and optical imaging probes targeting the CXCR4 chemokine receptor

James C. Knight and Frank R. Wuest

Med. Chem. Commun., 2012, 3, 1039
DOI: 10.1039/c2md20117h

Comment: 2004’s fastest organic and biomolecular chemistry!

Caroline V. Potter, Graham McCann, Janet L. Dean, Adrian P. Kybett, Richard Kidd, Melanie James and Michelle Canning

J. Mater. Chem., 2004, 14, E17
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Structure-activity relationship study of CXCR4 antagonists bearing the cyclic pentapeptide scaffold: identification of the new pharmacophore

Tomohiro Tanaka, Hiroshi Tsutsumi, Wataru Nomura, Yasuaki Tanabe, Nami Ohashi, Ai Esaka, Chihiro Ochiai, Jun Sato, Kyoko Itotani, Tsutomu Murakami, Kenji Ohba, Naoki Yamamoto, Nobutaka Fujii and Hirokazu Tamamura

Org. Biomol. Chem., 2008, 6, 4374
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Peptide and peptidomimetic ligands for CXC chemokine receptor 4 (CXCR4)

Shinya Oishi and Nobutaka Fujii

Org. Biomol. Chem., 2012, 10, 5720
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Comment: 2004’s fastest organic and biomolecular chemistry!

Caroline V. Potter, Sarah Thomas, Janet L. Dean, Adrian P. Kybett, Richard Kidd, Melanie James and Helen Saxton

Chem. Commun., 2004, 2781
DOI: 10.1039/B417565B

Comment: 2004’s fastest organic and biomolecular chemistry!

Caroline V. Potter, Janet L. Dean, Adrian P. Kybett, Richard Kidd, Melanie James and Michelle Canning

Org. Biomol. Chem., 2004, 2, 3535
DOI: 10.1039/B417338B

Comment: 2004’s fastest organic and biomolecular chemistry!

Caroline V. Potter, Mike Corkill, Janet L. Dean, Adrian P. Kybett, Richard Kidd, Melanie James and Helen Saxton

New J. Chem., 2004, 28, 1395
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Imaging agents for the chemokine receptor 4 (CXCR4)

Joeri Kuil, Tessa Buckle and Fijs W. B. van Leeuwen

Chem. Soc. Rev., 2012, 41, 5239
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Comment: 2004’s fastest organic and biomolecular chemistry!

Caroline V. Potter, Janet Freshwater, Janet L. Dean, Adrian P. Kybett, Richard Kidd, Melanie James and Helen Saxton

Chem. Soc. Rev., 2004, 33, 567
DOI: 10.1039/B417566M

Structure-activity relationship study on artificial CXCR4 ligands possessing the cyclic pentapeptide scaffold: the exploration of amino acid residues of pentapeptides by substitutions of several aromatic amino acids

Tomohiro Tanaka, Wataru Nomura, Tetsuo Narumi, Ai Esaka, Shinya Oishi, Nami Ohashi, Kyoko Itotani, Barry J. Evans, Zi-xuan Wang, Stephen C. Peiper, Nobutaka Fujii and Hirokazu Tamamura

Org. Biomol. Chem., 2009, 7, 3805
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Forcefield_NCAA: Ab Initio Charge Parameters to Aid in the Discovery and Design of Therapeutic Proteins and Peptides with Unnatural Amino Acids and Their Application to Complement Inhibitors of the Compstatin Family

George A. Khoury, James Smadbeck, Phanourios Tamamis, Andrew C. Vandris, Chris A. Kieslich and Christodoulos A. Floudas

ACS Synth. Biol., 2014, 3, 855
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Discovery of novel, highly potent and selective β-hairpin mimetic CXCR4 inhibitors with excellent anti-HIV activity and pharmacokinetic profiles

Steven J. DeMarco, Heiko Henze, Alexander Lederer, Kerstin Moehle, Reshmi Mukherjee, Barbara Romagnoli, John A. Robinson, Federico Brianza, Frank O. Gombert, Sergio Lociuro, Christian Ludin, Jan Willem Vrijbloed, Jürg Zumbrunn, Jean-Pierre Obrecht, Daniel Obrecht, Vincent Brondani, François Hamy and Thomas Klimkait

Bioorganic & Medicinal Chemistry, 2006, 14, 8396
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Harnessing CXCR4 antagonists in stem cell mobilization, HIV infection, ischemic diseases, and oncology

Lun Kelvin Tsou, Ying‐Huey Huang, Jen‐Shin Song, Yi‐Yu Ke, Jing‐Kai Huang and Kak‐Shan Shia

Medicinal Research Reviews, 2018, 38, 1188
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Therapeutic potential of the chemokine receptor CXCR4 antagonists as multifunctional agents

Hiroshi Tsutsumi, Tomohiro Tanaka, Nami Ohashi, Hiroyuki Masuno, Hirokazu Tamamura, Kenichi Hiramatsu, Takanobu Araki, Satoshi Ueda, Shinya Oishi and Nobutaka Fujii

Biopolymers, 2007, 88, 279
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Improving chemotherapeutic efficiency in acute myeloid leukemia treatments by chemically synthesized peptide interfering with CXCR4/CXCL12 axis

Xiaojin Li, Hua Guo, Hongyang Duan, Yanlian Yang, Jie Meng, Jian Liu, Chen Wang and Haiyan Xu

Sci Rep, 2015, 5
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At the Bench: Pre-clinical evidence for multiple functions of CXCR4 in cancer

Gary D Luker, Jinming Yang, Ann Richmond, Stefania Scala, Claudio Festuccia, Margret Schottelius, Hans-Jürgen Wester and Johann Zimmermann

Journal of Leukocyte Biology, 2021, 109, 969
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Development of a 111In-labeled peptide derivative targeting a chemokine receptor, CXCR4, for imaging tumors

Hirofumi Hanaoka, Takahiro Mukai, Hirokazu Tamamura, Tomohiko Mori, Seigo Ishino, Kazuma Ogawa, Yasuhiko Iida, Ryuichiro Doi, Nobutaka Fujii and Hideo Saji

Nuclear Medicine and Biology, 2006, 33, 489
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Innovations in hematopoietic stem-cell mobilization: a review of the novel CXCR4 inhibitor motixafortide

Zachary D. Crees, Michael P. Rettig and John F. DiPersio

Therapeutic Advances in Hematology, 2023, 14
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Identification of a CXCR4 antagonist, a T140 analog, as an anti‐rheumatoid arthritis agent

Hirokazu Tamamura, Miho Fujisawa, Kenichi Hiramatsu, Makiko Mizumoto, Hideki Nakashima, Naoki Yamamoto, Akira Otaka and Nobutaka Fujii

FEBS Letters, 2004, 569, 99
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Development of Anti-HIV Agents Based on Chemical Biology

Hirokazu Tamamura

YAKUGAKU ZASSHI, 2012, 132, 69
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Novel Compounds Containing Multiple Guanide Groups That Bind the HIV Coreceptor CXCR4

Royce A. Wilkinson, Seth H. Pincus, Joyce B. Shepard, Sarah K. Walton, Edward P. Bergin, Mohamed Labib and Martin Teintze

Antimicrob Agents Chemother, 2011, 55, 255
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CXCR4 antagonists mobilize childhood acute lymphoblastic leukemia cells into the peripheral blood and inhibit engraftment

J Juarez, A Dela Pena, R Baraz, J Hewson, M Khoo, A Cisterne, S Fricker, N Fujii, K F Bradstock and L J Bendall

Leukemia, 2007, 21, 1249
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Hybrid Peptide Dendrimers for Imaging of Chemokine Receptor 4 (CXCR4) Expression

Joeri Kuil, Tessa Buckle, Joppe Oldenburg, Hushan Yuan, Alexander D. Borowsky, Lee Josephson and Fijs W. B. van Leeuwen

Mol. Pharmaceutics, 2011, 8, 2444
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Fmoc‐based solid‐phase synthesis of GPR54‐agonistic pentapeptide derivatives containing alkene‐ and fluoroalkene‐dipeptide isosteres

Kenji Tomita, Tetsuo Narumi, Ayumu Niida, Shinya Oishi, Hiroaki Ohno and Nobutaka Fujii

Biopolymers, 2007, 88, 272
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Synthesis and Application of Fluorescein‐ and Biotin‐Labeled Molecular Probes for the Chemokine Receptor CXCR4

Shinya Oishi, Ryo Masuda, Barry Evans, Satoshi Ueda, Yukiko Goto, Hiroaki Ohno, Akira Hirasawa, Gozoh Tsujimoto, Zixuan Wang, Stephen C. Peiper, Takeshi Naito, Eiichi Kodama, Masao Matsuoka and Nobutaka Fujii

ChemBioChem, 2008, 9, 1154
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Inhibitors of CXCR4 affect the migration and fate of CXCR4+ progenitors in the developing limb of chick embryos

Faisal Yusuf, Rizwan Rehimi, Gabriela Moroşan‐Puopolo, Fangping Dai, Xiaobing Zhang and Beate Brand‐Saberi

Developmental Dynamics, 2006, 235, 3007
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Synthesis and Evaluation of a Bimodal CXCR4 Antagonistic Peptide

Joeri Kuil, Tessa Buckle, Hushan Yuan, Nynke S. van den Berg, Shinya Oishi, Nobutaka Fujii, Lee Josephson and Fijs W. B. van Leeuwen

Bioconjugate Chem., 2011, 22, 859
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HIV-1 entry inhibitors: closing the front door

Brian Tomkowicz and Ronald G Collman

Expert Opinion on Therapeutic Targets, 2004, 8, 65
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Bivalent 14‐mer peptide ligands of CXCR4 with polyproline linkers with anti‐chemotactic activity against Jurkat cells

Tomohiro Tanaka, Toru Aoki, Wataru Nomura and Hirokazu Tamamura

Journal of Peptide Science, 2017, 23, 574
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A single treatment with microcapsules containing a CXCR4 antagonist suppresses pulmonary metastasis of murine melanoma

M Takenaga, H Tamamura, K Hiramatsu, N Nakamura, Y Yamaguchi, A Kitagawa, S Kawai, H Nakashima, N Fujii and R Igarashi

Biochemical and Biophysical Research Communications, 2004, 320, 226
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Stromal cell–derived factor 1/CXCR4 signaling is critical for the recruitment of mesenchymal stem cells to the fracture site during skeletal repair in a mouse model

Toshiyuki Kitaori, Hiromu Ito, Edward M. Schwarz, Ryosuke Tsutsumi, Hiroyuki Yoshitomi, Shinya Oishi, Masakazu Nakano, Nobutaka Fujii, Takashi Nagasawa and Takashi Nakamura

Arthritis & Rheumatism, 2009, 60, 813
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BL-8040, a CXCR4 antagonist, in combination with pembrolizumab and chemotherapy for pancreatic cancer: the COMBAT trial

Bruno Bockorny, Valerya Semenisty, Teresa Macarulla, Erkut Borazanci, Brian M. Wolpin, Salomon M. Stemmer, Talia Golan, Ravit Geva, Mitesh J. Borad, Katrina S. Pedersen, Joon Oh Park, Robert A. Ramirez, David G. Abad, Jaime Feliu, Andres Muñoz, Mariano Ponz-Sarvise, Amnon Peled, Tzipora M. Lustig, Osnat Bohana-Kashtan, Stephen M. Shaw, Ella Sorani, Marya Chaney, Shaul Kadosh, Abi Vainstein Haras, Daniel D. Von Hoff and Manuel Hidalgo

Nat Med, 2020, 26, 878
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Exploratory Studies on Development of the Chemokine Receptor CXCR4 Antagonists toward Downsizing

Hirokazu Tamamura, Hiroshi Tsutsumi, Wataru Nomura and Nobutaka Fujii

Perspect Medicin Chem, 2008, 2
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The Chemokine System in Oncogenic Pathways Driven by Viruses: Perspectives for Cancer Immunotherapy

Géraldine Schlecht-Louf, Claire Deback and Françoise Bachelerie

Cancers, 2022, 14, 848
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Potent Synergistic Anti-Human Immunodeficiency Virus (HIV) Effects Using Combinations of the CCR5 Inhibitor Aplaviroc with Other Anti-HIV Drugs

Hirotomo Nakata, Seth M. Steinberg, Yasuhiro Koh, Kenji Maeda, Yoshikazu Takaoka, Hirokazu Tamamura, Nobutaka Fujii and Hiroaki Mitsuya

Antimicrob Agents Chemother, 2008, 52, 2111
DOI: 10.1128/AAC.01299-07

Design, synthesis and biological evaluation of low molecular weight CXCR4 ligands

Maxwell M. Sakyiamah, Takuya Kobayakawa, Masayuki Fujino, Makoto Konno, Tetsuo Narumi, Tomohiro Tanaka, Wataru Nomura, Naoki Yamamoto, Tsutomu Murakami and Hirokazu Tamamura

Bioorganic & Medicinal Chemistry, 2019, 27, 1130
DOI: 10.1016/j.bmc.2019.02.013

Benzenesulfonamides: A Unique Class of Chemokine Receptor Type 4 Inhibitors

Suazette Reid Mooring, Jin Liu, Zhongxing Liang, Jeffrey Ahn, Samuel Hong, Younghyoun Yoon, James P. Snyder and Hyunsuk Shim

ChemMedChem, 2013, 8, 622
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Development of a NanoBRET-Based Sensitive Screening Method for CXCR4 Ligands

Maxwell M. Sakyiamah, Wataru Nomura, Takuya Kobayakawa and Hirokazu Tamamura

Bioconjugate Chem., 2019, 30, 1442
DOI: 10.1021/acs.bioconjchem.9b00182

Fluorinated PEG-PEI Coated Magnetic Nanoparticles for siRNA Delivery and CXCR4 Knockdown

Yixiang Cao, Shiyin Zhang, Ming Ma and Yu Zhang

Nanomaterials, 2022, 12, 1692
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Motixafortide and G-CSF to mobilize hematopoietic stem cells for autologous transplantation in multiple myeloma: a randomized phase 3 trial

Zachary D. Crees, Michael P. Rettig, Reyka G. Jayasinghe, Keith Stockerl-Goldstein, Sarah M. Larson, Illes Arpad, Giulio A. Milone, Massimo Martino, Patrick Stiff, Douglas Sborov, Denise Pereira, Ivana Micallef, Gemma Moreno-Jiménez, Gabor Mikala, Maria Liz Paciello Coronel, Udo Holtick, John Hiemenz, Muzaffar H. Qazilbash, Nancy Hardy, Tahir Latif, Irene García-Cadenas, Abi Vainstein-Haras, Ella Sorani, Irit Gliko-Kabir, Inbal Goldstein, Debby Ickowicz, Liron Shemesh-Darvish, Shaul Kadosh, Feng Gao, Mark A. Schroeder, Ravi Vij and John F. DiPersio

Nat Med, 2023, 29, 869
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Modulators of CXCR4 and CXCR7/ACKR3 Function

Ilze Adlere, Birgit Caspar, Marta Arimont, Sebastian Dekkers, Kirsten Visser, Jeffrey Stuijt, Chris de Graaf, Michael Stocks, Barrie Kellam, Stephen Briddon, Maikel Wijtmans, Iwan de Esch, Stephen Hill and Rob Leurs

Molecular Pharmacology, 2019, 96, 737
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Comparison of 18F-labeled CXCR4 antagonist peptides for PET imaging of CXCR4 expression

Xiao-Xiang Zhang, Zhongchan Sun, Jinxia Guo, Zhe Wang, Chenxi Wu, Gang Niu, Ying Ma, Dale O. Kiesewetter and Xiaoyuan Chen

Mol Imaging Biol, 2013, 15, 758
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Development of Peptide-targeted Lipoplexes to CXCR4-expressing Rat Glioma Cells and Rat Proliferating Endothelial Cells

Wouter HP Driessen, Nobutaka Fujii, Hirokazu Tamamura and Sean M Sullivan

Molecular Therapy, 2008, 16, 516
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Chemokine receptor CXCR4 as a therapeutic target for neuroectodermal tumors

Hyunsuk Shim, Shinya Oishi and Nobutaka Fujii

Seminars in Cancer Biology, 2009, 19, 123
DOI: 10.1016/j.semcancer.2008.11.004

The successes and failures of HIV drug discovery

Chie Hashimoto, Tomohiro Tanaka, Tetsuo Narumi, Wataru Nomura and Hirokazu Tamamura

Expert Opinion on Drug Discovery, 2011, 6, 1067
DOI: 10.1517/17460441.2011.611129

Understanding Tricky Cellular and Molecular Interactions in Pancreatic Tumor Microenvironment: New Food for Thought

Antonio Agostini, Arturo Orlacchio, Carmine Carbone and Ilaria Guerriero

Front. Immunol., 2022, 13
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Design, synthesis and evaluation of bioactivity of peptidomimetics based on chloroalkene dipeptide isosteres

Takuya Kobayakawa, Kohei Tsuji and Hirokazu Tamamura

Bioorganic & Medicinal Chemistry, 2024, 110, 117811
DOI: 10.1016/j.bmc.2024.117811

Advance of T regulatory cells in tumor microenvironment remodeling and immunotherapy in pancreatic cancer

Zetian Gao, Qiubo Zhang, Xie Zhang and Yufei Song

Eur J Inflamm, 2022, 20
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Improved guanide compounds which bind the CXCR4 co-receptor and inhibit HIV-1 infection

Royce A. Wilkinson, Seth H. Pincus, Kejing Song, Joyce B. Shepard, Alan J. Weaver, Mohamed E. Labib and Martin Teintze

Bioorganic & Medicinal Chemistry Letters, 2013, 23, 2197
DOI: 10.1016/j.bmcl.2013.01.107

A future perspective on the development of chemokine receptor CXCR4 antagonists

Hirokazu Tamamura, Hiroshi Tsutsumi, Wataru Nomura, Tomohiro Tanaka and Nobutaka Fujii

Expert Opinion on Drug Discovery, 2008, 3, 1155
DOI: 10.1517/17460441.3.10.1155

Synthesis and preliminary evaluation of a novel 125I-labeled T140 analog for quantitation of CXCR4 expression

Yanjiang Han, Duanzhi Yin, Mingqiang Zheng, Wei Zhou, ZhenHong Lee, Lan Zhan, Yufei Ma, Mingxing Wu, Lingli Shi, Ni Wang, Jianbo Lee, Cheng Wang, Zheng Lee and Yongxian Wang

J Radioanal Nucl Chem, 2010, 284, 279
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