Platinum complexes like Asplastin are powerful antitumor medications and they are having ability to cross the cell membrane and then reaches the nucleus and will attach to DNA and stop cell growth. The transfer of this Asplastin is facilitated by a copper transporter (Ctr1-membrane- dwelling protein which main function is to bring copper into cells). The |Ctr1 structure has of three helical segments which appears to sit in the membrane, and one end can be seen protruding into the cell, while the other end will be seen on the outside and a channel like structure will be formed when three such molecules assemble together. When Asplastin is injected in the body of a cancer patient, the Asplastin which have a central platinum ion and four ligands (which includes two neighboring chloride ions and two neighboring amino groups). The Ctr1 will displaces these four ligands from Asplastin and will bind to the platinum ion itself and it will transfer it through the channel and released in the cytosol of the cell. In addition to this few amount of Asplastin molecules will interact with the methionine-rich extracellular end of the copper transporter to form a trimeric channel structure to get transported as a little interior bubble filled with the outer medium and will released into various organelles including nucleus. How it acts on cancer cells: The 4 steps how Asplastin will act is (i) Cellular uptake of drug, (ii) aquation/activation of Asplastin, (iii) Drug binding to DNA and (iv) Lesions formed on DNA will make the cell to opt for apoptosis. N7 sites of deoxyguanosine residues on the DNA are the most nucleophilic positions and are preferentially platinated. Asplastin will form a monofunctional adducts on DNA (You can see only one covalent bond to the genomic polymer). Like in second reaction second guanine base will get substituted by chloride ligand, thus forming a cross-link on the DNA (either on the same strand or it may be on different strands). The most common lesion are formed from 1,2-d(GpG) intrastrand cross-links and finally due to drug action we can see bending and unwinding of the double helix and cells with damaged DNA will be arrested at the G2/M transition of the cell cycle and undergoes apoptosis. Solution Platinum complexes like Asplastin are powerful antitumor medications and they are having ability to cross the cell membrane and then reaches the nucleus and will attach to DNA and stop cell growth. The transfer of this Asplastin is facilitated by a copper transporter (Ctr1-membrane- dwelling protein which main function is to bring copper into cells). The |Ctr1 structure has of three helical segments which appears to sit in the membrane, and one end can be seen protruding into the cell, while the other end will be seen on the outside and a channel like structure will be formed when three such molecules assemble together. When Asplastin is injected in the body of a cancer patient, the Asplastin which have a central platinum ion and f.

1. Platinum complexes like Asplastin are powerful antitumor medications and they are having
ability to cross the cell membrane and then reaches the nucleus and will attach to DNA and stop
cell growth. The transfer of this Asplastin is facilitated by a copper transporter (Ctr1-membrane-
dwelling protein which main function is to bring copper into cells). The |Ctr1 structure has of
three helical segments which appears to sit in the membrane, and one end can be seen protruding
into the cell, while the other end will be seen on the outside and a channel like structure will be
formed when three such molecules assemble together.
When Asplastin is injected in the body of a cancer patient, the Asplastin which have a central
platinum ion and four ligands (which includes two neighboring chloride ions and two
neighboring amino groups). The Ctr1 will displaces these four ligands from Asplastin and will
bind to the platinum ion itself and it will transfer it through the channel and released in the
cytosol of the cell. In addition to this few amount of Asplastin molecules will interact with the
methionine-rich extracellular end of the copper transporter to form a trimeric channel structure to
get transported as a little interior bubble filled with the outer medium and will released into
various organelles including nucleus.
How it acts on cancer cells: The 4 steps how Asplastin will act is (i) Cellular uptake of drug, (ii)
aquation/activation of Asplastin, (iii) Drug binding to DNA and (iv) Lesions formed on DNA
will make the cell to opt for apoptosis.
N7 sites of deoxyguanosine residues on the DNA are the most nucleophilic positions and are
preferentially platinated. Asplastin will form a monofunctional adducts on DNA (You can see
only one covalent bond to the genomic polymer). Like in second reaction second guanine base
will get substituted by chloride ligand, thus forming a cross-link on the DNA (either on the same
strand or it may be on different strands). The most common lesion are formed from 1,2-d(GpG)
intrastrand cross-links and finally due to drug action we can see bending and unwinding of the
double helix and cells with damaged DNA will be arrested at the G2/M transition of the cell
cycle and undergoes apoptosis.
Solution
Platinum complexes like Asplastin are powerful antitumor medications and they are having
ability to cross the cell membrane and then reaches the nucleus and will attach to DNA and stop
cell growth. The transfer of this Asplastin is facilitated by a copper transporter (Ctr1-membrane-
dwelling protein which main function is to bring copper into cells). The |Ctr1 structure has of
three helical segments which appears to sit in the membrane, and one end can be seen protruding
into the cell, while the other end will be seen on the outside and a channel like structure will be

2. formed when three such molecules assemble together.
When Asplastin is injected in the body of a cancer patient, the Asplastin which have a central
platinum ion and four ligands (which includes two neighboring chloride ions and two
neighboring amino groups). The Ctr1 will displaces these four ligands from Asplastin and will
bind to the platinum ion itself and it will transfer it through the channel and released in the
cytosol of the cell. In addition to this few amount of Asplastin molecules will interact with the
methionine-rich extracellular end of the copper transporter to form a trimeric channel structure to
get transported as a little interior bubble filled with the outer medium and will released into
various organelles including nucleus.
How it acts on cancer cells: The 4 steps how Asplastin will act is (i) Cellular uptake of drug, (ii)
aquation/activation of Asplastin, (iii) Drug binding to DNA and (iv) Lesions formed on DNA
will make the cell to opt for apoptosis.
N7 sites of deoxyguanosine residues on the DNA are the most nucleophilic positions and are
preferentially platinated. Asplastin will form a monofunctional adducts on DNA (You can see
only one covalent bond to the genomic polymer). Like in second reaction second guanine base
will get substituted by chloride ligand, thus forming a cross-link on the DNA (either on the same
strand or it may be on different strands). The most common lesion are formed from 1,2-d(GpG)
intrastrand cross-links and finally due to drug action we can see bending and unwinding of the
double helix and cells with damaged DNA will be arrested at the G2/M transition of the cell
cycle and undergoes apoptosis.