PMID: 8610113Apr 2, 1996Paper

Batimastat, a potent matrix mealloproteinase inhibitor, exhibits an unexpected mode of binding

Proceedings of the National Academy of Sciences of the United States of America
I BotosE F Meyer

Abstract

Matrix metalloproteinase enzymes have been implicated in degenerative processes like tumor cell invasion, metastasis, and arthritis. Specific metalloproteinase inhibitors have been used to block tumor cell proliferation. We have examined the interaction of batimastat (BB-94) with a metalloproteinase [atrolysin C (Ht-d), EC 3.4.24.42] active site at 2.0-angstroms resolution (R = 16.8%). The title structure exhibits an unexpected binding geometry, with the thiophene ring deeply inserted into the primary specificity site. This unprecedented binding geometry dramatizes the significance of the cavernous primary specificity site, pointing the way for the design of a new generation of potential antitumor drugs.

References

Jun 5, 1991·Journal of the National Cancer Institute·A AlbiniW G Stetler-Stevenson
Mar 1, 1990·Journal of Computer-aided Molecular Design·J J Stewart
Apr 20, 1967·Biochemical and Biophysical Research Communications·I Schechter, A Berger
Aug 1, 1994·International Journal of Cancer. Journal International Du Cancer·R G ChiriviR Giavazzi
Aug 30, 1994·Proceedings of the National Academy of Sciences of the United States of America·D ZhangE F Meyer
Jan 1, 1993·Annual Review of Cell Biology·W G Stetler-StevensonL A Liotta
Aug 1, 1993·Journal of Cellular Physiology·H W SchnaperD L French
Mar 1, 1993·Clinical & Experimental Metastasis·P D BrownA Howell
Oct 1, 1995·Protein Science : a Publication of the Protein Society·J W BeckerJ D Hermes
Nov 20, 2009·Electrophoresis·Dawid R Zalewski, Han J G E Gardeniers

❮ Previous
Next ❯

Citations

Apr 1, 1998·Protein Science : a Publication of the Protein Society·F X Gomis-RüthV Politi
Mar 19, 1999·Protein Science : a Publication of the Protein Society·I L AlbertsS J Wodak
Apr 8, 2009·Cancer Chemotherapy and Pharmacology·Nina Saban, Maro Bujak
Aug 21, 2012·Cell Biochemistry and Biophysics·Liang Xiao, Man Wang
Apr 2, 2011·Neurotherapeutics : the Journal of the American Society for Experimental NeuroTherapeutics·Haoqian ZhangLinda J Noble-Haeusslein
Apr 29, 1999·Toxicon : Official Journal of the International Society on Toxinology·J C Pérez, E E Sánchez
Mar 31, 2000·Pharmacology & Therapeutics·E F MeyerJ A Williams
Apr 13, 2001·Drug Discovery Today·M L. MossR C. Andrews
Jul 11, 2000·Molecular Biology of the Cell·I Yana, S J Weiss
Jun 12, 2012·Acta Crystallographica. Section F, Structural Biology and Crystallization Communications·Troii HallMarc D Zack
Apr 8, 2006·Biomedical Papers of the Medical Faculty of the University Palacký, Olomouc, Czechoslovakia·Jirí KukackaVáclav Pelouch
Jun 22, 2000·Biochemical and Biophysical Research Communications·H Wang, J A Keiser
Aug 12, 2004·The Journal of Investigative Dermatology·Christina SiemesVolker Herzog
Aug 4, 2004·Journal of Molecular Biology·Renaud MoralesMargaret O'Gara
Aug 22, 2000·The Journal of Investigative Dermatology·N Buisson-LegendreW Hornebeck
Nov 22, 2005·Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy·Agnieszka Kaczor, Leonard M Proniewicz
Nov 9, 2005·Bioorganic & Medicinal Chemistry Letters·Jason S XiangSteve Tam
Sep 23, 2003·Protein Science : a Publication of the Protein Society·Leandra WatanabeRaghuvir K Arni
Sep 29, 2011·Cell Biochemistry and Function·Govinda BhattaraiHo-Keun Yi
Nov 13, 1998·Arteriosclerosis, Thrombosis, and Vascular Biology·S BellostaF Bernini
Mar 6, 2012·Chemical Biology & Drug Design·Torsten LingottThomas Steinbrecher
Apr 17, 2020·Nucleic Acids Research·Katrin Schöning-StierandMatthias Rarey
Mar 5, 2010·Journal of Enzyme Inhibition and Medicinal Chemistry·Neeraj SharmaS C Chaudhry
Jan 5, 2002·The Journal of Immunology : Official Journal of the American Association of Immunologists·Andreas LudwigGayle Chapman

❮ Previous
Next ❯

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.