scholarly journals C-Terminal KDEL Sequence of A KDEL-Tailed Cysteine Proteinase (Sulfhydryl-Endopeptidase) Is Involved in Formation of KDEL Vesicle and in Efficient Vacuolar Transport of Sulfhydryl-Endopeptidase

2003 ◽  
Vol 132 (4) ◽  
pp. 1892-1900 ◽  
Author(s):  
Takashi Okamoto ◽  
Tomoo Shimada ◽  
Ikuko Hara-Nishimura ◽  
Mikio Nishimura ◽  
Takao Minamikawa
Keyword(s):  
Cysteine Proteinase ◽  
Vacuolar Transport ◽  
Kdel Sequence

Major Kinds of Drug Targets in Chagas Disease or American Trypanosomiasis

2019 ◽  
Vol 20 (11) ◽  
pp. 1203-1216 ◽  
Author(s):  
Vilma G. Duschak
Keyword(s):  
Chagas Disease ◽  
Latin American ◽  
Drug Targets ◽  
Defense Mechanisms ◽  
Cysteine Proteinase ◽  
Parasitic Infection ◽  
Etiologic Agent ◽  
World Health ◽  
American Trypanosomiasis ◽  
Group I

American Trypanosomiasis, a parasitic infection commonly named Chagas disease, affects millions of people all over Latin American countries. Presently, the World Health Organization (WHO) predicts that the number of international infected individuals extends to 7 to 8 million, assuming that more than 10,000 deaths occur annually. The transmission of the etiologic agent, Trypanosoma cruzi, through people migrating to non-endemic world nations makes it an emergent disease. The best promising targets for trypanocidal drugs may be classified into three main groups: Group I includes the main molecular targets that are considered among specific enzymes involved in the essential processes for parasite survival, principally Cruzipain, the major antigenic parasite cysteine proteinase. Group II involves biological pathways and their key specific enzymes, such as Sterol biosynthesis pathway, among others, specific antioxidant defense mechanisms, and bioenergetics ones. Group III includes the atypical organelles /structures present in the parasite relevant clinical forms, which are absent or considerably different from those present in mammals and biological processes related to them. These can be considered potential targets to develop drugs with extra effectiveness and fewer secondary effects than the currently used therapeutics. An improved distinction between the host and the parasite targets will help fight against this neglected disease.

Molecular Characterization and Mapping of Murine Genes Encoding Three Members of the Stefin Family of Cysteine Proteinase Inhibitors

Genomics ◽  
1993 ◽  
Vol 15 (3) ◽  
pp. 507-514 ◽  
Author(s):  
Florence W.L. Tsui ◽  
Hing-Wo Tsui ◽  
Samuel Mok ◽  
Irena Mlinaric ◽  
Neal G. Copeland ◽  
...  
Keyword(s):  
Molecular Characterization ◽  
Proteinase Inhibitors ◽  
Cysteine Proteinase ◽  
Cysteine Proteinase Inhibitors ◽  
Genes Encoding

scholarly journals A novel cysteine proteinase inhibitor from seeds of Enterolobium contortisiliquum and its effect on Callosobruchus maculatus larvae

2021 ◽  
Vol 25 ◽  
pp. 100876
Author(s):  
Natalia N.S. Nunes ◽  
Rodrigo S. Ferreira ◽  
Leonardo F.R. de Sá ◽  
Antônia Elenir A. de Oliveira ◽  
Maria Luiza V. Oliva
Keyword(s):  
Proteinase Inhibitor ◽  
Callosobruchus Maculatus ◽  
Cysteine Proteinase ◽  
Cysteine Proteinase Inhibitor

scholarly journals Identification of pyrogallol as a warhead in design of covalent inhibitors for the SARS-CoV-2 3CL protease

2021 ◽  
Vol 12 (1) ◽  
Author(s):  
Haixia Su ◽  
Sheng Yao ◽  
Wenfeng Zhao ◽  
Yumin Zhang ◽  
Jia Liu ◽  
...  
Keyword(s):  
Theoretical Calculations ◽  
Cysteine Proteinase ◽  
Covalent Binding ◽  
Food Sources ◽  
Binding Mechanism ◽  
Covalent Inhibitors ◽  
Catalytic Cysteine ◽  
3Cl Protease ◽  
Covalent Ligands ◽  
Covalent Inhibitor

AbstractThe ongoing pandemic of coronavirus disease 2019 (COVID-19) caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) urgently needs an effective cure. 3CL protease (3CLpro) is a highly conserved cysteine proteinase that is indispensable for coronavirus replication, providing an attractive target for developing broad-spectrum antiviral drugs. Here we describe the discovery of myricetin, a flavonoid found in many food sources, as a non-peptidomimetic and covalent inhibitor of the SARS-CoV-2 3CLpro. Crystal structures of the protease bound with myricetin and its derivatives unexpectedly revealed that the pyrogallol group worked as an electrophile to covalently modify the catalytic cysteine. Kinetic and selectivity characterization together with theoretical calculations comprehensively illustrated the covalent binding mechanism of myricetin with the protease and demonstrated that the pyrogallol can serve as an electrophile warhead. Structure-based optimization of myricetin led to the discovery of derivatives with good antiviral activity and the potential of oral administration. These results provide detailed mechanistic insights into the covalent mode of action by pyrogallol-containing natural products and a template for design of non-peptidomimetic covalent inhibitors against 3CLpros, highlighting the potential of pyrogallol as an alternative warhead in design of targeted covalent ligands.

Specific cleavage sites on human IgG subclasses by cruzipain, the major cysteine proteinase from Trypanosoma cruzi

2003 ◽  
Vol 130 (1) ◽  
pp. 23-29 ◽  
Author(s):  
Patricia Berasain ◽  
Carlos Carmona ◽  
Blas Frangione ◽  
Juan José Cazzulo ◽  
Fernando Goñi
Keyword(s):  
Trypanosoma Cruzi ◽  
Cysteine Proteinase ◽  
Igg Subclasses ◽  
Cleavage Sites ◽  
Human Igg

Purification and Structure of a Novel Cysteine Proteinase Inhibitor, Strepin P-1

1985 ◽  
Vol 49 (3) ◽  
pp. 799-805
Author(s):  
Kyoichi Ogura ◽  
Mitsuru Maeda ◽  
Masami Nagai ◽  
Takaharu Tanaka ◽  
Kyosuke Nomoto ◽  
...  
Keyword(s):  
Proteinase Inhibitor ◽  
Cysteine Proteinase ◽  
Cysteine Proteinase Inhibitor
Sign in / Sign up

Export Citation Format

Share Document