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Yang Zhou
University of Arizona
ReceptorChemistryMelanocortin receptorMelanocortinBiochemistry
11Publications
2H-index
11Citations
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Publications 11
Newest
#1Yang ZhouH-Index: 2
#2Abid H. BandayH-Index: 7
Last. Minying CaiH-Index: 20
view all 4 authors...
Cancer vaccine is a promising immunotherapeutic approach to train the immune system with vaccines to recognize and eliminate tumors. Adjuvants are compounds that are necessary in cancer vaccines to mimic an infection process and amplify immune responses. The Toll-like receptor 2 and 6 (TLR2/TLR6) agonist dipalmitoyl-S-glyceryl cysteine (Pam2Cys) was demonstrated as an ideal candidate for synthetic vaccine adjuvants. However, the synthesis of Pam2Cys requires expensive N-protected cysteine as a k...
1 CitationsSource
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#1Saghar Mowlazadeh Haghighi (UA: University of Arizona)H-Index: 3
#2Yang Zhou (UA: University of Arizona)H-Index: 2
Last. Minying Cai (UA: University of Arizona)H-Index: 20
view all 6 authors...
Abstract Melanoma skin cancer is the fastest growing cancer in the US [1]. A great need exists for improved formulations and mechanisms to prevent and protect human skin from cancers and other skin damage caused by sunlight exposure. Current efforts to prevent UV damage to human skin, which in many cases leads to melanoma and other skin cancers. The primordial melanocortin-1 receptor (MC1R) is involved in regulating skin pigmentation and hair color, which is a natural prevention from UV damage. ...
2 CitationsSource
#1Thomas Durek (UQ: University of Queensland)H-Index: 17
#2Philipp M. Cromm (TUM: Technische Universität München)H-Index: 1
Last. David J. Craik (UQ: University of Queensland)H-Index: 82
view all 21 authors...
Ultrastable cyclic peptide frameworks offer great potential for drug design due to their improved bioavailability compared to their linear analogues. Using the sunflower trypsin inhibitor-1 (SFTI-1) peptide scaffold in combination with systematic N-methylation of the grafted pharmacophore led to the identification of novel subtype selective melanocortin receptor (MCR) agonists. Multiple bicyclic peptides were synthesized and tested toward their activity at MC1R and MC3–5R. Double N-methylated co...
5 CitationsSource
#1Francesco Merlino (University of Naples Federico II)H-Index: 9
#2Yang Zhou (UA: University of Arizona)H-Index: 2
Last. Victor J. Hruby (UA: University of Arizona)H-Index: 78
view all 12 authors...
We report the development of macrocyclic melanocortin derivatives of MT-II and SHU-9119, achieved by modifying the cycle dimension and incorporating constrained amino acids in ring-closing. This study culminated in the discovery of novel agonists/antagonists with an unprecedented activity profile by adding pieces to the puzzle of the melanocortin receptor selectivity. Finally, the resulting 19- and 20-membered rings represent a suitable frame for the design of further therapeutic ligands as sele...
Source
#1Minying CaiH-Index: 20
#3Yang ZhouH-Index: 2
Last. Jixun DaiH-Index: 1
view all 6 authors...
Source
#1Yang Zhou (UA: University of Arizona)H-Index: 2
#2Saghar Mowlazadeh Haghighi (UA: University of Arizona)H-Index: 3
Last. Minying CaiH-Index: 20
view all 6 authors...
Melanoma is a lethal form of skin cancer. Skin pigmentation, which is regulated by the melanocortin 1 receptor (MC1R), is an effective protection against melanoma. However, the endogenous MC1R agonists lack selectivity for the MC1R and thus can have side effects. The use of non-canonical amino acids in previous MC1R ligand development raises safety concerns. Here we report the development of the first potent and selective hMC1R agonist with only canonical amino acids. Using γ-MSH as a template, ...
3 CitationsSource
#1Yang Zhou (UA: University of Arizona)H-Index: 2
#2Minying Cai (UA: University of Arizona)H-Index: 20
ABSTRACTIntroduction: The melanocortin system is a primordial and critical system for survival, involved in a wide variety of physiological functions. It includes melanocortin receptors (MCRs) and melanotropin ligands (MCLs). MCRs are important drug targets that can regulate several key physiological processes. Extensive efforts have been made to develop peptide and peptidomimetics targeting melanocortin receptors including MC1R, MC3R, MC4R and MC5R. Most research is focused on developing potent...
1 CitationsSource
#2Minying CaiH-Index: 20
Last. Victor J. HrubyH-Index: 78
view all 5 authors...
Skin pigmentation shows substantial variation within human populations and within regional groupings or races. High levels of UVR can lead to skin damage such as sunburn or skin cancer, as well as the breakdown of folic acid. Melanin provides some protection from UVR induced damage [1]. MC1-R has a well-defined role in the regulation of skin pigmentation, provides protection against damaging and mutagenic effects of UV radiation (skin cancer) and has been recently implicated in the control of in...
Source
#1Yang ZhouH-Index: 2
#2Abid H. BandayH-Index: 7
Last. Victor J. HrubyH-Index: 2
view all 4 authors...
Synthetic vaccines use synthetic molecules as antigens for vaccination. Since real pathogens are no longer needed in synthetic vaccines, they are considered safer than the traditional inactivated or attenuated vaccines. The development of synthetic vaccines can be achieved on the genome sequence of the pathogen, which is much more efficient than the traditional way of sampling pathogens from the outbreak and grow cultures. Despite these advantages, the development of synthetic vaccines is hinder...
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