Caspases as targets for anti-inflammatory and anti-apoptotic drug discovery

Journal of Medicinal Chemistry

Volumn 43, Issue 18, 2000, Pages 3351-3371

  Talanian, R V ^a   Brady, K D ^a   Cryns, V L ^b  

^a BASF Bioresearch Corporation   (United States)

^b NORTHWESTERN UNIVERSITY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CAPTOPRIL; CASPASE; CASPASE 3; CASPASE INHIBITOR; DIPEPTIDYL CARBOXYPEPTIDASE INHIBITOR; INTERLEUKIN 1BETA CONVERTING ENZYME; INTERLEUKIN 1BETA CONVERTING ENZYME INHIBITOR;

ANTIINFLAMMATORY ACTIVITY; APOPTOSIS; CYTOKINE PRODUCTION; DRUG SCREENING; DRUG TARGETING; ENZYME DEFECT; ENZYME INHIBITION; ENZYME REGULATION; ENZYME STRUCTURE; INFLAMMATION; MULTIGENE FAMILY; PROTEIN DEGRADATION; REVIEW; SIGNAL TRANSDUCTION;

ANIMALS; ANTI-INFLAMMATORY AGENTS; ANTINEOPLASTIC AGENTS; APOPTOSIS; CASPASE 1; CASPASES; CYSTEINE PROTEINASE INHIBITORS; CYTOKINES; DRUG DESIGN; HUMANS; SIGNAL TRANSDUCTION; SUBSTRATE SPECIFICITY;

EID: 0034618635     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm000060f     Document Type: Review

References (299)

1. Mammalian caspases: Structure, activation, substrates, and functions during apoptosis
2. Identification of a new caspase homologue: Caspase-14
3. Identification and mapping Casp7, a cysteine protease resembling CPP32β, interleukin-1β converting enzymes, and CED-3
4. Characterization of seven murine caspase family members
5. Identification and characterization of murine caspase-14, a new member of the caspase family
6. Caspase-14 is a novel developmentally regulated protease
7. Murine caspase-11, an ICE-interacting protease, is essential for the activation of ICE
8. The C. elegans cell death gene ced-3 encodes a protein similar to mammalian interleukin-1β-converting enzyme
9. Protease activity of in vitro transcribed and translated Caenorhabditis elegans cell death gene (ced-3) product
10. The Caenorhabditis elegans cell-death protein CED-3 is a cysteine protease with substrate specificities similar to those of the human CPP32 protease
11. Proteases to die for
12. The Fas antigen is involved in peripheral but not thymic deletion of T lymphocytes in T cell receptor transgenic mice
13. Autocrine T-cell suicide mediated by APO-1/(Fas/CD95)
14. Fas ligand-induced apoptosis as a mechanism of immune privilege
15. Fas(CD95)/FasL interactions required for programmed cell death after T-cell activation
16. Die and let live: Eliminating dangerous lymphocytes
17. Caspases in T-cell receptor-induced thymocyte apoptosis
18. Mechanisms of lysis by cytotoxic T cells
19. Kinases in pro-inflammatory signal transduction pathways: New opportunities for drug discovery
20. Prodomain-dependent nuclear localization of the caspase-2 (Nedd2) precursor. A novel function for a caspase prodomain
21. Caspases: Their intracellular localization and translocation during apoptosis
22. Different subcellular distribution of caspase-3 and caspase-7 following Fas-induced apoptosis in mouse liver
23. An induced proximity model for caspase-8 activation
24. Autoproteolytic activation of pro-caspases by oligomerization
25. Caspase-9 can be activated without proteolytic processing
26. The domains of death: Evolution of the apoptosis machinery
27. The CARD domain: A new apoptotic signaling motif
28. NMR structure and mutagenesis of the Fas (APO-1/CD95) death domain
29. NMR structure and mutagenesis of the FADD (Mort1) death-effector domain
30. Solution structure of the RAIDD CARD and model for CARD/CARD interaction in caspase-2 and caspase-9 recruitment
31. Crystal structure of Apaf-1 caspase recruitment domain: An α-helical Greek key fold for apoptotic signaling
32. Solution structure of Apaf-1 CARD and its interaction with caspase-9 CARD: A structural basis for specific adaptor/caspase interaction
33. Structural basis of procaspase-9 recruitment by the apoptotic protease-activating factor 1
34. 2 homodimer
35. Structure and mechanism of interleukin-1β converting enzyme
36. The three-dimensional structure of apopain/CPP32, a key mediator of apoptosis
37. Structure of recombinant human CPP32 in complex with the tetrapeptide acetyl-Asp-Val-Ala-Asp fluoromethyl ketone
38. The three-dimensional structure of caspase-8: An initiator enzyme in apoptosis
39. The atomic-resolution structure of human caspase-8, a key activator of apoptosis
40. A novel heterodimeric cysteine protease is required for interleukin-1β processing in monocytes
41. A combinatorial approach defines specificities of members of the caspase family and granzyme B
42. Substrate specificities of caspase family proteases
43. Use of monoclonal antibodies to study interleukin-1β-converting enzyme expression: Only precursor forms are detected in interleukin-1β-secreting cells
44. CPP32, a novel human apoptotic protein with homology to Caenorhabditis elegans cell death protein Ced-3 and mammalian interleukin-1β-converting enzyme
45. Mch3, a novel human apoptotic cysteine protease highly related to CPP32
46. Regulation of cell death protease caspase-9 by phosphorylation
47. Phosphorylated forms of activated caspases are present in cytosol from HL-60 cells during etoposide-induced apoptosis
48. Prevention of apoptosis by a baculovirus gene during infection of insect cells
49. Viral inhibition of inflammation: Cowpox virus encodes an inhibitor of the interleukin-1β converting enzyme
50. Inhibition of ICE family proteases by baculovirus antiapoptotic protein p35
51. Interaction of the adenovirus 14.7-kDa protein with FLICE inhibits Fas ligand-induced apoptosis
52. The TNFR2-TRAF signaling complex contains two novel proteins related to Baculoviral inhibitor of apoptosis proteins
53. The gene for neuronal apoptosis inhibitory protein is partially deleted in individuals with spinal muscular atrophy
54. A conserved family of cellular genes related to the baculovirus iap gene and encoding apoptosis inhibitors
55. Suppression of apoptosis in mammalian cells by NAIP and a related family of IAP genes
56. Cloning and expression of apoptosis inhibitory protein homologues that function to inhibit apoptosis and/or bind tumor necrosis factor receptor-associated factors
57. A novel anti-apoptosis gene, survivin, expressed in cancer and lymphoma
58. X-linked IAP is a direct inhibitor of cell-death proteases
59. The c-IAP-1 and c-IAP-2 proteins are direct inhibitors of specific caspases
60. Nitric oxide (NO): An effector of apoptosis
61. The anti-apoptotic actions of nitric oxide in hepatocytes
62. Macrophage cytotoxicity: Role for L-arginine deiminase and imino nitrogen oxidation to nitrite
63. Nitric oxide: A cytotoxic activated macrophage effector molecule
64. Apparent hydroxyl radical production by peroxynitrite: Implications for endothelial injury from nitric oxide and superoxide
65. DNA deaminating ability and genotoxicity of nitric oxide and its progenitors
66. Islet cell DNA is a target of inflammatory attack by nitric oxide
67. p53 Expression in nitric oxide-induced apoptosis
68. Nitric oxide produced by human B lymphocytes inhibits apoptosis and Epstein-Barr virus reactivation
69. S-Nitrosylation of proteins with nitric oxide: Synthesis and characterization of biologically active compounds
70. Nitric oxide reversibly inhibits seven members of the caspase family via S-nitrosylation
71. Nitric oxide inhibits caspase-3 by S-nitrosation in vivo
72. Mass spectrometric analysis of nitric oxide-modified caspase-3
73. Suppression of apoptosis by nitric oxide via inhibition of interleukin-1β-converting enzyme (ICE)-like and cysteine protease protein (CPP)-32-like proteases
74. Nitric oxide inhibits apoptosis by preventing increases in caspase-3-like activity via two distinct mechanisms
75. Nitric oxide prevents IL-1 and IGIF (IL-18) release from macrophages by inhibiting caspase-1 (ICE)
76. Nitric oxide inhibits Fas-induced apoptosis
77. Fas-induced caspase denitrosylation
78. Targeting nitric oxide (NO) delivery in Vivo. Design of a liver-selective NO donor prodrug that blocks tumor necrosis factor-α-induced apoptosis and toxicity in the liver
79. Molecular cloning of the interleukin-1β converting enzyme
80. Caspase-1 processes IFN-γ-inducing factor and regulates LPS-induced IFN-γ production
81. Activation of interferon-γ inducing factor mediated by interleukin-1β converting enzyme
82. Altered cytokine export and apoptosis in mice deficient in interleukin-1β converting enzyme
83. Mice deficient in IL-1β-converting enzyme are defective in production of mature IL-1β and resistant to endotoxic shock
84. Reduction of inflammation and pyrexia in the rat by oral administration of SDZ 224-015, an inhibitor of the interleukin-1β converting enzyme
85. A synthetic inhibitor of interleukin-1β converting enzyme prevents endotoxin-induced interleukin-1β production in vitro and in vivo
86. Inhibition of mature IL-1β production in murine macrophages and a murine model of inflammation by WIN 67694, an inhibitor of IL-1β converting enzyme
87. Identification of CARDIAK, a RIP-like kinase that associates with caspase-1
88. Differential roles of TLR2 and TLR4 in recognition of gram-negative and gram-positive bacterial cell wall components
89. Serial killers: Ordering caspase activation events in apoptosis
90. Apoptosis induction by caspase-8 is amplified through the mitochondrial release of cytochrome c
91. Two CD95 (APO-1/Fas) signaling pathways
92. Differential modulation of apoptosis sensitivity in CD95 type I and type II cells
93. Cleavage of BID by caspase 8 mediates the mitochondrial damage in the Fas pathway of apoptosis
94. Bid, a Bcl2 interacting protein, mediates cytochrome c release from mitochondria in response to activation of cell surface death receptors
95. Induction of apoptotic program in cell-free extracts: Requirement for dATP and cytochrome c
96. Induction of apoptosis by the transcription factor c-Jun
97. Role for Bcl-x(L) as an inhibitor of cytosolic cytochrome c accumulation in DNA-damage induced apoptosis
98. The release of cytochrome c from mitochondria: A primary site for Bcl-2 regulation of apoptosis
99. Prevention of apoptosis by Bcl-2: Release of cytochrome c from mitochondria blocked
100. Bax directly induces release of cytochrome c from isolated mitochondria
101. Bax interacts with the permeability transition pore to induce permeability transition and cytochrome c release in isolated mitochondria
102. Bcl-x(L) regulates the membrane potential and volume homeostasis of mitochondria
103. Bax and adenine nucleotide translocator cooperate in the mitochondrial control of apoptosis
104. Bcl-2 famiy proteins regulate the release of apoptogenic cytochrome c by the mitochondrial channel VDAC
105. WD-40 repeat region regulates Apaf-1 self-association and procaspase-9 activation
106. Autoactivation of procaspase-9 by Apaf-1-mediated oligomerization
107. Essential role of CED-4 oligomerization in CED-3 activation and apoptosis
108. Regulation of apoptotic protease activating factor-1 oligomerization and apoptosis by the WD-40 repeat region
109. Cytochrome c and dATP-mediated oligomerization of Apaf-1 is a prerequisite for procaspase-9 activation
110. An APAF-1/cytochrome c multimeric complex is a functional apoptosome that activates procaspase-9
111. Apaf-1 oligomerizes into biologically active ~700-kDa and inactive ~1.4-MDa apoptosome complexes
112. TRAIL and its receptors
113. Apoptosis control by death and decoy receptors
114. Caspase activation: The induced-proximity model
115. A novel protein that interacts with the death domain of Fas/APO1 contains a sequence motif related to the death domain
116. FADD, a novel death domain-containing protein, interacts with the death domain of Fas and initiates apoptosis
117. Involvement of MACH, a novel MORT1/FADD-interacting protease, in Fas/APO-1- and TNF receptor-induced cell death
118. FLICE, a novel FADD-homologous ICE/CED-3-like protease, is recruited to the CD95 (Fas/APO-1) death-inducing signal complex
119. CASH, a novel caspase homologue with death effector domains
120. I-FLICE, a novel inhibitor of tumor necrosis factor receptor-1 and CD-95-induced apoptosis
121. Inhibition of death receptor signals by cellular FLIP
122. FLAME-1, a novel FADD-like anti-apoptotic molecule that regulates Fas/TNFR1-induced apoptosis
123. Conversion of Bcl-2 to a Bax-like death effector by caspases
124. Modulation of cell death by Bcl-X(L) through caspase interaction
125. Alphaviruses induce apoptosis in Bcl-2-overexpressing cells: Evidence for a caspase-mediated, proteolytic inactivation of Bcl-2
126. Caspase-3-dependent cleavage of Bcl-2 promotes release of cytochrome c
127. Cleavage of human inhibitor of apoptosis protein XIAP results in fragments with distinct specificities for caspases
128. NF-κB antiapoptosis: Induction of TRAF1 and TRAF2 and c-IAP1 and c- IAP2 to suppress caspase-8 activation
129. Cleavage of the death domain kinase RIP by caspase-8 prompts TNF-induced apoptosis
130. Apoptosis promotes a caspase-induced amino-terminal truncation of IκBα that functions as a stable inhibitor of NF-κB
131. Bid-deficient mice are resistant to Fas-induced hepatocellular apoptosis
132. Proteolytic activation of protein kinase Cδ by an ICE-like protease in apoptotic cells
133. The regulation of anoikis: MEKK-1 activation requires cleavage by caspases
134. Caspase-3-mediated cleavage of protein kinase C θ in induction of apoptosis
135. Activation of hPAK65 by caspase cleavage induces some of the morphological and biochemical changes of apoptosis
136. Membrane and morphological changes in apoptotic cells regulated by caspase-mediated activation of PAK2
137. MEK kinase 1, a substrate for DEVD-directed caspases, is involved in genotoxin-induced apoptosis
138. Proteolytic cleavage and activation of protein kinase Cμ by caspase-3 in the apoptotic response of cells to 1-β-D-Arabinofuranosylcytosine and other genotoxic agents
139. Cleavage of poly(ADP-ribose) polymerase by a proteinase with properties such as ICE
140. Apopain/CPP32 cleaves proteins that are essential for cellular repair: A fundamental principle of apoptotic death
141. DNA-dependent protein kinase is a target for a CPP32-like apoptotic protease
142. The large subunit of replication factor C is a substrate for caspase-3 in vitro and is cleaved by a caspase-3-like protease during Fas-mediated apoptosis
143. The large subunit of the DNA replication complex C (DSEB/RF-C140) cleaved and inactivated by caspase-3 (CPP32/YAMA) during Fas-induced apoptosis
144. Role of caspase-mediated cleavage of rad51 in induction of apoptosis by DNA damage
145. Cleavage and inactivation of ATM during apoptosis
146. Rad51 protein involved in repair and recombination in Saccharomyces cerevisiae is a RecA-like protein
147. DNA-dependent protein kinase is one of a subset of autoantigens specifically cleaved early during apoptosis
148. trans-Dominant inhibition of poly(ADP-ribosyl)ation sensitizes cells against γ-irradiation and N-methyl-N'-nitro-N-nitrosoguanidine but does not limit DNA replication of a polyomavirus replicon
149. Characterization of the execution phase of apoptosis in vitro using extracts from condemned-phase cells
150. A dominant-negative mutant of human poly-(ADP-ribose) polymerase affects cell recovery, apoptosis, and sister chromatid exchange following DNA damage
151. Interleukin-1β-converting enzyme-like protease cleaves DNA-dependent protein kinase in cytotoxic T cell killing
152. Acinus is a caspase-3-activated protein required for apoptotic condensation
153. DFF, a heterodimeric protein that functions downstream of caspase-3 to trigger DNA fragmentation during apoptosis
154. A caspase-activated DNase that degrades DNA during apoptosis, and its inhibitor ICAD
155. Cleavage of CAD inhibitor in CAD activation and DNA degradation during apoptosis
156. Microfilament reorganization during apoptosis: The role of Gas2, a possible substrate for ICE-like proteases
157. Studies of the lamin proteinase reveal multiple parallel biochemical pathways during apoptotic execution
158. Cleavage of actin by interleukin 1β-converting enzyme to reverse DNase I inhibition
159. Lamin proteolysis facilitates nuclear events during apoptosis
160. Cleavage of lamin A by Mch2α but not CPP32: Multiple interleukin 1β-converting enzyme-related proteases with distinct substrate recognition properties are active in apoptosis
161. Dismantling cell-cell contacts during apoptosis is coupled to a caspase-dependent proteolytic cleavage of beta-catenin
162. Caspase cleavage of keratin 18 and reorganization of intermediate filaments during epithelial cell apoptosis
163. Caspase-3-generated fragment of gelsolin: Effector of morphological change in apoptosis
164. Apoptosis generates stable fragments of human type I keratins
165. Actin cleavage by CPP-32/apopain during the development of apoptosis
166. Plasma membrane alterations and cytoskeletal changes in apoptosis
167. Cleavage of focal adhesion kinase by caspases during apoptosis
168. Rapid fragmentation of vimentin in human skin fibroblasts exposed to tamoxifen: A possible involvement of caspase-3
169. Caspase-mediated cleavage of focal adhesion kinase pp125FAK and disassembly of focal adhesions in human endothelial cell apoptosis
170. Apoptosis in the pathogenesis and treatment of disease
171. ICE/CED-3-like proteases as therapeutic targets for the control of inappropriate apoptosis
172. Inherited human caspase 10 mutations underlie defective lymphocyte and dendritic cell apoptosis in autoimmune lymphoproliferative syndrome type II
173. Activation of apoptosis pathways by anticancer treatment
174. Caspase 8 is deleted or silenced preferentially in childhood neuroblastomas with amplification of MYCN
175. High levels of expression and nuclear localization of interleukin-1β converting enzyme (ICE) and CPP32 in favorable human neuroblastomas
176. Relationship between the expression of caspase-3 and the clinical outcome of patients with nonsmall cell lung cancer
177. Modulation of caspase-8 and FLICE-inhibitory protein expression as a potential mechanism of Epstein-Barr virus tumorigenesis in Burkitt's lymphoma
178. Developmentally regulated expression of the novel cancer anti-apoptosis gene survivin in human and mouse differentiation
179. IAP-family protein survivin inhibits caspase activity and apoptosis induced by Fas (CD95), Bax, caspases, and anticancer drugs
180. Caspase-8 is required for cell death induced by expanded polyglutamine repeats
181. Involvement ofcaspases in proteolytic cleavage of Alzheimer's amyloid-β-precursor protein and amyloidogenic Aβ peptide formation
182. Caspase-12 mediates endoplasmic-reticulum-specific apoptosis and cytotoxicity by amyloid-β
183. Antibody to caspase-cleaved actin detects apoptosis in differentiated neuroblastoma and microglia in Alzheimer's disease
184. Cleavage of huntingtin by apopain, a proapoptotic cysteine protease, is modulated by the polyglutamine tract
185. Alternative cleavage of Alzheimer-associated presenilins during apoptosis by a caspase-3 family protease
186. Presenilins are processed by caspase-type proteases
187. Dentatorubral pallidoluysian atrophy (DRPLA) protein cleaved by caspase-3 during apoptosis
188. Tau cleavage and dephosphorylation in cerebellar granule neurons undergoing apoptosis
189. Caspase cleavage of gene products associated with triplet expansion disorders generates truncated fragments containing the polyglutamine tract
190. Cleavage of atrophin-1 at caspase site aspartic acid 109 modulates cytotoxicity
191. Inhibiting caspase cleavage of huntingtin reduces toxicity and aggregate formation in neuronal and nonneuronal cells
192. Attenuation of transient focal cerebral ischemic injury in transgenic mice expressing a mutant ICE inhibitory protein
193. Inhibition of interleukin 1β converting enzyme family proteases reduces ischemic and excitotoxic neuronal damage
194. Co-localization of the cysteine protease caspase-3 with apoptotic myocytes aider in vivo myocardial ischemia and reperfusion in the rat
195. Caspase inhibitor affords neuroprotection with delayed administration in a rat model of neonatal hypoxicischemic brain injury
196. Attenuation of ischemia/reperfusion injury in rats by a caspase inhibitor
197. A specific inhibitor of apoptosis decreases tissue injury after intestinal ischemia-reperfusion in mice
198. Caspase inhibition reduces myocyte cell death induced by myocardial ischemia and reperfusion in vivo
199. Release of caspase-9 from mitochondria during neuronal apoptosis and cerebral ischemia
200. Caspase-8 and caspase-3 are expressed by different populations of cortical neurons undergoing delayed cell death after focal stroke in the rat
201. Increases in Bcl-2 and cleavage of caspase-1 and caspase-3 in human brain after head injury
202. Activation of the caspase-3 apoptotic cascade in traumatic spinal cord injury
203. The mitochondrial apoptotic pathway is activated by serum and glucose deprivation in cardiac myocytes
204. Apoptosis in heart failure: Release of cytochrome c from mitochondria and activation of caspase-3 in human cardiomyopathy
205. Reduced ischemic brain injury in interleukin-1β converting enzyme-deficient mice
206. Inhibition of apoptosis induced by ischemia-reperfusion prevents inflammation
207. Synthetic activation of caspases: Artificial death switches
208. Improved artificial death switches based on caspases and FADD
209. Induction of apoptosis and 1inhibition of cell proliferation by survivin gene targeting
210. Killing HIV-infected cells by transduction with an HIV protease-activated caspase-3 protein
211. In vivo protein transduction: Delivery of a biologically active protein into the mouse
212. Inhibition of ICE slows ALS in mice
213. Inhibition of caspase-1 slows disease progression in a mouse model of Huntington's disease
214. Expression of a dominant negative mutant of interleukin-1 β converting enzyme in transgenic mice prevents neuronal cell death induced by trophic factor withdrawal and ischemic brain injury
215. Elevation of neuronal expression of NAIP reduces ischemic damage in the rat hippocampus
216. Attenuation of ischemia-induced cellular and behavioral defecits by X chromosome-linked inhibitor of apoptosis protein overexpression in the rat hippocampus
217. Prolonged therapeutic window for ischemic brain damage caused by delayed caspase activation
218. Functional role of caspase-1 and caspase-3 in an ALS transgenic mouse model
219. BAX-induced cell death may not require interleukin 1β-converting enzyme-like proteases
220. Inhibition of Ced-3/ICE-related proteases does not prevent cell death induced by oncogenes, DNA damage, or the Bcl-2 homologue Bak
221. Inhibition of caspases inhibits the release of apoptotic bodies: Bcl-2 inhibits the initiation and formation of apoptotic bodies in chemotherapeutic agent-induced apoptosis
222. Antimalarial synergy of cysteine and aspartic protease inhibitors
223. Antimalarial effects in mice of orally administered peptidyl cysteine protease inhibitors
224. Crystal structure of gingipain R: An Arg-specific bacterial cysteine proteinase with a caspase-like fold
225. Arg-gingipain inhibition and anti-bacterial activity selective for Porphyromonas gingivalis by malabaricone C
226. Inhibition of cathepsin K - A novel approach to antiresorptive therapy
227. Cysteine proteases as therapeutic targets
228. Cysteine proteinase inhibitors decrease articular cartilage and bone destruction in chronic inflammatory arthritis
229. Cysteine proteinases in arthritis and inflammation
230. Activation of interleukin-1β by a co-induced protease
231. A pre-aspartate-specific protease from human leukocytes that cleaves pro-interleukin-1β
232. Synthesis of a potent, reversible inhibitor of interleukin-1β converting enzyme
233. Phenylalkyl ketones as potent reversible inhibitors of interleukin-1β converting enzyme
234. Inactivation ofinterleukin-1β converting enzyme by peptide (acyloxy)methyl ketones
235. A catalytic mechanism for caspase-1 and for bimodal inhibition of caspase-1 by activated aspartic ketones
236. Pharmacologic, pharmacokinetic, and therapeutic differences among ACE inhibitors
237. In vitro and in vivo studies of ICE inhibitors
238. Bimodal inhibition of caspase-1 by aryloxymethyl and acyloxymethyl ketones
239. P1 aspartate-based peptide α-((2,6-dichlorobenzoyl)oxy)methyl ketones as potent time-dependent inhibitors of interleukin-1β-converting enzyme
240. Synthesis of P1 aspartate-based peptide acyloxymethyl and fiuoromethyl ketones as inhibitors of interleukin-1β-converting enzyme
241. Peptidyl (acyloxy)methyl ketones and the quiescent affinity label concept: The departing group as a variable structural element in the design of inactivators of cysteine proteinases
242. Inhibition of interleukin-1β converting enzyme by N-acyl-aspartic acid ketones
243. Activated ketones as potent reversible inhibitors of interleukin-1β converting enzyme
244. Peptidomimetic aminomethylene ketone inhibitors of interleukin-1β-converting enzyme (ICE)
245. Inhibition of interleukin-1β converting enzyme by N-acyl-aspartyl aryloxymethyl ketones
246. Peptidyl α-ketoheterocyclic inhibitors of human neutrophil elastase. 2. Effect of varying the hetrocyclic ring on in vitro potency
247. Potent and selective nonpeptide inhibitors of caspases 3 and 7 inhibit apoptosis and maintain cell functionality
248. Caspase inhibitors - A chemist's perspective
249. Preparation of an autolysis-resistant interleukin-1β converting enzyme mutant
250. Disulfiram is a potent inhibitor of proteases of the caspase family
251. Peptide aldehydes and nitriles as transition state analogue inhibitors of cysteine proteases
252. Aminoacylpyrrolidine-2-nitriles: Potent and stable inhibitors of dipeptidyl-peptidase IV (CD 26)
253. Mechanism of inhibition of cathepsin K by potent, selective 1,5-diacylcarbohydrazides: A new class of mechanism-based inhibitors of thiol proteases
254. Conformationally constrained 1,3-diamino ketones: A series of potent inhibitors of the cysteine protease cathepsin K
255. Cysteine protease inhibitors cure an experimental Trypanosoma cruzi infection
256. Nafamostat mesilate
257. Structure of human factor D. A complement system protein at 2.0 Å resolution
258. The crystal structure of the catalytic domain of human urokinase-type plasminogen activator
259. Rational design, synthesis, and x-ray structure of selective noncovalent thrombin inhibitors
260. Peptide based interleukin-1β converting enzyme (ICE) inhibitors: Synthesis, structure activity relationships and crystallographic study of the ICE-inhibitor complex
261. Substrate specificity of the protease that processes human interleukin-1β
262. The synthesis and evaluation of peptidyl aspartyl aldehydes as inhibitors of ICE
263. Structure-based design: From renin to HIV-1 protease
264. Examples of active areas of structure based-design
265. Aspartyl α-((1-phenyl-3-(trifluoromethyl)-pyrazol-5-yl)oxy)methyl ketones as interleukin-1β converting enzyme inhibitors. Significance of the P1 and P3 amido nitrogens for enzyme-peptide inhibitor binding
266. Structure-based design of nonpeptidic pyridone aldehydes as inhibitors of interleukin-1β converting enzyme
267. Pyridone-based peptidomimetic inhibitors of interleukin-1β-converting enzyme (ICE)
268. First examples of peptidomimetic inhibitors of interleukin-1β converting enzyme
269. Pyridazinodiazepines as a high-affinity, P2-P3 peptidomimetic class of interleukin-1β-converting enzyme inhibitor
270. Conformationally constrained inhibitors of caspase-1 (interleukin-1β converting enzyme) and of the human CED-3 homologue caspase-3 (CPP32, apopain)
271. A combinatorial approach for determining protease specificities: Application to interleukin-1β converting enzyme (ICE)
272. Hsp60 accelerates the maturation of pro-caspase-3 by upstream activator proteases during apoptosis
273. Aspartyl α-((diphenylphosphinyl)oxy)methyl ketones as novel inhibitors of interleukin-1β converting enzyme. Utility of the diphenylphosphinic acid leaving group for the inhibition of cysteine proteases
274. α-[(Tetronoyl)oxy]- and α-[(tetramoyl)oxy]-methyl ketone inhibitors of the interleukin-1β converting enzyme (ICE)
275. α-Keto amide inhibitors of interleukin-1β converting enzyme (caspase-1)
276. Synthesis and evaluation of diacylhydrazines as inhibitors of the interleukin-1β converting enzyme (ICE)
277. Vinyl sulfones as mechanism-based cysteine protease inhibitors
278. Synthesis of a peptidyl difluoro ketone bearing the aspartic acid side chain: An inhibitor of interleukin-1β converting enzyme
279. X-ray crystallographic structure of a papain-leupeptin complex
280. α-Helix dipoles and catalysis: Absorption and Raman spectroscopic studies of acyl cysteine proteases