Results 161 to 170 of about 8,600 (184)

A molecular modeling analysis of novel non-hydroxamate inhibitors of TACE

Bioorganic & Medicinal Chemistry Letters, 2007
Recently, an X-ray co-crystal structure of our hydroxamate inhibitor IK682 and TACE [Niu, X.; Umland, S.; Ingram, R.; Beyer, B. M.; Liu, Y.-H.; Sun, J.; Lundell, D.; Orth, P. Arch. Biochem. Biophys. 2006, 451, 43-50] was published that explicitly shows the orientation of the hydroxamate and the TACE-selective 4-[(2-methyl-4-quinolinyl)methoxy]phenyl P1'
James E, Sheppeck, Andrew, Tebben, John L, Gilmore, Anle, Yang, Zelda R, Wasserman, Carl P, Decicco, James J-W, Duan   +6 more
openaire   +2 more sources

Discovery of low nanomolar non-hydroxamate inhibitors of tumor necrosis factor-α converting enzyme (TACE)

Bioorganic & Medicinal Chemistry Letters, 2007
Using a pyrimidine-2,4,6-trione motif as a zinc-binding group, a series of selective inhibitors of tumor necrosis factor-alpha converting enzyme (TACE) was discovered. Optimization of initial lead 1 resulted in a potent inhibitor (51), with an IC(50) of 2 nM in a porcine TACE assay.
James J-W, Duan, Lihua, Chen, Zhonghui, Lu, Bin, Jiang, Naoyuki, Asakawa, James E, Sheppeck, Rui-Qin, Liu, Maryanne B, Covington, William, Pitts, Soong-Hoon, Kim, Carl P, Decicco   +10 more
openaire   +3 more sources

Water molecule-mediated selective inhibition of bacterial zinc metalloproteinases by non-hydroxamate compounds: Ab initio molecular simulations

Journal of Molecular Graphics and Modelling, 2022
UDP-3-O-acyl-N acetylglucosamine deacetylase (LpxC), Zn metalloenzyme for Gram-negative bacteria is an attractive target for developing novel therapeutic agents. Since LpxC has the similar binding pocket as the human matrix metalloproteinases (MMPs), LpxC inhibitors might also inhibit MMP functions producing side effects in human bodies.
Ryosuke Saito, Kyohei Imai, Daichi Takimoto, Takuya Ezawa, Satoshi Sugiyama, Midori Takimoto-Kamimura, Noriyuki Kurita   +6 more
openaire   +2 more sources

Synthesis of Novel Hydroxamate and Non‐Hydroxamate Histone Deacetylase Inhibitors

ChemInform, 2005
AbstractFor Abstract see ChemInform Abstract in Full Text.
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Identification of a potent non-hydroxamate histone deacetylase inhibitor by mechanism-based drug design

Bioorganic & Medicinal Chemistry Letters, 2005
In order to find novel non-hydroxamate histone deacetylase (HDAC) inhibitors, we synthesized several suberoylanilide hydroxamic acid (SAHA)-based compounds designed on the basis of the catalytic mechanism of HDACs. Among these compounds, 5b was found to be as potent as SAHA.
Takayoshi, Suzuki, Azusa, Matsuura, Akiyasu, Kouketsu, Hidehiko, Nakagawa, Naoki, Miyata   +4 more
openaire   +2 more sources

Novel benzimidazole‐linked (thio)barbiturates as non‐hydroxamate HDAC6 inhibitors targeting leukemia: Design, synthesis, and structure–activity relationship

Archiv der Pharmazie, 2023
AbstractBased on the well‐established pharmacophoric features required for histone deacetylase (HDAC) inhibition, novel easy‐to‐prepare benzimidazole‐linked (thio)barbiturate derivatives were designed and synthesized as HDAC6 inhibitors. The proposed structures of the title compounds were confirmed based on their spectral data and elemental analyses ...
Reda El‐Sayed Mansour, Hanan Gaber Abdulwahab, Hend M. El‐Sehrawi   +2 more
openaire   +2 more sources

Targeted Polypharmacology: Discovery of a Highly Potent Non-Hydroxamate Dual Matrix Metalloproteinase (MMP)-10/-13 Inhibitor

Journal of Medicinal Chemistry, 2017
Matrix metalloproteinases (MMPs) play a key role in many diseases like cancer, atherosclerosis or arthritis. Interest in MMP inhibition has been revitalized very recently as the knowledge on the underlying network of biological pathways is steadily growing.
Nicole Senn, Michael Ott, Jan Lanz, Rainer Riedl   +3 more
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Non-hydroxamate inhibitors of 1-deoxy-d-xylulose 5-phosphate reductoisomerase (DXR): A critical review and future perspective

European Journal of Medicinal Chemistry, 2021
1-deoxy-d-xylulose 5-phosphate reductoisomerase (DXR) catalyzes the second step of the non-mevalonate (or MEP) pathway that functions in several organisms and plants for the synthesis of isoprenoids. DXR is essential for the survival of multiple pathogenic bacteria/parasites, including those that cause tuberculosis and malaria in humans.
Sharyu Kesharwani, Sandeep Sundriyal
openaire   +2 more sources

Novel Histone Deacetylase Inhibitors: Design, Synthesis, Enzyme Inhibition, and Binding Mode Study of SAHA‐Based Non‐Hydroxamates.

ChemInform, 2003
AbstractFor Abstract see ChemInform Abstract in Full Text.
Takayoshi, Suzuki, Yuki, Nagano, Azusa, Matsuura, Arihiro, Kohara, Shin-ichi, Ninomiya, Kohfuku, Kohda, Naoki, Miyata   +6 more
openaire   +2 more sources

Discovery of novel hydantoins as selective non-hydroxamate inhibitors of tumor necrosis factor-α converting enzyme (TACE)

Bioorganic & Medicinal Chemistry Letters, 2007
AbstractChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.
James E, Sheppeck, John L, Gilmore, Anle, Yang, Xiao-Tao, Chen, Chu-Biao, Xue, John, Roderick, Rui-Qin, Liu, Maryanne B, Covington, Carl P, Decicco, James J-W, Duan   +9 more
openaire   +2 more sources