Cathepsin D
Cathepsin D is a lysosomal aspartic protease whose major described function is intracellular catabolism in lysosomal compartments, with additional roles in hormone processing and antigen processing[1]. Its function extends beyond nonspecific acidic bulk degradation, because cathepsin D-deficient mice maintain lysosomal bulk proteolysis but develop intestinal mucosal atrophy, lymphoid-cell destruction, and early death, indicating roles in limited proteolysis and tissue homeostasis[2]. Mechanistically, cathepsin D participates in endocytic and autophagic pathways where lysosomal proteases regulate substrate degradation and cellular remodeling[3]. In apoptosis-related models, mature lysosomal cathepsin D can translocate to the cytosol, and cathepsin D activity has been linked to induced apoptosis[4]. In breast cancer biology, cathepsin D is overexpressed and hypersecreted by epithelial breast cancer cells, correlates with clinical metastasis, and stimulates tumorigenicity, metastasis, cancer-cell proliferation, fibroblast outgrowth, and angiogenesis[4]. Compared with cathepsin E, cathepsin D showed distinct cytosolic activity after lysosomal permeabilization, because cathepsin D silencing prevented stefin B degradation whereas cathepsin E silencing did not[5]. For experimental applications, pepstatin A inhibited aspartic-protease-dependent stefin B degradation, and fluorogenic peptide probes detected cathepsin D activity in macrophages challenged with bacteria[5][6].
References:
- [1]. Fusek M, et al. Dual role of cathepsin D: ligand and protease. Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub. 2005 Jun;149(1):43-50. [Content Brief]
- [2]. Saftig P, et al. Mice deficient for the lysosomal proteinase cathepsin D exhibit progressive atrophy of the intestinal mucosa and profound destruction of lymphoid cells. EMBO J. 1995 Aug 1;14(15):3599-608. [Content Brief]
- [3]. Müller S, et al. Specific functions of lysosomal proteases in endocytic and autophagic pathways. Biochim Biophys Acta. 2012 Jan;1824(1):34-43. [Content Brief]
- [4]. Liaudet-Coopman E, et al. Cathepsin D: newly discovered functions of a long-standing aspartic protease in cancer and apoptosis. Cancer Lett. 2006 Jun 18;237(2):167-79. [Content Brief]
- [5]. Železnik TZ, et al. Aspartic cathepsin D degrades the cytosolic cysteine cathepsin inhibitor stefin B in the cells. Biochem Biophys Res Commun. 2015 Sep 18;465(2):213-7. [Content Brief]
- [6]. Rodriguez-Rios M, et al. A fluorogenic, peptide-based probe for the detection of Cathepsin D in macrophages. Commun Chem. 2023 Nov 2;6(1):237. [Content Brief]
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Cathepsin D Related Products (10)
Related Products (10)
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Recombinant Proteins (5)
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Antibodies (1)
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NOTA-FZCD-3
0 ImagesCat. No.: HY-P11844Purity: 98.43%NOTA-FZCD-3 is a NOTA (HY-134418)-labeled FZCD-3 polypeptide precursor that targets cathepsin D (CTSD) with a KD of 0.65 μM. NOTA-FZCD-3 binds specifically to the active site of CTSD, exhibits rapid in vivo clearance properties, and remains stable in blood for more than 2 h. NOTA-FZCD-3 can be used in studies monitoring CTSD-positive tumors.
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Ac-Glu-Asp(EDANS)-Lys-Pro-Ile-Leu-Phe-Phe-Arg-Leu-Gly-Lys(DABCYL)-Glu-NH2 acetate
0 ImagesCat. No.: HY-P4787APurity: 99.44%Ac-Glu-Asp(EDANS)-Lys-Pro-Ile-Leu-Phe-Phe-Arg-Leu-Gly-Lys(DABCYL)-Glu-NH2 acetate is a Cathepsin D substrate, that can be used for cathepsin D FRET assay.
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Cathepsin D and E FRET Substrate
0 ImagesCat. No.: HY-P2498CAS No.: 839730-93-7Cathepsin D and E FRET Substrate is a fluorogenic substrate for cathepsins D and E and not for B, H or L. The cleavage occurs at the Phe-Phe amide bond resul. Cathepsin D and E FRET Substrate is a valuable tool for routine assays and for mechanistic studies on cathepsins E and D.
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Ac-Glu-Asp(EDANS)-Lys-Pro-Ile-Leu-Phe-Phe-Arg-Leu-Gly-Lys(DABCYL)-Glu-NH2
0 ImagesCat. No.: HY-P4787CAS No.: 400716-78-1Ac-Glu-Asp(EDANS)-Lys-Pro-Ile-Leu-Phe-Phe-Arg-Leu-Gly-Lys(DABCYL)-Glu-NH2 is a cathepsin D substrate, that can be used for cathepsin D FRET assay.
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Cathepsin D degrader 1
0 ImagesCat. No.: HY-181655CAS No.: 3127060-85-6Anti-hepatic fibrosis agent 3 is an orally active anti-hepatic fibrosis compound targeting Cathepsin D. Anti-hepatic fibrosis agent 3 shows an IC50 of 53.18 μM against COL1A1-promoter and a Kd of 8.86 μM for binding to Cathepsin D. Anti-hepatic fibrosis agent 3 directly binds to and promotes the degradation of Cathepsin D, with no significant effect on Cathepsin B or Cathepsin L. Anti-hepatic fibrosis agent 3 inhibits hepatic stellate cell activation and reduces extracellular matrix deposition and inflammatory cytokine expression. Anti-hepatic fibrosis agent 3 exhibits remarkable anti-fibrotic activity in rat BDL and mouse CDAHFD-induced hepatic fibrosis models. Anti-hepatic fibrosis agent 3 can be used for the study of hepatic fibrosis.
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NB-533
0 ImagesCat. No.: HY-182429CAS No.: 1146544-18-4NB-533 is an orally active and brain-penetrant BACE-1 inhibitor with a human IC50 of 0.002 μM. NB-533 also inhibits human cathepsin D with an IC50 of 0.001 μM. NB-533 inhibits amyloidogenic amyloid precursor protein (APP) processing and reduces Aβ40 release. NB-533 reduces brain levels of APP metabolite C99 and Aβ40 in transgenic mice. NB-533 can be used for the research of Alzheimer’s disease.
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Tasiamide B
0 ImagesCat. No.: HY-N15154CAS No.: 587014-85-5Tasiamide B is a Cathepsin D inhibitor, which is a linear peptide found in the marine cyanobacteria Symploca sp.. Tasiamide B is proved as a good template for the development of aspartic proteases inhibitors. Tasiamide B is effective against skin cancer by strongly interacting with the target protein HSP90.
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NB-216
0 ImagesCat. No.: HY-11014CAS No.: 943924-04-7NB-216 is an orally active and brain-penetrant BACE-1 inhibitor (IC50 = 17 nM). NB-216 has a strong inhibitory effect on cathepsin D (IC50 = 1 nM) and cathepsin E (IC50 = 0.4 nM). NB-216 can be used for the study of Alzheimer's disease.
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TB-9
0 ImagesCat. No.: HY-164956CAS No.: 1415033-91-8TB-9, a Tasiamide B (HY-N15154) derivative, is a potent cathepsin D, cathepsin E, and BACE1 inhibitor with IC50s of 0.0783 nM, 0.724 nM, and 54.2 nM, respectively.
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TB-11
0 ImagesTB-11 is a Cathepsin D inhibitor, with IC50s of 0.126 nM (Cathepsin D), 1.92 nM (Cathepsin E), 48.8 nM (BACE1), respectively. TB-11 can be used for tumor research.
