464
Views
49
CrossRef citations to date
0
Altmetric
Reviews

Phospholipase A2 inhibitors for the treatment of inflammatory diseases: a patent review (2010 – present)

, PhD & , PhD
Pages 333-344 | Published online: 08 Jan 2013

Keep up to date with the latest research on this topic with citation updates for this article.

Read on this site (5)

J. Abhithaj, K. G. Arun, C. S. Sharanya, M. Haridas & E. Jayadevi Variyar. (2019) Isozymes inhibited by active site blocking: versatility of calcium indifferent hesperidin binding to phospholipase A2 and its significance. Journal of Receptors and Signal Transduction 39:1, pages 60-66.
Read now
Maroula G. Kokotou, Dimitris Limnios, Aikaterini Nikolaou, Anastasia Psarra & George Kokotos. (2017) Inhibitors of phospholipase A2 and their therapeutic potential: an update on patents (2012-2016). Expert Opinion on Therapeutic Patents 27:2, pages 217-225.
Read now
Sabine Grösch, Ellen Niederberger & Gerd Geisslinger. (2017) Investigational drugs targeting the prostaglandin E2 signaling pathway for the treatment of inflammatory pain. Expert Opinion on Investigational Drugs 26:1, pages 51-61.
Read now
Jan Althaus, Theresa Hake, Walburga Hanekamp & Matthias Lehr. (2016) 1-(5-Carboxyindazol-1-yl)propan-2-ones as dual inhibitors of cytosolic phospholipase A2α and fatty acid amide hydrolase: bioisosteric replacement of the carboxylic acid moiety. Journal of Enzyme Inhibition and Medicinal Chemistry 31:sup1, pages 131-140.
Read now

Articles from other publishers (44)

Eunsook Jeon, Kyungkook Kim, Hyunjeong Park & Keuntae Cho. (2023) Global Collaboration in Technology Sectors during the COVID-19 Pandemic: A Patent Review. Sustainability 15:15, pages 11831.
Crossref
Andreja Leskovac. 2023. Phospholipases in Physiology and Pathology. Phospholipases in Physiology and Pathology 67 77 .
Manikkam Rajalakshmi, Sabapathy Indu & Periyasamy Vijayalakshmi. 2023. Phospholipases in Physiology and Pathology. Phospholipases in Physiology and Pathology 3 13 .
Nur Mahammad, Felicity J. Ashcroft, Astrid J. Feuerherm, Samah Elsaadi, Esten N. Vandsemb, Magne Børset & Berit Johansen. (2021) Inhibition of Cytosolic Phospholipase A2α Induces Apoptosis in Multiple Myeloma Cells. Molecules 26:24, pages 7447.
Crossref
Eirini Tsirvouli, Felicity Ashcroft, Berit Johansen & Martin Kuiper. (2021) Logical and experimental modeling of cytokine and eicosanoid signaling in psoriatic keratinocytes. iScience 24:12, pages 103451.
Crossref
José María Gutiérrez, Laura-Oana Albulescu, Rachel H. Clare, Nicholas R. Casewell, Tarek Mohamed Abd El-Aziz, Teresa Escalante & Alexandra Rucavado. (2021) The Search for Natural and Synthetic Inhibitors That Would Complement Antivenoms as Therapeutics for Snakebite Envenoming. Toxins 13:7, pages 451.
Crossref
Ming Cai, Wei-Jian Ni, Lan Han, Wei-Dong Chen & Dai-Yin Peng. (2021) Research Progress of Therapeutic Enzymes and Their Derivatives: Based on Herbal Medicinal Products in Rheumatoid Arthritis. Frontiers in Pharmacology 12.
Crossref
Qiangzhe Zhang, Ronnie H. Fang, Weiwei Gao & Liangfang Zhang. (2020) A Biomimetic Nanoparticle to “Lure and Kill” Phospholipase A2. Angewandte Chemie International Edition 59:26, pages 10461-10465.
Crossref
Qiangzhe Zhang, Ronnie H. Fang, Weiwei Gao & Liangfang Zhang. (2020) A Biomimetic Nanoparticle to “Lure and Kill” Phospholipase A2. Angewandte Chemie 132:26, pages 10547-10551.
Crossref
A. J. Feuerherm, E. A. Dennis & B. Johansen. (2019) Cytosolic group IVA phospholipase A2 inhibitors, AVX001 and AVX002, ameliorate collagen-induced arthritis. Arthritis Research & Therapy 21:1.
Crossref
Christina Dedaki, Maroula G. Kokotou, Varnavas D. Mouchlis, Dimitris Limnios, Xiaoyong Lei, Carol T. Mu, Sasanka Ramanadham, Victoria Magrioti, Edward A. Dennis & George Kokotos. (2019) β-Lactones: A Novel Class of Ca 2+ -Independent Phospholipase A 2 (Group VIA iPLA 2 ) Inhibitors with the Ability To Inhibit β-Cell Apoptosis . Journal of Medicinal Chemistry 62:6, pages 2916-2927.
Crossref
Octavio A. Gonzalez, Vanessa Euzebio-Alves, Yelena Alimova, Ahmad Al-Attar & J. L. Ebersole. 2019. Oral Mucosal Immunity and Microbiome. Oral Mucosal Immunity and Microbiome 79 95 .
Wanyeon Kim, Beomseok Son, Sungmin Lee, Hyunhee Do & BuHyun Youn. (2018) Targeting the enzymes involved in arachidonic acid metabolism to improve radiotherapy. Cancer and Metastasis Reviews 37:2-3, pages 213-225.
Crossref
Tommaso C. Bulfone, Stephen P. Samuel, Philip E. Bickler & Matthew R. Lewin. (2018) Developing Small Molecule Therapeutics for the Initial and Adjunctive Treatment of Snakebite. Journal of Tropical Medicine 2018, pages 1-10.
Crossref
Xiaobin Ren, Mingzhu Zhang, Lingxiang Chen, Wanli Zhang, Yu Huang, Huazhen Luo, Ling Li & Hongbing He. (2017) The anti-inflammatory effects of Yunnan Baiyao are involved in regulation of the phospholipase A2/arachidonic acid metabolites pathways in acute inflammation rat model. Molecular Medicine Reports 16:4, pages 4045-4053.
Crossref
Maroula G. Kokotou, Gerasimia Galiatsatou, Victoria Magrioti, Giorgos Koutoulogenis, Efrosini Barbayianni, Dimitris Limnios, Varnavas D. Mouchlis, Banita Satpathy, Aaron Navratil, Edward A. Dennis & George Kokotos. (2017) 2-Oxoesters: A Novel Class of Potent and Selective Inhibitors of Cytosolic Group IVA Phospholipase A2. Scientific Reports 7:1.
Crossref
S.H. Omland, A. Habicht, P. Damsbo, J. Wilms, B. Johansen & R. Gniadecki. (2017) A randomized, double-blind, placebo-controlled, dose-escalation first-in-man study (phase 0) to assess the safety and efficacy of topical cytosolic phospholipase A2 inhibitor, AVX001, in patients with mild to moderate plaque psoriasis. Journal of the European Academy of Dermatology and Venereology 31:7, pages 1161-1167.
Crossref
Anneta Smyrniotou, Maroula G. Kokotou, Varnavas D. Mouchlis, Efrosini Barbayianni, George Kokotos, Edward A. Dennis & Violetta Constantinou-Kokotou. (2017) 2-Oxoamides based on dipeptides as selective calcium-independent phospholipase A 2 inhibitors. Bioorganic & Medicinal Chemistry 25:3, pages 926-940.
Crossref
Martina Arnsmann, Walburga Hanekamp, Alwine Schulze Elfringhoff & Matthias Lehr. (2017) Structure–activity relationship studies on 1-(2-oxopropyl)indole-5-carboxylic acids acting as inhibitors of cytosolic phospholipase A2α: Effect of substituents at the indole 3-position on activity, solubility, and metabolic stability. European Journal of Medicinal Chemistry 125, pages 1107-1114.
Crossref
Syed Nasir Abbas Bukhari, Gianluigi Lauro, Ibrahim Jantan, Chin Fei Chee, Muhammad Wahab Amjad, Giuseppe Bifulco, Hassan Sher, Iskandar Abdullah & Noorsaadah Abd Rahman. (2016) Anti-inflammatory trends of new benzimidazole derivatives. Future Medicinal Chemistry 8:16, pages 1953-1967.
Crossref
Georgia Antonopoulou, Victoria Magrioti, Maroula G. Kokotou, Aikaterini Nikolaou, Efrosini Barbayianni, Varnavas D. Mouchlis, Edward A. Dennis & George Kokotos. (2016) 2-Oxoamide inhibitors of cytosolic group IVA phospholipase A2 with reduced lipophilicity. Bioorganic & Medicinal Chemistry 24:19, pages 4544-4554.
Crossref
Sofia Vasilakaki, Efrosini Barbayianni, Victoria Magrioti, Oleksandr Pastukhov, Violetta Constantinou-Kokotou, Andrea Huwiler & George Kokotos. (2016) Inhibitors of secreted phospholipase A 2 suppress the release of PGE 2 in renal mesangial cells. Bioorganic & Medicinal Chemistry 24:13, pages 3029-3034.
Crossref
Varnavas D. Mouchlis, Dimitris Limnios, Maroula G. Kokotou, Efrosini Barbayianni, George Kokotos, J. Andrew McCammon & Edward A. Dennis. (2016) Development of Potent and Selective Inhibitors for Group VIA Calcium-Independent Phospholipase A 2 Guided by Molecular Dynamics and Structure–Activity Relationships . Journal of Medicinal Chemistry 59:9, pages 4403-4414.
Crossref
Sofia Vasilakaki, Efrosini Barbayianni, Georgios Leonis, Manthos G. Papadopoulos, Thomas Mavromoustakos, Michael H. Gelb & George Kokotos. (2016) Development of a potent 2-oxoamide inhibitor of secreted phospholipase A2 guided by molecular docking calculations and molecular dynamics simulations. Bioorganic & Medicinal Chemistry 24:8, pages 1683-1695.
Crossref
Xinde Chen, Kai Wang, Wenwei Xu, Quanxin Ma, Minli Chen, Lili Du, Mingguang Mo, Yiping Wang & Jianhua Shen. (2016) Discovery of Potent and Orally Active Lipoprotein-Associated Phospholipase A 2 (Lp-PLA 2 ) Inhibitors as a Potential Therapy for Diabetic Macular Edema . Journal of Medicinal Chemistry 59:6, pages 2674-2687.
Crossref
BHADRAPURA LAKKAPPA DHANANJAYA & SUDHARSHAN SHIVALINGAIAH. (2016) The anti-inflammatory activity of standard aqueous stem bark extract of Mangifera indica L. as evident in inhibition of Group IA sPLA2. Anais da Academia Brasileira de Ciências 88:1, pages 197-209.
Crossref
Xinde Chen, Wenwei Xu, Kai Wang, Mingguang Mo, Wei Zhang, Lili Du, Xiaojing Yuan, Yechun Xu, Yiping Wang & Jianhua Shen. (2015) Discovery of a Novel Series of Imidazo[1,2- a ]pyrimidine Derivatives as Potent and Orally Bioavailable Lipoprotein-Associated Phospholipase A 2 Inhibitors . Journal of Medicinal Chemistry 58:21, pages 8529-8541.
Crossref
R. HAMPL, M. BIČÍKOVÁ & L. SOSVOROVÁ. (2015) How Hormones Influence Composition and Physiological Function of the Brain-Blood Barrier. Physiological Research, pages S259-S264.
Crossref
Chunfeng Xie, Xiaoting Li, Jieshu Wu, Zhaofeng Liang, Feifei Deng, Wei Xie, Mingming Zhu, Jianyun Zhu, Weiwei Zhu, Shanshan Geng & Caiyun Zhong. (2015) Anti-inflammatory Activity of Magnesium Isoglycyrrhizinate Through Inhibition of Phospholipase A2/Arachidonic Acid Pathway. Inflammation 38:4, pages 1639-1648.
Crossref
Wei-Yi Ong, Tahira Farooqui, George Kokotos & Akhlaq A. Farooqui. (2015) Synthetic and Natural Inhibitors of Phospholipases A 2 : Their Importance for Understanding and Treatment of Neurological Disorders . ACS Chemical Neuroscience 6:6, pages 814-831.
Crossref
Tom Sundermann, Jörg Fabian, Walburga Hanekamp & Matthias Lehr. (2015) 1-Heteroaryl-3-phenoxypropan-2-ones as inhibitors of cytosolic phospholipase A2α and fatty acid amide hydrolase: Effect of the replacement of the ether oxygen with sulfur and nitrogen moieties on enzyme inhibition and metabolic stability. Bioorganic & Medicinal Chemistry 23:10, pages 2579-2592.
Crossref
Arjun Ram, Ulaganathan Mabalirajan, Ashish Jaiswal, Rakhshinda Rehman, Vijay Pal Singh & Balaram Ghosh. (2015) Parabromophenacyl Bromide Inhibits Subepithelial Fibrosis by Reducing TGF-β<sub>1</sub> in a Chronic Mouse Model of Allergic Asthma. International Archives of Allergy and Immunology 167:2, pages 110-118.
Crossref
Julian Schwarzkopf, Tom Sundermann, Martina Arnsmann, Walburga Hanekamp, Jörg Fabian, Jan Heidemann, Anna Friederike Pott, Dominik Bettenworth & Matthias Lehr. (2014) Inhibitors of cytosolic phospholipase A2α with carbamate structure: synthesis, biological activity, metabolic stability, and bioavailability. Medicinal Chemistry Research 23:12, pages 5250-5262.
Crossref
George Kokotos, Astrid J. Feuerherm, Efrosini Barbayianni, Ishita Shah, Mari Sæther, Victoria Magrioti, Thuy Nguyen, Violetta Constantinou-Kokotou, Edward A. Dennis & Berit Johansen. (2014) Inhibition of Group IVA Cytosolic Phospholipase A 2 by Thiazolyl Ketones in Vitro, ex Vivo, and in Vivo . Journal of Medicinal Chemistry 57:18, pages 7523-7535.
Crossref
Toshiyuki Tomoo, Takashi Nakatsuka, Toyoko Katayama, Yasuhiro Hayashi, Yusuke Fujieda, Maki Terakawa & Kazuhiro Nagahira. (2014) Design, Synthesis, and Biological Evaluation of 3-(1-Aryl-1 H -indol-5-yl)propanoic Acids as New Indole-Based Cytosolic Phospholipase A 2 α Inhibitors . Journal of Medicinal Chemistry 57:17, pages 7244-7262.
Crossref
Sarah Natalie Cirilo Gimenes, Francis Barbosa Ferreira, Ana Carolina Portella Silveira, Renata Santos Rodrigues, Kelly Aparecida Geraldo Yoneyama, Juliana Izabel dos Santos, Marcos Roberto de Mattos Fontes, Vera Lúcia de Campos Brites, André Luiz Quagliatto Santos, Márcia Helena Borges, Daiana Silva Lopes & Veridiana M. Rodrigues. (2014) Isolation and biochemical characterization of a γ-type phospholipase A2 inhibitor from Crotalus durissus collilineatus snake serum. Toxicon 81, pages 58-66.
Crossref
Dan Yang, Hong-Fei Ji, Xue-Mei Zhang, Hui Yue, Lin Lin, Yu-Yan Ma, Xiang-nan Huang, Jin Fu & Wei-Zhi Wang. (2014) Protective Effect of Cytosolic Phospholipase A2 Inhibition against Inflammation and Degeneration by Promoting Regulatory T Cells in Rats with Experimental Autoimmune Encephalomyelitis. Mediators of Inflammation 2014, pages 1-7.
Crossref
Tom Sundermann, Martina Arnsmann, Julian Schwarzkopf, Walburga Hanekamp & Matthias Lehr. (2014) Convergent and enantioselective syntheses of cytosolic phospholipase A 2 α inhibiting N -(1-indazol-1-ylpropan-2-yl)carbamates . Org. Biomol. Chem. 12:23, pages 4021-4030.
Crossref
Anja Pucer, Vesna Brglez, Christine Payré, Jože Pungerčar, Gérard Lambeau & Toni Petan. (2013) Group X secreted phospholipase A2 induces lipid droplet formation and prolongs breast cancer cell survival. Molecular Cancer 12:1.
Crossref
Jörg Fabian, Walburga Hanekamp, Mélanie H. Thomas, Jean Luc Olivier & Matthias Lehr. (2013) Investigations on the metabolic stability of cytosolic phospholipase A2α inhibitors with 1-indolylpropan-2-one structure. Chemico-Biological Interactions 206:2, pages 356-363.
Crossref
Jung Eun Lee, Soo-Muk Cho, Jin Kim & Jung-Hyun Kim. (2013) Effects Unripe and Ripe Rubus coreanus Miquel on Peritoneal Macrophage Gene Expression Using cDNA Microarray Analysis. Journal of the Korean Society of Food Science and Nutrition 42:10, pages 1552-1559.
Crossref
Victoria Magrioti, Aikaterini Nikolaou, Annetta Smyrniotou, Ishita Shah, Violetta Constantinou-Kokotou, Edward A. Dennis & George Kokotos. (2013) New potent and selective polyfluoroalkyl ketone inhibitors of GVIA calcium-independent phospholipase A2. Bioorganic & Medicinal Chemistry 21:18, pages 5823-5829.
Crossref
Xing Gao, Haojun Gong, Peng Men, Lu Zhou & Deyong Ye. (2013) Design, Synthesis, and Biological Evaluation of Novel Dual Inhibitors of Secretory Phospholipase A2 and Sphingomyelin Synthase. Chinese Journal of Chemistry 31:9, pages 1164-1170.
Crossref
Tomader Ali, George Kokotos, Victoria Magrioti, Robert N. Bone, James A. Mobley, William Hancock & Sasanka Ramanadham. (2013) Characterization of FKGK18 as Inhibitor of Group VIA Ca2+-Independent Phospholipase A2 (iPLA2β): Candidate Drug for Preventing Beta-Cell Apoptosis and Diabetes. PLoS ONE 8:8, pages e71748.
Crossref

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.