182 articles for thisTarget

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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
31786008	37	Preparation and biological evaluation of BACE1 inhibitors: Leveraging trans-cyclopropyl moieties as ligand efficient conformational constraints.	Eli Lilly
27563406	128	Discovery of Fluoromethylketone-Based Peptidomimetics as Covalent ATG4B (Autophagin-1) Inhibitors.	Roche Pharma Research and Early Development
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
31913032	86	Plasmepsin Inhibitors in Antimalarial Drug Discovery: Medicinal Chemistry and Target Validation (2000 to Present).	University of Zambia
31062983	83	Exploiting Structural Dynamics To Design Open-Flap Inhibitors of Malarial Aspartic Proteases.	Latvian Institute of Organic Synthesis
31589043	91	Discovery of AM-6494: A Potent and Orally Efficacious ?-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor with in Vivo Selectivity over BACE2.	TBA
30709653	173	New evolutions in the BACE1 inhibitor field from 2014 to 2018.	Janssen Research & Development
30529637	76	Peptidomimetic plasmepsin inhibitors with potent anti-malarial activity and selectivity against cathepsin D.	Latvian Institute of Organic Synthesis
32003991	36	Biomimetic Macrocyclic Inhibitors of Human Cathepsin D: Structure-Activity Relationship and Binding Mode Analysis.	Czech Academy of Sciences
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
12061879	44	SMall Molecule Growth 2001 (SMoG2001): an improved knowledge-based scoring function for protein-ligand interactions.	Harvard University
29775538	47	Discovery of Potent and Centrally Active 6-Substituted 5-Fluoro-1,3-dihydro-oxazine ?-Secretase (BACE1) Inhibitors via Active Conformation Stabilization.	TBA
29636223	84	2-Aminoquinazolin-4(3H)-one based plasmepsin inhibitors with improved hydrophilicity and selectivity.	Latvian Institute of Organic Synthesis
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
29733614	47	Rational Design of Novel 1,3-Oxazine Based ?-Secretase (BACE1) Inhibitors: Incorporation of a Double Bond To Reduce P-gp Efflux Leading to Robust A? Reduction in the Brain.	TBA
29613789	138	Design and Synthesis of Clinical Candidate PF-06751979: A Potent, Brain Penetrant, ?-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor Lacking Hypopigmentation.	Pfizer
29944370	4	Izenamides A and B, Statine-Containing Depsipeptides, and an Analogue from a Marine Cyanobacterium.	Keio University
29087712	34	Grassystatins D-F, Potent Aspartic Protease Inhibitors from Marine Cyanobacteria as Potential Antimetastatic Agents Targeting Invasive Breast Cancer.	University of Florida
27997172	109	Aminomethyl-Derived Beta Secretase (BACE1) Inhibitors: Engaging Gly230 without an Anilide Functionality.	The Scripps Research Institute
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
34347470	98	Structure-Based Optimization of ML300-Derived, Noncovalent Inhibitors Targeting the Severe Acute Respiratory Syndrome Coronavirus 3CL Protease (SARS-CoV-2 3CL	Cleveland Clinic
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