The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
27774132 |
20 |
Discovery of TAK-272: A Novel, Potent, and Orally Active Renin Inhibitor. |
Takeda Pharmaceutical |
27690432 |
75 |
Discovery of Second Generation Reversible Covalent DPP1 Inhibitors Leading to an Oxazepane Amidoacetonitrile Based Clinical Candidate (AZD7986). |
Charles River Discovery Research Services |
27687967 |
17 |
Structure-based design of a new series of N-(piperidin-3-yl)pyrimidine-5-carboxamides as renin inhibitors. |
Takeda Pharmaceutical |
27211244 |
9 |
Tasiamide F, a potent inhibitor of cathepsins D and E from a marine cyanobacterium. |
University of Florida |
26978477 |
25 |
Fragment-Linking Approach Using (19)F NMR Spectroscopy To Obtain Highly Potent and Selective Inhibitors ofß-Secretase. |
Amgen |
26670264 |
73 |
Fragment-Based Discovery of 2-Aminoquinazolin-4(3H)-ones As Novel Class Nonpeptidomimetic Inhibitors of the Plasmepsins I, II, and IV. |
Latvian Institute of Organic Synthesis |
26608551 |
35 |
Synthesis of (3S,4S)-4-aminopyrrolidine-3-ol derivatives and biological evaluation for their BACE1 inhibitory activities. |
Korea University of Science and Technology |
25167370 |
75 |
Transition state mimetics of the Plasmodium export element are potent inhibitors of Plasmepsin V from P. falciparum and P. vivax. |
The Walter and Eliza Hall Institute of Medical Research |
26001341 |
19 |
Preparation and biological evaluation of conformationally constrained BACE1 inhibitors. |
Eli Lilly |
25781223 |
96 |
Utilizing structures of CYP2D6 and BACE1 complexes to reduce risk of drug-drug interactions with a novel series of centrally efficacious BACE1 inhibitors. |
The Scripps Research Institute |
25695670 |
35 |
Discovery of a series of efficient, centrally efficacious BACE1 inhibitors through structure-based drug design. |
Eurofarma Laboratorios |
25782742 |
76 |
trans-(3S,4S)-Disubstituted pyrrolidines as inhibitors of the human aspartyl protease renin. Part I: prime site exploration using an amino linker. |
Novartis Pharma |
25754490 |
44 |
trans-3,4-Disubstituted pyrrolidines as inhibitors of the human aspartyl protease renin. Part II: prime site exploration using an oxygen linker. |
Novartis Pharma |
25728416 |
25 |
Iminopyrimidinones: a novel pharmacophore for the development of orally active renin inhibitors. |
Merck Research Laboratories |
25613679 |
79 |
Development of 2-aminooxazoline 3-azaxanthenes as orally efficaciousß-secretase inhibitors for the potential treatment of Alzheimer's disease. |
Amgen |
25086681 |
57 |
Structure-based optimization of non-peptidic Cathepsin D inhibitors. |
Merck |
25050166 |
58 |
Structure-based design of substituted piperidines as a new class of highly efficacious oral direct Renin inhibitors. |
Novartis Institutes For Biomedical Research |
25537272 |
17 |
Structure-based design, synthesis and biological evaluation of novelß-secretase inhibitors containing a pyrazole or thiazole moiety as the P3 ligand. |
Purdue University |
25455483 |
61 |
Discovery of potent iminoheterocycle BACE1 inhibitors. |
Merck Research Laboratories |
25363711 |
62 |
Inhibitors ofß-site amyloid precursor protein cleaving enzyme (BACE1): identification of (S)-7-(2-fluoropyridin-3-yl)-3-((3-methyloxetan-3-yl)ethynyl)-5'H-spiro[chromeno[2,3-b]pyridine-5,4'-oxazol]-2'-amine (AMG-8718). |
Amgen |
25313316 |
20 |
3-Cyano-3-aza-ß-amino Acid Derivatives as Inhibitors of Human Cysteine Cathepsins. |
University of Bonn |
24921156 |
6 |
Dose-dependent inhibition of BACE-1 by the monoterpenoid 2,3,4,4-tetramethyl-5-methylenecyclopent-2-enone in cellular and mouse models of Alzheimer's disease. |
University of Coimbra |
24900843 |
60 |
Plasmepsin inhibitory activity and structure-guided optimization of a potent hydroxyethylamine-based antimalarial hit. |
Latvian Institute of Organic Synthesis |
24397738 |
41 |
Discovery of 7-tetrahydropyran-2-yl chromans:ß-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors that reduce amyloidß-protein (Aß) in the central nervous system. |
Array Biopharma |
23993670 |
2 |
Novel BACE1 inhibitors with a non-acidic heterocycle at the P1' position. |
Kyoto Pharmaceutical University |
24054120 |
5 |
The thermodynamic basis for the use of lipophilic efficiency (LipE) in enthalpic optimizations. |
Novartis Institutes For Biomedical Research |
23981898 |
20 |
Discovery of cyclic sulfoxide hydroxyethylamines as potent and selectiveß-site APP-cleaving enzyme 1 (BACE1) inhibitors: structure based design and in vivo reduction of amyloidß-peptides. |
Novartis Pharma |
23856050 |
28 |
Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: prime side chromane-containing inhibitors. |
Elan Pharmaceuticals |
23769639 |
17 |
Hydroxyethylamine-based inhibitors of BACE1: P1-P3 macrocyclization can improve potency, selectivity, and cell activity. |
Amgen |
23570791 |
2 |
Design and synthesis of thiophene dihydroisoquinolines as novel BACE1 inhibitors. |
Elan Pharmaceuticals |
23590342 |
105 |
ß-Secretase (BACE1) inhibitors with high in vivo efficacy suitable for clinical evaluation in Alzheimer's disease. |
F. Hoffmann-La Roche |
23537249 |
165 |
Spirocyclicß-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors: from hit to lowering of cerebrospinal fluid (CSF) amyloidß in a higher species. |
Array Biopharma |
23425156 |
24 |
The discovery of novel potent trans-3,4-disubstituted pyrrolidine inhibitors of the human aspartic protease renin from in silico three-dimensional (3D) pharmacophore searches. |
Novartis Pharma |
23360239 |
19 |
A novel class of oral direct renin inhibitors: highly potent 3,5-disubstituted piperidines bearing a tricyclic p3-p1 pharmacophore. |
Novartis Pharma |
23181502 |
57 |
Cyanobacterial peptides as a prototype for the design of potentß-secretase inhibitors and the development of selective chemical probes for other aspartic proteases. |
University of Florida |
22954357 |
29 |
Structure-based design of highly selectiveß-secretase inhibitors: synthesis, biological evaluation, and protein-ligand X-ray crystal structure. |
Purdue University |
22928914 |
104 |
Structure- and property-based design of aminooxazoline xanthenes as selective, orally efficacious, and CNS penetrable BACE inhibitors for the treatment of Alzheimer's disease. |
Amgen |
23010268 |
32 |
Design and synthesis of potent hydroxyethylamine (HEA) BACE-1 inhibitors carrying prime side 4,5,6,7-tetrahydrobenzazole and 4,5,6,7-tetrahydropyridinoazole templates. |
Medivir |
24900544 |
8 |
Discovery of DS-8108b, a Novel Orally Bioavailable Renin Inhibitor. |
TBA |
22884991 |
9 |
Antiplasmodial activities of 4-aminoquinoline-statine compounds. |
Universit£ |
22748705 |
2 |
Total synthesis of grassystatin A, a probe for cathepsin E function. |
Fudan University |
22727644 |
43 |
Synthesis and structure-activity relationship studies of 1,3-disubstituted 2-propanols as BACE-1 inhibitors. |
University of South Florida |
22380629 |
174 |
Discovery of cyclic sulfone hydroxyethylamines as potent and selectiveß-site APP-cleaving enzyme 1 (BACE1) inhibitors: structure-based design and in vivo reduction of amyloidß-peptides. |
Novartis Pharma |
22572583 |
49 |
Structure guided P1' modifications of HEA derivedß-secretase inhibitors for the treatment of Alzheimer's disease. |
Envoy Therapeutics |
20579874 |
150 |
BACE-1 hydroxyethylamine inhibitors using novel edge-to-face interaction with Arg-296. |
Glaxosmithkline |
20045648 |
39 |
Di-substituted pyridinyl aminohydantoins as potent and highly selective human beta-secretase (BACE1) inhibitors. |
Wyeth Research |
19715320 |
87 |
Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation. |
University of Florida |
19811916 |
83 |
Design and synthesis of cell potent BACE-1 inhibitors: structure-activity relationship of P1' substituents. |
Elan Pharmaceuticals |
19419206 |
77 |
Identification of 3-acetyl-2-aminoquinolin-4-one as a novel, nonpeptidic scaffold for specific calpain inhibitory activity. |
Ewha Womans University |
18434152 |
64 |
Synthesis, SAR, and X-ray structure of human BACE-1 inhibitors with cyclic urea derivatives. |
Lg Life Sciences |
18417344 |
6 |
Identification of acridinyl hydrazides as potent aspartic protease inhibitors. |
University of Karachi |
17980584 |
72 |
Discovery of an orally efficaceous 4-phenoxypyrrolidine-based BACE-1 inhibitor. |
Schering-Plough Research Institute |
18171614 |
63 |
BACE-1 inhibitors part 1: identification of novel hydroxy ethylamines (HEAs). |
Glaxosmithkline |
18068983 |
51 |
Acylguanidine inhibitors of beta-secretase: optimization of the pyrrole ring substituents extending into the S1' substrate binding pocket. |
Wyeth Research |
18023580 |
50 |
Potent pyrrolidine- and piperidine-based BACE-1 inhibitors. |
Schering-Plough Research Institute |
16797987 |
11 |
Synthesis of gallic acid based naphthophenone fatty acid amides as cathepsin D inhibitors. |
Institute of Medicinal and Aromatic Plants |
15139758 |
50 |
Incorporating molecular shape into the alignment-free Grid-Independent Descriptors. |
Universitat Pompeu Fabra |
10669559 |
180 |
Protease inhibitors: current status and future prospects. |
University of Queensland |
1527792 |
55 |
Specific inhibition of HIV-1 protease by boronated porphyrins. |
University of California |
2002469 |
80 |
Renin inhibitors containing conformationally restricted P1-P1' dipeptide mimetics. |
Merck Sharp and Dohme Research Laboratories |
3906131 |
61 |
Renin inhibitors. Syntheses of subnanomolar, competitive, transition-state analogue inhibitors containing a novel analogue of statine. |
TBA |
10498202 |
43 |
Synthesis and structure activity relationships of novel small molecule cathepsin D inhibitors. |
Bayer |
9873534 |
36 |
Identification of potent inhibitors of Plasmodium falciparum plasmepsin II from an encoded statine combinatorial library. |
Pharmacopeia |
| 37 |
Peptidomimetic inhibitors of human immunodeficiency virus protease (HIV-PR): Design, enzyme binding and selectivity, antiviral efficacy, and cell permeability properties |
TBA |
22204908 |
22 |
New benzimidazole derivatives as antiplasmodial agents and plasmepsin inhibitors: synthesis and analysis of structure-activity relationships. |
University of Karachi |
22130130 |
19 |
Discovery of pyrrolidine-basedß-secretase inhibitors: lead advancement through conformational design for maintenance of ligand binding efficiency. |
Merck Research Laboratories |
21835615 |
165 |
New pyrazolyl and thienyl aminohydantoins as potent BACE1 inhibitors: exploring the S2' region. |
Pfizer |
21388807 |
45 |
Structure based design, synthesis and SAR of cyclic hydroxyethylamine (HEA) BACE-1 inhibitors. |
Novartis Institutes For Biomedical Research |
21112780 |
30 |
Design and synthesis of potent macrocyclic renin inhibitors. |
Medivir |
20731374 |
65 |
Direct renin inhibitors as a new therapy for hypertension. |
Novartis Pharmaceuticals |
20943389 |
2 |
Triazolyl tryptoline derivatives asß-secretase inhibitors. |
Mahidol University |
20880704 |
200 |
Design and synthesis of aminohydantoins as potent and selective humanß-secretase (BACE1) inhibitors with enhanced brain permeability. |
Pfizer |
20833041 |
40 |
Design of an orally efficacious hydroxyethylamine (HEA) BACE-1 inhibitor in a preclinical animal model. |
Elan Pharmaceuticals |
20822903 |
87 |
Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: structure-activity relationship of the aryl region. |
Elan Pharmaceuticals |
20656487 |
45 |
Fragment-based discovery and optimization of BACE1 inhibitors. |
Evotec |
20347593 |
76 |
Piperazine sulfonamide BACE1 inhibitors: design, synthesis, and in vivo characterization. |
Merck Research Laboratories |
20438064 |
14 |
Mechanism-based inhibitors of the aspartyl protease plasmepsin II as potential antimalarial agents. |
Wayne State University |
20223661 |
48 |
Novel pyrrolyl 2-aminopyridines as potent and selective human beta-secretase (BACE1) inhibitors. |
Wyeth |
20202842 |
47 |
Pyridinyl aminohydantoins as small molecule BACE1 inhibitors. |
Wyeth Research |
20172717 |
35 |
Structure-based design and synthesis of novel P2/P3 modified, non-peptidic beta-secretase (BACE-1) inhibitors. |
Universit£ |
20102207 |
7 |
Synthesis and preclinical evaluations of 2-(2-fluorophenyl)-6,7-methylenedioxyquinolin-4-one monosodium phosphate (CHM-1-P-Na) as a potent antitumor agent. |
China Medical University |
20036448 |
20 |
Synthesis of potent BACE-1 inhibitors incorporating a hydroxyethylene isostere as central core. |
Link£Ping University |
20128595 |
24 |
Design and synthesis of potent and selective BACE-1 inhibitors. |
Stockholm University |
20122837 |
21 |
Discovery of potent BACE-1 inhibitors containing a new hydroxyethylene (HE) scaffold: exploration of P1' alkoxy residues and an aminoethylene (AE) central core. |
Stockholm University |
19963375 |
30 |
Macrocyclic BACE-1 inhibitors acutely reduce Abeta in brain after po application. |
Novartis Institutes For Biomedical Research |
19959359 |
46 |
Discovery and initial optimization of 5,5'-disubstituted aminohydantoins as potent beta-secretase (BACE1) inhibitors. |
Wyeth Research |
19968289 |
201 |
Design and synthesis of 5,5'-disubstituted aminohydantoins as potent and selective human beta-secretase (BACE1) inhibitors. |
Wyeth Research |
19757823 |
98 |
Aminoimidazoles as potent and selective human beta-secretase (BACE1) inhibitors. |
Wyeth Research |
20043696 |
17 |
Discovery of cyclic acylguanidines as highly potent and selective beta-site amyloid cleaving enzyme (BACE) inhibitors: Part I--inhibitor design and validation. |
Schering-Plough Research Institute |
19635672 |
35 |
alpha-Substituted norstatines as the transition-state mimic in inhibitors of multiple digestive vacuole malaria aspartic proteases. |
Uppsala University |
19576765 |
15 |
Design and synthesis of BACE-1 inhibitors utilizing a tertiary hydroxyl motif as the transition state mimic. |
Uppsala University |
19195887 |
18 |
Macrocyclic peptidomimetic beta-secretase (BACE-1) inhibitors with activity in vivo. |
Novartis Institutes For Biomedical Research |
| 10 |
Synthesis of irreversible HIV-1 protease inhibitors containing sulfonamide and sulfone as amide bond isosteres |
TBA |
| 6 |
Design, synthesis, and characterization of dipeptide isostere containing cis-epoxide for the irreversible inactivation of HIV protease |
TBA |
| 25 |
Synthesis and structure-activity relationships of benzophenones as inhibitors of cathepsin D |
TBA |
| 22 |
Novel pseudosymmetric inhibitors of HIV-1 protease |
TBA |
19323562 |
14 |
2-Pyridyl P1'-substituted symmetry-based human immunodeficiency virus protease inhibitors (A-792611 and A-790742) with potential for convenient dosing and reduced side effects. |
Abbott Laboratories |
19323561 |
11 |
Harnessing nature's insight: design of aspartyl protease inhibitors from treatment of drug-resistant HIV to Alzheimer's disease. |
Purdue University |
18842420 |
44 |
Design, synthesis and SAR of potent statine-based BACE-1 inhibitors: exploration of P1 phenoxy and benzyloxy residues. |
LinköPing University |
18468890 |
69 |
Rational design of novel, potent piperazinone and imidazolidinone BACE1 inhibitors. |
Schering-Plough Research Institute |
17638694 |
2 |
In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. |
Ambrilia Biopharma |
18166458 |
90 |
BACE-1 inhibitors part 2: identification of hydroxy ethylamines (HEAs) with reduced peptidic character. |
Glaxosmithkline |
18162398 |
43 |
Acylguanidine inhibitors of beta-secretase: optimization of the pyrrole ring substituents extending into the S1 and S3 substrate binding pockets. |
Wyeth Research |
17482814 |
37 |
Design, synthesis, and SAR of macrocyclic tertiary carbinamine BACE-1 inhibitors. |
Merck Research Laboratories |
17434734 |
28 |
Potent and selective isophthalamide S2 hydroxyethylamine inhibitors of BACE1. |
Pfizer |
17433698 |
6 |
Synthesis and biological evaluation of phosphino dipeptide isostere inhibitor of human beta-secretase (BACE1). |
Technische UniversitäT MüNchen |
17046251 |
38 |
Design of potent inhibitors of human beta-secretase. Part 1. |
Pfizer |
16162010 |
78 |
Synthesis of malarial plasmepsin inhibitors and prediction of binding modes by molecular dynamics simulations. |
Uppsala University |
15974592 |
68 |
Design and synthesis of potent inhibitors of plasmepsin I and II: X-ray crystal structure of inhibitor in complex with plasmepsin II. |
LinköPing University |
14741251 |
12 |
Rational design and synthesis of selective BACE-1 inhibitors. |
Merck Research Laboratories |
11906282 |
6 |
Molecular dynamics and free energy analyses of cathepsin D-inhibitor interactions: insight into structure-based ligand design. |
University of California |
10212129 |
20 |
Potent, low-molecular-weight non-peptide inhibitors of malarial aspartyl protease plasmepsin II. |
University of California |
9873703 |
4 |
Evaluation of a structure-based statine cyclic diamino amide encoded combinatorial library against plasmepsin II and cathepsin D. |
Pharmacopeia |
8410992 |
35 |
Renin inhibitors containing a pyridyl amino diol derived C-terminus. |
Hoechst |
8410973 |
75 |
Specificity in the binding of inhibitors to the active site of human/primate aspartic proteinases: analysis of P2-P1-P1'-P2' variation. |
University of Florida |
3126296 |
43 |
Inhibition of porcine pepsin by two substrate analogues containing statine. The effect of histidine at the P2 subsite on the inhibition of aspartic proteinases. |
University of Wisconsin |
1738148 |
16 |
Renin inhibitory pentols showing improved enteral bioavailability. |
Hoechst |
28820267 |
4 |
Causes and Significance of Increased Compound Potency in Cellular or Physiological Contexts. |
Merck |
28427814 |
24 |
Design, synthesis, and X-ray structural studies of BACE-1 inhibitors containing substituted 2-oxopiperazines as P1'-P2' ligands. |
Purdue University |
23853092 |
3 |
Histone deacetylase 7 promotes Toll-like receptor 4-dependent proinflammatory gene expression in macrophages. |
University of Queensland |
14730417 |
62 |
Comparative pharmacology of human beta-adrenergic receptor subtypes--characterization of stably transfected receptors in CHO cells. |
UniversitÄT WÜRzburg |
9225287 |
174 |
RS-102221: a novel high affinity and selective, 5-HT2C receptor antagonist. |
Roche Bioscience |
9223586 |
8 |
[125I]IPH, an epibatidine analog, binds with high affinity to neuronal nicotinic cholinergic receptors. |
Georgetown University |
9223553 |
16 |
[35S]Guanosine-5'-O-(3-thio)triphosphate binding as a measure of efficacy at human recombinant dopamine D4.4 receptors: actions of antiparkinsonian and antipsychotic agents. |
Institut De Recherches Servier |
9203642 |
14 |
Binding of a thrombin receptor tethered ligand analogue to human platelet thrombin receptor. |
Schering-Plough Research Institute |
7616392 |
5 |
Functional characterization of the nonpeptide neurokinin3 (NK3) receptor antagonist, SR142801 on the human NK3 receptor expressed in Chinese hamster ovary cells. |
Sanofi Recherche |
6325601 |
52 |
Cholecystokinin receptors: biochemical demonstration and autoradiographical localization in rat brain and pancreas using [3H] cholecystokinin8 as radioligand. |
F. Hoffmann-La Roche |
12498885 |
9 |
Neoglycopeptides as inhibitors of oligosaccharyl transferase: insight into negotiating product inhibition. |
Massachusetts Institute of Technology |
18835174 |
17 |
Preparation of (4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepin-5-ylidene)acetamide derivatives as novel arginine vasopressin V(2) receptor agonists. |
Astellas Pharma |
17961830 |
38 |
Allosteric inhibition of the protein-protein interaction between the leukemia-associated proteins Runx1 and CBFbeta. |
University of Virginia At Charlottesville |
17349580 |
6 |
Structures of lung cancer-derived EGFR mutants and inhibitor complexes: mechanism of activation and insights into differential inhibitor sensitivity. |
Harvard Medical School |
15658851 |
42 |
Selective estrogen receptor modulators with conformationally restricted side chains. Synthesis and structure-activity relationship of ERalpha-selective tetrahydroisoquinoline ligands. |
Novartis Pharmaceuticals |
15689158 |
21 |
Novel transient receptor potential vanilloid 1 receptor antagonists for the treatment of pain: structure-activity relationships for ureas with quinoline, isoquinoline, quinazoline, phthalazine, quinoxaline, and cinnoline moieties. |
Abbott Laboratories |
18072720 |
30 |
Stereospecific high-affinity TRPV1 antagonists: chiral N-(2-Benzyl-3-pivaloyloxypropyl) 2-[4-(methylsulfonylamino)phenyl]propionamide analogues. |
Seoul National University |
12639546 |
30 |
Identification of a high-affinity phosphopeptide inhibitor of Stat3. |
The University of Texas At Houston |
16942027 |
69 |
Carbonic anhydrase inhibitors: Hypoxia-activatable sulfonamides incorporating disulfide bonds that target the tumor-associated isoform IX. |
Istituto Di Biostrutture E Bioimmagini-Cnr |
15653343 |
20 |
Cyclic sulfamide HIV-1 protease inhibitors, with sidechains spanning from P2/P2' to P1/P1'. |
Uppsala University |