A Conjugate, having the structure as set forth in Formula: including pharmaceutically-acceptable salts, hydrates, solvates and metal chelates of the compound represented by the structure as set forth in Formula, and solvates and hydrates of the salts, wherein: D is the drug to be delivered across biological membranes, selected from a group consisting of a peptide, a protein, and a native or modified, single-stranded or double-stranded DNA or RNA, siRNA or ASO; y, z and w are each an integer, independently selected from 0, 1, 2, 3, 4, 5 or 6, wherein whenever the integer is 0, it means that the respective E moiety is null; at least one of y, z or w is different from 0; E, E', or E" can be the same or different, each having independently a structure as set forth in general Formula: including pharmaceutically acceptable salts, hydrates, solvates and metal chelates of the compound represented by the structure as set forth in Formula, and solvates and hydrates of the salts, wherein: G 1, G 2, G 3 and G 4 are each independently selected from the group consisting of hydrogen, methyl or ethyl; at least two G groups are hydrogen; Z and Z' are each independently selected from the group consisting of null; -CH 2; -NH-; - N(R')-; -C (CH 2) n [N(R")(R′′′)]-; -N(R')-C -C (CH 2) n [N(R")(R′′′)]-; wherein each of R', R" and R′′′ is independently selected from the group consisting of hydrogen, C 1, C 2, C 3, C 4 alkyl; or C 1, C 2, C 3, C 4 alkyl amine, wherein the amine is a primary, secondary or tertiary amine; n stands for an integer of 0, 1, 2, 3, 4; wherein n =0 means null; at least one of Z or Z' is an amine; L is a linker, selected from null; ether; amide; ester; carbonate; carbamate group(s); one or two hydrocarbon chains, each comprising 1-4 carbon atoms, being optionally-substituted by hydroxyl or amine group(s); or any combination thereof; K is selected from null, -CH- and -N-; a is an integer, selected from the group consisting of 0, 1, 2, 3 and 4; b is an integer, selected from the group consisting of 0, 1, 2, 3 and 4; c is an integer, selected from the group consisting of 1, 2, 3 and 4; d is an integer, selected from the group consisting of 2, 3 and 4; e, f are each an integer, selected independently form the group consisting of 0, 1, 2 and 3; and ∗ is a linkage point to D. D is the drug to be delivered across biological membranes, selected from a group consisting of a peptide, a protein, and a native or modified, single-stranded or double-stranded DNA or RNA, siRNA or ASO; y, z and w are each an integer, independently selected from 0, 1, 2, 3, 4, 5 or 6, wherein whenever the integer is 0, it means that the respective E moiety is null; at least one of y, z or w is different from 0; E, E', or E" can be the same or different, each having independently a structure as set forth in general Formula: including pharmaceutically acceptable salts, hydrates, solvates and metal chelates of the compound represented by the structure as set forth in Formula, and solvates and hydrates of the salts, wherein: G 1, G 2, G 3 and G 4 are each independently selected from the group consisting of hydrogen, methyl or ethyl; at least two G groups are hydrogen; Z and Z' are each independently selected from the group consisting of null; -CH 2; -NH-; - N(R')-; -C (CH 2) n [N(R")(R′′′)]-; -N(R')-C -C (CH 2) n [N(R")(R′′′)]-; wherein each of R', R" and R′′′ is independently selected from the group consisting of hydrogen, C 1, C 2, C 3, C 4 alkyl; or C 1, C 2, C 3, C 4 alkyl amine, wherein the amine is a primary, secondary or tertiary amine; n stands for an integer of 0, 1, 2, 3, 4; wherein n =0 means null; at least one of Z or Z' is an amine; L is a linker, selected from null; ether; amide; ester; carbonate; carbamate group(s); one or two hydrocarbon chains, each comprising 1-4 carbon atoms, being optionally-substituted by hydroxyl or amine group(s); or any combination thereof; K is selected from null, -CH- and -N-; a is an integer, selected from the group consisting of 0, 1, 2, 3 and 4; b is an integer, selected from the group consisting of 0, 1, 2, 3 and 4; c is an integer, selected from the group consisting of 1, 2, 3 and 4; d is an integer, selected from the group consisting of 2, 3 and 4; e, f are each an integer, selected independently form the group consisting of 0, 1, 2 and 3; and ∗ is a linkage point to D. G 1, G 2, G 3 and G 4 are each independently selected from the group consisting of hydrogen, methyl or ethyl; at least two G groups are hydrogen; Z and Z' are each independently selected from the group consisting of null; -CH 2; -NH-; - N(R')-; -C (CH 2) n [N(R")(R′′′)]-; -N(R')-C -C (CH 2) n [N(R")(R′′′)]-; wherein each of R', R" and R′′′ is independently selected from the group consisting of hydrogen, C 1, C 2, C 3, C 4 alkyl; or C 1, C 2, C 3, C 4 alkyl amine, wherein the amine is a primary, secondary or tertiary amine; n stands for an integer of 0, 1, 2, 3, 4; wherein n =0 means null; at least one of Z or Z' is an amine; L is a linker, selected from null; ether; amide; ester; carbonate; carbamate group(s); one or two hydrocarbon chains, each comprising 1-4 carbon atoms, being optionally-substituted by hydroxyl or amine group(s); or any combination thereof; K is selected from null, -CH- and -N-; a is an integer, selected from the group consisting of 0, 1, 2, 3 and 4; b is an integer, selected from the group consisting of 0, 1, 2, 3 and 4; c is an integer, selected from the group consisting of 1, 2, 3 and 4; d is an integer, selected from the group consisting of 2, 3 and 4; e, f are each an integer, selected independently form the group consisting of 0, 1, 2 and 3; and ∗ is a linkage point to D.