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author:

Kamkaew, Anyanee (Kamkaew, Anyanee.) [1] | Fu, Nanyan (Fu, Nanyan.) [2] (Scholars:傅南雁) | Cai, Weibo (Cai, Weibo.) [3] | Burgess, Kevin (Burgess, Kevin.) [4]

Indexed by:

Scopus SCIE

Abstract:

Actively targeting probe 1b, an unsymmetrical bivalent dipeptide mimic, selectively bound melanoma over healthy skin tissue in histological samples from patients and Sinclair swine. Modifications to 1b gave agents 2-4 that contain a near-IR aza-BODIPY fluor. Contrary to our expectations, symmetrical probe 3 gave the highest melanoma-to-healthy skin selectivity in histochemistry and experiments with live cells; this was surprising because 2, not 3, is unsymmetrical like the original lead 1. Optical imaging of 3 in a mouse melanoma model failed to show tumor accumulation in vivo, but the probe did selectively accumulate in the tumor (some in lung and less in the liver) as proven by analysis of the organs post mortem.

Keyword:

cancer melanoma small molecule ligand Targeting

Community:

  • [ 1 ] [Kamkaew, Anyanee]Texas A&M Univ, Dept Chem, Box 30012, College Stn, TX 77842 USA
  • [ 2 ] [Fu, Nanyan]Texas A&M Univ, Dept Chem, Box 30012, College Stn, TX 77842 USA
  • [ 3 ] [Burgess, Kevin]Texas A&M Univ, Dept Chem, Box 30012, College Stn, TX 77842 USA
  • [ 4 ] [Kamkaew, Anyanee]Univ Wisconsin, Dept Radiol, Madison, WI 53705 USA
  • [ 5 ] [Cai, Weibo]Univ Wisconsin, Dept Radiol, Madison, WI 53705 USA
  • [ 6 ] [Fu, Nanyan]Fuzhou Univ, Dept Chem, Fuzhou 350116, Peoples R China
  • [ 7 ] [Burgess, Kevin]Univ Malaya, Fac Med, Dept Pharmacol, Kuala Lumpur 50603, Malaysia
  • [ 8 ] [Cai, Weibo]Univ Wisconsin, Carbone Canc Ctr, Madison, WI 53705 USA

Reprint 's Address:

  • [Burgess, Kevin]Texas A&M Univ, Dept Chem, Box 30012, College Stn, TX 77842 USA;;[Burgess, Kevin]Univ Malaya, Fac Med, Dept Pharmacol, Kuala Lumpur 50603, Malaysia

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Source :

ACS MEDICINAL CHEMISTRY LETTERS

ISSN: 1948-5875

Year: 2017

Issue: 2

Volume: 8

Page: 179-184

3 . 7 9 4

JCR@2017

3 . 5 0 0

JCR@2023

ESI Discipline: CHEMISTRY;

ESI HC Threshold:226

JCR Journal Grade:1

CAS Journal Grade:2

Cited Count:

WoS CC Cited Count: 11

SCOPUS Cited Count: 11

ESI Highly Cited Papers on the List: 0 Unfold All

WanFang Cited Count:

Chinese Cited Count:

30 Days PV: 1

Online/Total:1/10106845
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