Structural Modifications of Thalidomide Produce Analogs with Enhanced Tumor Necrosis Factor Inhibitory Activity
Abstract
ADVERTISEMENT RETURN TO ISSUEPREVLetterNEXTStructural Modifications of Thalidomide Produce Analogs with Enhanced Tumor Necrosis Factor Inhibitory Activity 1George W. Muller, Laura G. Corral, Mary G. Shire, Hua Wang, Andre Moreira, Gilla Kaplan, and David I. StirlingView Author Information Celgene Corporation, Warren, New Jersey 07059, and Department of Cellular Immunology, The Rockefeller University, New York, New York 10021 Cite this: J. Med. Chem. 1996, 39, 17, 3238–3240Publication Date (Web):August 16, 1996Publication History Received3 May 1996Published online16 August 1996Published inissue 1 January 1996https://doi.org/10.1021/jm9603328Copyright © 1996 American Chemical SocietyRIGHTS & PERMISSIONSArticle Views2642Altmetric-Citations123LEARN ABOUT THESE METRICSArticle Views are the COUNTER-compliant sum of full text article downloads since November 2008 (both PDF and HTML) across all institutions and individuals. These metrics are regularly updated to reflect usage leading up to the last few days.Citations are the number of other articles citing this article, calculated by Crossref and updated daily. Find more information about Crossref citation counts.The Altmetric Attention Score is a quantitative measure of the attention that a research article has received online. Clicking on the donut icon will load a page at altmetric.com with additional details about the score and the social media presence for the given article. Find more information on the Altmetric Attention Score and how the score is calculated. Share Add toView InAdd Full Text with ReferenceAdd Description ExportRISCitationCitation and abstractCitation and referencesMore Options Share onFacebookTwitterWechatLinked InReddit Read OnlinePDF (134 KB) Get e-AlertsSUBJECTS:Amides,Hydrolysis,Inhibition,Molecular structure,Reaction products Get e-Alerts
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Thalidomide, lenalidomide and pomalidomide are currently FDA approved in a variety of clinical settings, including MM, NHL, MDS and Kaposi sarcoma.
“Thalidomide, lenalidomide and pomalidomide are currently FDA approved in a variety of clinical settings, including MM, NHL and MDS as well as Kaposi sarcoma (KS)19–22.”
From Cancer therapies based on targeted protein degradation — lessons learned with lenalidomide (2021) · cites this paper as [22]
Despite clear effects on immune cell function and clinical activity against erythema nodosum leprosum and Kaposi sarcoma, no strong data support a primarily immunomodulatory mechanism of antitumour action of thalidomide analogues.
“Thus, despite clear effects on immune cell function and clinical activity against erythema nodosum leprosum and KS22, no strong data support a primarily immunomodulatory mechanism of antitumour action of thalidomide analogues.”
From Cancer therapies based on targeted protein degradation — lessons learned with lenalidomide (2021) · cites this paper as [22]
In 2020, pomalidomide was approved by the FDA for the treatment of Kaposi sarcoma, an endothelial cell-derived solid tumour caused by human herpesvirus 8 infection, based on data from a phase I/II trial that demonstrated an ORR of 73% in patients with newly diagnosed Kaposi sarcoma.
“In 2020, pomalidomide was approved by the FDA for the treatment of KS, an endothelial cell-derived solid tumour caused by human herpesvirus 8 (HHV8) infection110, based on data from a phase I/II trial that demonstrated an ORR of 73% in patients with newly diagnosed KS22.”
From Cancer therapies based on targeted protein degradation — lessons learned with lenalidomide (2021) · cites this paper as [22]
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Zhu, Y. X., Kortuem, K. M., & Stewart, A. K. (2013) · Leukemia & Lymphoma · doi:10.3109/10428194.2012.728597 · Cited by 293 · see citing works
Cancer therapies based on targeted protein degradation — lessons learned with lenalidomide
Jan, M., Sperling, A. S., & Ebert, B. L. (2021) · Nature Reviews Clinical Oncology · doi:10.1038/s41571-021-00479-z · Cited by 137 · see citing works
- Authors
- Muller, G. W., Corral, L. G., Shire, M. G., Wang, H., Moreira, A., Kaplan, G., & Stirling, D. I.
- Affiliations
- Rockefeller University (US)
- ORCID
- Wang, Hua
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 1996-01-01
- Volume
- 39
- Issue
- 17
- Pages
- 3238-3240
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W2129539691
- Cited by
- 158
- References
- 14
- Citations by year
- 2025: 2 · 2024: 1 · 2023: 3 · 2022: 2 · 2021: 5 · 2020: 5 · 2019: 6 · 2018: 6 · 2017: 10 · 2016: 7 · 2015: 6 · 2014: 4 · 2013: 8 · 2012: 7
- FWCI
- 6.58
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Journal of Medicinal Chemistry (publishedVersion)
- PubMed (publishedVersion)
- Funders
- National Institutes of Health (5r01ai033124-04)
- National Institute of Allergy and Infectious Diseases (AI 33124)
- Topics
- Physical Sciences › Chemistry › Organic Chemistry › Synthesis and biological activity
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Chemical Synthesis and Analysis
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Protein Degradation and Inhibitors
- Keywords
- thalidomide analogues, tumor necrosis factor inhibition, structural modification, TNF-alpha inhibitors, amide hydrolysis
- MeSH terms
- Humans, Kinetics, Lipopolysaccharides, Lymphocytes, Phthalimides, Pyrimidinones, Structure-Activity Relationship, Thalidomide, Tumor Necrosis Factor-alpha, Molecular Structure
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