The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
28274635 |
381 |
Identification of novel TACE inhibitors compatible with topical application. |
Nestl� |
28151653 |
35 |
Full Sequence Amino Acid Scanning of¿-Defensin RTD-1 Yields a Potent Anthrax Lethal Factor Protease Inhibitor. |
State University of New York |
27966948 |
86 |
Discovery of Novel, Highly Potent, and Selective Matrix Metalloproteinase (MMP)-13 Inhibitors with a 1,2,4-Triazol-3-yl Moiety as a Zinc Binding Group Using a Structure-Based Design Approach. |
Pharmaceutical |
27825552 |
152 |
Design, synthesis, and biological activity of novel, potent, and highly selective fused pyrimidine-2-carboxamide-4-one-based matrix metalloproteinase (MMP)-13 zinc-binding inhibitors. |
Takeda Pharmaceutical |
26871660 |
68 |
Discovery of a new selective inhibitor of A Disintegrin And Metalloprotease 10 (ADAM-10) able to reduce the shedding of NKG2D ligands in Hodgkin's lymphoma cell models. |
San Raffaele Scientific Institute |
26653735 |
81 |
Discovery of N-(4-Fluoro-3-methoxybenzyl)-6-(2-(((2S,5R)-5-(hydroxymethyl)-1,4-dioxan-2-yl)methyl)-2H-tetrazol-5-yl)-2-methylpyrimidine-4-carboxamide. A Highly Selective and Orally Bioavailable Matrix Metalloproteinase-13 Inhibitor for the Potential Treatment of Osteoarthritis. |
Pfizer |
26753813 |
22 |
Design and synthesis of an activity-based protein profiling probe derived from cinnamic hydroxamic acid. |
University of Minnesota |
26638045 |
58 |
Synthesis, experimental evaluation and molecular modelling of hydroxamate derivatives as zinc metalloproteinase inhibitors. |
Uit The Arctic University of Norway |
26288689 |
37 |
Discovery of Potent and Selective Inhibitors for ADAMTS-4 through DNA-Encoded Library Technology (ELT). |
Glaxosmithkline |
26192023 |
71 |
SAR Studies of Exosite-Binding Substrate-Selective Inhibitors of A Disintegrin And Metalloprotease 17 (ADAM17) and Application as Selective in Vitro Probes. |
Florida Atlantic University |
25264600 |
64 |
Discovery of novel, highly potent, and selective quinazoline-2-carboxamide-based matrix metalloproteinase (MMP)-13 inhibitors without a zinc binding group using a structure-based design approach. |
Takeda Pharmaceutical |
25415648 |
63 |
Identification of potent and selective hydantoin inhibitors of aggrecanase-1 and aggrecanase-2 that are efficacious in both chemical and surgical models of osteoarthritis. |
Eli Lilly |
25192810 |
66 |
Thieno[2,3-d]pyrimidine-2-carboxamides bearing a carboxybenzene group at 5-position: highly potent, selective, and orally available MMP-13 inhibitors interacting with the S1¿ binding site. |
Takeda Pharmaceutical |
24735644 |
19 |
Imidazole-derived 2-[N-carbamoylmethyl-alkylamino]acetic acids, substrate-dependent modulators of insulin-degrading enzyme in amyloid-ß hydrolysis. |
University of Lille |
24316668 |
34 |
Discovery of a benzimidazole series of ADAMTS-5 (aggrecanase-2) inhibitors by scaffold hopping. |
Asahi Kasei Pharma |
24044937 |
59 |
Aggrecanase-2 inhibitors based on the acylthiosemicarbazide zinc-binding group. |
University of Lille |
24044434 |
71 |
Selective arylsulfonamide inhibitors of ADAM-17: hit optimization and activity in ovarian cancer cell models. |
UniversitÀ |
23453070 |
42 |
A series of thiazole derivatives bearing thiazolidin-4-one as non-competitive ADAMTS-5 (aggrecanase-2) inhibitors. |
Asahi Kasei Pharma |
22891645 |
83 |
Discovery of highly potent and selective small molecule ADAMTS-5 inhibitors that inhibit human cartilage degradation via encoded library technology (ELT). |
Glaxosmithkline |
22175799 |
22 |
Discovery and evaluation of a non-Zn chelating, selective matrix metalloproteinase 13 (MMP-13) inhibitor for potential intra-articular treatment of osteoarthritis. |
Alantos Pharmaceuticals |
19715320 |
87 |
Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation. |
University of Florida |
19095454 |
63 |
Current perspective of TACE inhibitors: a review. |
The M. S. University of Baroda |
18257543 |
16 |
Carbamoylphosphonate matrix metalloproteinase inhibitors 6: cis-2-aminocyclohexylcarbamoylphosphonic acid, a novel orally active antimetastatic matrix metalloproteinase-2 selective inhibitor--synthesis and pharmacodynamic and pharmacokinetic analysis. |
The Hebrew University of Jerusalem |
12773042 |
195 |
Synthesis and structure-activity relationship of N-substituted 4-arylsulfonylpiperidine-4-hydroxamic acids as novel, orally active matrix metalloproteinase inhibitors for the treatment of osteoarthritis. |
Wyeth Research |
12773041 |
119 |
Synthesis and structure-activity relationship of alpha-sulfonylhydroxamic acids as novel, orally active matrix metalloproteinase inhibitors for the treatment of osteoarthritis. |
Wyeth Research |
11831904 |
172 |
New type of metalloproteinase inhibitor: design and synthesis of new phosphonamide-based hydroxamic acids. |
Nippon Organon K.K. |
11472217 |
157 |
Design, synthesis, and structure-activity relationships of macrocyclic hydroxamic acids that inhibit tumor necrosis factor alpha release in vitro and in vivo. |
Dupont Pharmaceuticals |
10669559 |
180 |
Protease inhibitors: current status and future prospects. |
University of Queensland |
11677139 |
92 |
The discovery of anthranilic acid-based MMP inhibitors. Part 3: incorporation of basic amines. |
Wyeth-Ayerst Research |
11206468 |
24 |
Heteroaryl and cycloalkyl sulfonamide hydroxamic acid inhibitors of matrix metalloproteinases. |
Wyeth-Ayerst Research |
11206467 |
44 |
The discovery of anthranilic acid-based MMP inhibitors. Part 1: SAR of the 3-position. |
Wyeth-Ayerst Research |
11514167 |
88 |
The discovery of anthranilic acid-based MMP inhibitors. Part 2: SAR of the 5-position and P1(1) groups. |
Wyeth-Ayerst Research |
22175825 |
19 |
Potent inhibitors of LpxC for the treatment of Gram-negative infections. |
Pfizer |
22017477 |
35 |
Novel 1-hydroxypiperazine-2,6-diones as new leads in the inhibition of metalloproteinases. |
Instituto Superior T£Cnico |
21963348 |
7 |
Synthesis, preliminary biological evaluation and molecular modeling of some new heterocyclic inhibitors of TACE. |
Sun Pharma Advanced Research |
20638281 |
56 |
Structure and activity relationships of tartrate-based TACE inhibitors. |
Merck Research Laboratories |
21458257 |
87 |
2-(2-Aminothiazol-4-yl)pyrrolidine-based tartrate diamides as potent, selective and orally bioavailable TACE inhibitors. |
Merck Research Laboratories |
21417219 |
179 |
Discovery of (1S,2R,3R)-2,3-dimethyl-2-phenyl-1-sulfamidocyclopropanecarboxylates: novel and highly selective aggrecanase inhibitors. |
Central Pharmaceutical Research Institute |
21300546 |
129 |
The design and synthesis of novel N-hydroxyformamide inhibitors of ADAM-TS4 for the treatment of osteoarthritis. |
Astrazeneca |
21078557 |
34 |
Structure based optimization of chromen-based TNF-a converting enzyme (TACE) inhibitors on S1' pocket and their quantitative structure-activity relationship (QSAR) study. |
Yonsei University |
21106451 |
39 |
Novel TNF-a converting enzyme (TACE) inhibitors as potential treatment for inflammatory diseases. |
Merck Research Laboratories |
20663669 |
36 |
Biaryl substituted hydantoin compounds as TACE inhibitors. |
Merck Research Laboratories |
20180536 |
128 |
Potent arylsulfonamide inhibitors of tumor necrosis factor-alpha converting enzyme able to reduce activated leukocyte cell adhesion molecule shedding in cancer cell models. |
Universit£ |
20172725 |
49 |
Discovery and SAR of hydantoin TACE inhibitors. |
Merck Research Laboratories |
19767207 |
17 |
Synthesis and SAR of 2-phenyl-1-sulfonylaminocyclopropane carboxylates as ADAMTS-5 (Aggrecanase-2) inhibitors. |
Central Pharmaceutical Research Institute |
20022498 |
71 |
The discovery of novel tartrate-based TNF-alpha converting enzyme (TACE) inhibitors. |
Schering-Plough Research Institute |
20005097 |
58 |
Discovery of (pyridin-4-yl)-2H-tetrazole as a novel scaffold to identify highly selective matrix metalloproteinase-13 inhibitors for the treatment of osteoarthritis. |
Pfizer |
19908842 |
84 |
Identification and optimization of inhibitors of Trypanosomal cysteine proteases: cruzain, rhodesain, and TbCatB. |
National Human Genome Research Institute |
19703773 |
63 |
The identification of beta-hydroxy carboxylic acids as selective MMP-12 inhibitors. |
Gsk Medicines Research Centre |
19725580 |
93 |
Identification of an orally efficacious matrix metalloprotease 12 inhibitor for potential treatment of asthma. |
Wyeth Research |
19606871 |
124 |
N-O-isopropyl sulfonamido-based hydroxamates: design, synthesis and biological evaluation of selective matrix metalloproteinase-13 inhibitors as potential therapeutic agents for osteoarthritis. |
Universit£ |
18835710 |
69 |
Discovery of novel hydroxamates as highly potent tumor necrosis factor-alpha converting enzyme inhibitors. Part II: optimization of the S3' pocket. |
Schering-Plough Research Institute |
19410464 |
71 |
Synthesis and activity of tryptophan sulfonamide derivatives as novel non-hydroxamate TNF-alpha converting enzyme (TACE) inhibitors. |
Wyeth Research |
19053764 |
101 |
Dual inhibitors of matrix metalloproteinases and carbonic anhydrases: iminodiacetyl-based hydroxamate-benzenesulfonamide conjugates. |
Instituto Superior TéCnico |
18790648 |
317 |
Specific targeting of metzincin family members with small-molecule inhibitors: progress toward a multifarious challenge. |
University of Athens |
17936631 |
25 |
Chromen-based TNF-alpha converting enzyme (TACE) inhibitors: design, synthesis, and biological evaluation. |
Yonsei University |
17531482 |
67 |
Design and synthesis of 3,3-piperidine hydroxamate analogs as selective TACE inhibitors. |
Wyeth Research |
17368021 |
55 |
Hydantoins, triazolones, and imidazolones as selective non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE). |
Bristol-Myers Squibb Pharmaceutical Research Institute |
17276676 |
112 |
A new 4-(2-methylquinolin-4-ylmethyl)phenyl P1' group for the beta-amino hydroxamic acid derived TACE inhibitors. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
17064892 |
123 |
Identification of potent and selective TACE inhibitors via the S1 pocket. |
Wyeth Research |
16723229 |
108 |
Design and synthesis of butynyloxyphenyl beta-sulfone piperidine hydroxamates as TACE inhibitors. |
Wyeth Research |
16516469 |
39 |
A cassette-dosing approach for improvement of oral bioavailability of dual TACE/MMP inhibitors. |
Novartis Institutes For Biomedical Research |
16516466 |
175 |
Synthesis and structure-activity relationship of a novel, achiral series of TNF-alpha converting enzyme inhibitors. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
16473009 |
23 |
Synthesis and evaluation of succinoyl-caprolactam gamma-secretase inhibitors. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
16426848 |
80 |
Acetylenic TACE inhibitors. Part 3: Thiomorpholine sulfonamide hydroxamates. |
Wyeth Research |
16289878 |
35 |
Conversion of potent MMP inhibitors into selective TACE inhibitors. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
16153831 |
87 |
Synthesis and SAR of highly selective MMP-13 inhibitors. |
Wyeth Research |
16084720 |
83 |
Acetylenic TACE inhibitors. Part 2: SAR of six-membered cyclic sulfonamide hydroxamates. |
Wyeth Research |
15953722 |
56 |
Discovery of 3-OH-3-methylpipecolic hydroxamates: potent orally active inhibitors of aggrecanase and MMP-13. |
Pfizer |
15911259 |
49 |
Discovery of 3,3-dimethyl-5-hydroxypipecolic hydroxamate-based inhibitors of aggrecanase and MMP-13. |
Pfizer |
15908214 |
95 |
Non-hydroxamate 5-phenylpyrimidine-2,4,6-trione derivatives as selective inhibitors of tumor necrosis factor-alpha converting enzyme. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
15745814 |
75 |
Synthesis and SAR of diazepine and thiazepine TACE and MMP inhibitors. |
Wyeth Research |
15686921 |
55 |
Structure-based design of potent and selective inhibitors of collagenase-3 (MMP-13). |
Pharmaceutical Research Institute |
15566296 |
142 |
Synthesis and structure-activity relationships of 4-alkynyloxy phenyl sulfanyl, sulfinyl, and sulfonyl alkyl hydroxamates as tumor necrosis factor-alpha converting enzyme and matrix metalloproteinase inhibitors. |
Wyeth Research |
15546732 |
11 |
Structure-based virtual screening and biological evaluation of potent and selective ADAM12 inhibitors. |
Department of Life Science and National Research Laboratory of Proteolysis |
15357971 |
228 |
Synthesis and structure-activity relationship of a novel sulfone series of TNF-alpha converting enzyme inhibitors. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
15261259 |
48 |
Benzodiazepine inhibitors of the MMPs and TACE. Part 2. |
Wyeth Research |
15125955 |
84 |
Reverse hydroxamate-based selective TACE inhibitors. |
Kaken Pharmaceutical |
15055993 |
30 |
Azasugar-based MMP/ADAM inhibitors as antipsoriatic agents. |
Hokkaido Collaboration Center N-21 |
15006405 |
20 |
Synthesis and biological activity of selective azasugar-based TACE inhibitors. |
Organon K.K. |
12951101 |
79 |
Synthesis and biological activity of piperazine-based dual MMP-13 and TNF-alpha converting enzyme inhibitors. |
Pfizer |
12877590 |
28 |
A potent, selective inhibitor of matrix metalloproteinase-3 for the topical treatment of chronic dermal ulcers. |
Pfizer |
12873518 |
81 |
Acetylenic TACE inhibitors. Part 1. SAR of the acyclic sulfonamide hydroxamates. |
Wyeth Research |
12873505 |
20 |
Design, synthesis and evaluation of novel azasugar-based MMP/ADAM inhibitors. |
Hokkaido Collaboration Center |
12873504 |
36 |
Structure--activity relationships of azasugar-based MMP/ADAM inhibitors. |
Hokkaido Collaboration Center |
12781190 |
113 |
Discovery of N-hydroxy-2-(2-oxo-3-pyrrolidinyl)acetamides as potent and selective inhibitors of tumor necrosis factor-alpha converting enzyme (TACE). |
Bristol-Myers Squibb Pharmaceutical Research Institute |
12781187 |
15 |
Discovery of selective phosphonamide-based inhibitors of tumor necrosis factor-alpha converting enzyme (TACE). |
Organon K.K. |
12723945 |
167 |
Design, synthesis, and evaluation of benzothiadiazepine hydroxamates as selective tumor necrosis factor-alpha converting enzyme inhibitors. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
12668018 |
138 |
Synthesis and SAR of bicyclic heteroaryl hydroxamic acid MMP and TACE inhibitors. |
Wyeth-Ayerst Research |
12408705 |
73 |
Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structure-activity relationships. |
Bristol-Myers Squibb |
12270165 |
80 |
Benzodiazepine inhibitors of the MMPs and TACE. |
Wyeth Research |
11992783 |
78 |
Synthesis and biological activity of selective pipecolic acid-based TNF-alpha converting enzyme (TACE) inhibitors. |
Pfizer |
11934588 |
69 |
Anthranilate sulfonamide hydroxamate TACE inhibitors. Part 2: SAR of the acetylenic P1' group. |
Wyeth-Ayerst Research |
11831905 |
33 |
New strategy for antedrug application: development of metalloproteinase inhibitors as antipsoriatic drugs. |
Organon K.K. |
11708926 |
84 |
Design of selective and soluble inhibitors of tumor necrosis factor-alpha converting enzyme (TACE). |
Glaxosmithkline |
11677124 |
67 |
Discovery of selective hydroxamic acid inhibitors of tumor necrosis factor-alpha converting enzyme. |
Abbott Laboratories |
11514157 |
48 |
N-hydroxyformamide peptidomimetics as TACE/matrix metalloprotease inhibitors: oral activity via P1' isobutyl substitution. |
Glaxosmithkline |
32470298 |
42 |
-Aryl-3-mercaptosuccinimides as Antivirulence Agents Targeting |
Helmholtz Institute For Pharmaceutical Research Saarland (Hips) - Helmholtz Centre For Infection Research (Hzi |
27045975 |
34 |
Notch Antagonists: Potential Modulators of Cancer and Inflammatory Diseases. |
Centre Hospitalier Universitaire Vaudois (Chuv) |
27194201 |
164 |
Use of Osmotic Pumps to Establish the Pharmacokinetic-Pharmacodynamic Relationship and Define Desirable Human Performance Characteristics for Aggrecanase Inhibitors. |
Eli Lilly |
10579851 |
151 |
New alpha-substituted succinate-based hydroxamic acids as TNFalpha convertase inhibitors. |
Astrazeneca |
12014967 |
25 |
Beta-aryl-succinic acid hydroxamates as dual inhibitors of matrix metalloproteinases and tumor necrosis factor alpha converting enzyme. |
Preclinical Research Novartis Pharma |
28818461 |
67 |
Discovery and process development of a novel TACE inhibitor for the topical treatment of psoriasis. |
Nestl� |
30034605 |
15 |
In Search of Selectivity in Inhibition of ADAM10. |
University of Notre Dame |
28711352 |
14 |
Development of a prodrug of hydantoin based TACE inhibitor. |
Merck |
28122457 |
12 |
Idiopathic Pulmonary Fibrosis: Current Status, Recent Progress, and Emerging Targets. |
Taipei Medical University |
28558971 |
38 |
Fused bi-heteroaryl substituted hydantoin compounds as TACE inhibitors. |
Merck |
28408220 |
55 |
First insight into structure-activity relationships of selective meprin? inhibitors. |
Fraunhofer Institute For Cell Therapy and Immunology Izi |
16206837 |
9 |
Tyrosinase inhibition: conformational analysis based studies on molecular dynamics calculations of bipiperidine based inhibitors. |
University of Karachi |
9353361 |
3 |
[3H]RY 80: A high-affinity, selective ligand for gamma-aminobutyric acidA receptors containing alpha-5 subunits. |
National Institute of Diabetes and Digestive and Kidney Diseases |
7515823 |
54 |
Actions of phenylglycine analogs at subtypes of the metabotropic glutamate receptor family. |
Novo Nordisk |
7509389 |
8 |
Pharmacological profile of FK480, a novel cholecystokinin type-A receptor antagonist: comparison to loxiglumide. |
Fujisawa Pharmaceutical |
7473144 |
1 |
Pharmacological characterization of GT-2016, a non-thiourea-containing histamine H3 receptor antagonist: in vitro and in vivo studies. |
Gliatech |
18355729 |
12 |
Structure-based dissection of the natural product cyclopentapeptide chitinase inhibitor argifin. |
University of Dundee |